fr en

Réactifs et instruments pour l'immunologie, la biologie cellulaire et la biologie moléculaire.

Adezmapimod [152121-47-6]

Imprimer

Référence HY-10256-10mg

Conditionnement : 10mg

Contactez votre distributeur local :

Téléphone : +1 850 650 7790

Marque : MedChemExpress

Demander plus d'informations

Contactez votre distributeur local :

Téléphone : +1 850 650 7790

Description

Adezmapimod (SB 203580) is a selective and ATP-competitive p38 MAPK inhibitor with IC₅₀s of 50 nM and 500 nM for SAPK2a/p38 and SAPK2b/p38β2, respectively. Adezmapimod inhibits LCK, GSK3β and PKBα with IC₅₀s of 100-500-fold higher than that for SAPK2a/p38. Adezmapimod can inhibit p38 MAPK and lead to the inhibition of downstream HSP27 phosphorylation. Adezmapimod does not disrupt JNK activity and is an autophagy and mitophagy activator^[1]^[2]^[3].

IC₅₀ & Target^[1]

p38

50 nM (IC₅₀)

p38β2

500 nM (IC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
BMDC	IC₅₀	3.45 μM Compound: SB203580	Antiinflammatory activity in C57BL/6 mouse BMDCs assessed as inhibition of LPS-stimulated IL12 production treated 1 hr before LPS challenge measured 18 hrs post stimulation by ELISA Antiinflammatory activity in C57BL/6 mouse BMDCs assessed as inhibition of LPS-stimulated IL12 production treated 1 hr before LPS challenge measured 18 hrs post stimulation by ELISA	[PMID: 23484668]
BMDC	IC₅₀	3.5 μM Compound: SB203580	Antiinflammatory activity in C57BL/6 mouse BMDC cells assessed as inhibition of LPS-induced IL-6 production preincubated for 1 hr prior to LPS-stimulation measured after 18 hrs by ELISA Antiinflammatory activity in C57BL/6 mouse BMDC cells assessed as inhibition of LPS-induced IL-6 production preincubated for 1 hr prior to LPS-stimulation measured after 18 hrs by ELISA	[PMID: 24047259]
BMDC	IC₅₀	3.5 μM Compound: SB203580	Anti-inflammatory activity in C57BL/6 mouse BMDC assessed as inhibition of LPS-induced IL-6 production pretreated for 1 hr followed by LPS-stimulation after 18 hrs by ELISA Anti-inflammatory activity in C57BL/6 mouse BMDC assessed as inhibition of LPS-induced IL-6 production pretreated for 1 hr followed by LPS-stimulation after 18 hrs by ELISA	[PMID: 28009172]
BMDC	IC₅₀	3.53 μM Compound: SB203580	Antiinflammatory activity in C57BL/6 mouse BMDC assessed as inhibition of LPS-stimulated IL-6 production preincubated for 1 hr before LPS-stimulation measured after 16 hrs by ELISA Antiinflammatory activity in C57BL/6 mouse BMDC assessed as inhibition of LPS-stimulated IL-6 production preincubated for 1 hr before LPS-stimulation measured after 16 hrs by ELISA	[PMID: 22071304]
BMDC	IC₅₀	3.56 μM Compound: SB203580	Antiinflammatory activity against in C57BL/6 mouse BMDC assessed as inhibition of LPS-stimulated IL6 production compound pre-incubated for 1 hr before LPS challenge by ELISA Antiinflammatory activity against in C57BL/6 mouse BMDC assessed as inhibition of LPS-stimulated IL6 production compound pre-incubated for 1 hr before LPS challenge by ELISA	[PMID: 23200246]
BMDC	IC₅₀	5 μM Compound: SB203580	Antiinflammatory activity in wild-type C57BL/6 mouse BMDCs assessed as inhibition of IL-12 p40 production incubated for 1 hr prior to LPS challenge measured after 16 hrs by ELISA Antiinflammatory activity in wild-type C57BL/6 mouse BMDCs assessed as inhibition of IL-12 p40 production incubated for 1 hr prior to LPS challenge measured after 16 hrs by ELISA	[PMID: 23395633]
BMDC	IC₅₀	5 μM Compound: SB203580	Antiinflammatory activity in C57BL/6 mouse BMDC cells assessed as inhibition of LPS-induced IL-12 p40 production preincubated for 1 hr prior to LPS-stimulation measured after 18 hrs by ELISA Antiinflammatory activity in C57BL/6 mouse BMDC cells assessed as inhibition of LPS-induced IL-12 p40 production preincubated for 1 hr prior to LPS-stimulation measured after 18 hrs by ELISA	[PMID: 24047259]
BMDC	IC₅₀	5 μM Compound: SB203580	Anti-inflammatory activity in C57BL/6 mouse BMDC assessed as inhibition of LPS-induced IL12 p40 production pretreated for 1 hr followed by LPS-stimulation after 18 hrs by ELISA Anti-inflammatory activity in C57BL/6 mouse BMDC assessed as inhibition of LPS-induced IL12 p40 production pretreated for 1 hr followed by LPS-stimulation after 18 hrs by ELISA	[PMID: 28009172]
BMDC	IC₅₀	5.02 μM Compound: SB203580	Antiinflammatory activity in C57BL/6 mouse BMDC assessed as inhibition of LPS-stimulated IL-12p40 production preincubated for 1 hr before LPS-stimulation measured after 16 hrs by ELISA Antiinflammatory activity in C57BL/6 mouse BMDC assessed as inhibition of LPS-stimulated IL-12p40 production preincubated for 1 hr before LPS-stimulation measured after 16 hrs by ELISA	[PMID: 22071304]
BMDC	IC₅₀	5.21 μM Compound: SB203580	Antiinflammatory activity in C57BL/6 mouse BMDCs assessed as inhibition of LPS-stimulated IL-12p40 production treated 1 hr before LPS challenge measured 18 hrs post stimulation by ELISA Antiinflammatory activity in C57BL/6 mouse BMDCs assessed as inhibition of LPS-stimulated IL-12p40 production treated 1 hr before LPS challenge measured 18 hrs post stimulation by ELISA	[PMID: 23484668]
BMDC	IC₅₀	5.67 μM Compound: SB203580	Antiinflammatory activity against in C57BL/6 mouse BMDC assessed as inhibition of LPS-stimulated IL12 production compound pre-incubated for 1 hr before LPS challenge by ELISA Antiinflammatory activity against in C57BL/6 mouse BMDC assessed as inhibition of LPS-stimulated IL12 production compound pre-incubated for 1 hr before LPS challenge by ELISA	[PMID: 23200246]
BMDC	IC₅₀	7.2 μM Compound: SB203580	Anti-inflammatory activity in C57BL/6 mouse BMDC assessed as inhibition of LPS-induced TNFalpha production pretreated for 1 hr followed by LPS-stimulation after 18 hrs by ELISA Anti-inflammatory activity in C57BL/6 mouse BMDC assessed as inhibition of LPS-induced TNFalpha production pretreated for 1 hr followed by LPS-stimulation after 18 hrs by ELISA	[PMID: 28009172]
BMDC	IC₅₀	7.24 μM Compound: SB203580	Antiinflammatory activity in C57BL/6 mouse BMDC assessed as inhibition of LPS-stimulated TNF-alpha production preincubated for 1 hr before LPS-stimulation measured after 16 hrs by ELISA Antiinflammatory activity in C57BL/6 mouse BMDC assessed as inhibition of LPS-stimulated TNF-alpha production preincubated for 1 hr before LPS-stimulation measured after 16 hrs by ELISA	[PMID: 22071304]
BMDC	IC₅₀	7.37 μM Compound: SB203580	Antiinflammatory activity against in C57BL/6 mouse BMDC assessed as inhibition of LPS-stimulated TNFalpha production compound pre-incubated for 1 hr before LPS challenge by ELISA Antiinflammatory activity against in C57BL/6 mouse BMDC assessed as inhibition of LPS-stimulated TNFalpha production compound pre-incubated for 1 hr before LPS challenge by ELISA	[PMID: 23200246]
BMDC	IC₅₀	7.5 μM Compound: SB203580	Antiinflammatory activity in C57BL/6 mouse BMDC cells assessed as inhibition of LPS-induced TNFalpha production preincubated for 1 hr prior to LPS-stimulation measured after 18 hrs by ELISA Antiinflammatory activity in C57BL/6 mouse BMDC cells assessed as inhibition of LPS-induced TNFalpha production preincubated for 1 hr prior to LPS-stimulation measured after 18 hrs by ELISA	[PMID: 24047259]
BMDC	IC₅₀	7.53 μM Compound: SB203580	Antiinflammatory activity in C57BL/6 mouse BMDCs assessed as inhibition of LPS-stimulated TNF-alpha production treated 1 hr before LPS challenge measured 18 hrs post stimulation by ELISA Antiinflammatory activity in C57BL/6 mouse BMDCs assessed as inhibition of LPS-stimulated TNF-alpha production treated 1 hr before LPS challenge measured 18 hrs post stimulation by ELISA	[PMID: 23484668]
HEK293	EC₅₀	0.06 μM Compound: SB 203580	Inhibition of recombinant Nanoluc-tagged p38alpha (unknown origin) expressed in HEK293 cells incubated for 2 to 3 mins by NanoBRET assay Inhibition of recombinant Nanoluc-tagged p38alpha (unknown origin) expressed in HEK293 cells incubated for 2 to 3 mins by NanoBRET assay	[PMID: 31520926]
HEK293	IC₅₀	250 nM Compound: 2; SB-203580	Inhibition of RIP2K in MDP-stimulated HEK-293 cells over-expressing NOD2 assessed as IL8 secretion Inhibition of RIP2K in MDP-stimulated HEK-293 cells over-expressing NOD2 assessed as IL8 secretion	[PMID: 27109867]
HEK293	IC₅₀	6310 nM Compound: 2; SB-203580	Inhibition of RIP2K in Pam2CSK4-stimulated HEK-293 cells over-expressing TLR2 assessed as IL8 secretion Inhibition of RIP2K in Pam2CSK4-stimulated HEK-293 cells over-expressing TLR2 assessed as IL8 secretion	[PMID: 27109867]
HL-60	IC₅₀	50.5 μM Compound: SB-203580	Antiinflammatory activity in PMA-stimulated human HL60 cells assessed as inhibition of LPS-induced TNFalpha production preincubated for 30 mins before LPS challenge measured after 24 hrs by ELISA Antiinflammatory activity in PMA-stimulated human HL60 cells assessed as inhibition of LPS-induced TNFalpha production preincubated for 30 mins before LPS challenge measured after 24 hrs by ELISA	[PMID: 22621841]
HL-60	IC₅₀	52.2 μM Compound: SB-203580	Antiinflammatory activity in PMA-stimulated human HL60 cells assessed as inhibition of LPS-induced IL-6 production preincubated for 30 mins before LPS challenge measured after 24 hrs by ELISA Antiinflammatory activity in PMA-stimulated human HL60 cells assessed as inhibition of LPS-induced IL-6 production preincubated for 30 mins before LPS challenge measured after 24 hrs by ELISA	[PMID: 22621841]
HL-60	IC₅₀	52.2 μM Compound: SB203580	Antiinflammatory activity in human HL-60 derived macrophage-like cells assessed as inhibition of LPS-induced IL-6 production treated 30 mins before LPS stimulation measured after 24 hrs by ELISA Antiinflammatory activity in human HL-60 derived macrophage-like cells assessed as inhibition of LPS-induced IL-6 production treated 30 mins before LPS stimulation measured after 24 hrs by ELISA	[PMID: 23811089]
HL-60	IC₅₀	8.6 μM Compound: SB203580	Antiinflammatory activity in human HL-60 derived macrophage-like cells assessed as inhibition of LPS-induced TNFalpha production treated 30 mins before LPS stimulation measured after 24 hrs by ELISA Antiinflammatory activity in human HL-60 derived macrophage-like cells assessed as inhibition of LPS-induced TNFalpha production treated 30 mins before LPS stimulation measured after 24 hrs by ELISA	[PMID: 23811089]
HeLa	IC₅₀	0.1 μM Compound: SB-203580	Inhibition of Tat-induced HIV1 LTR transactivation in human HeLa cells assessed as CAT expression after 2 days Inhibition of Tat-induced HIV1 LTR transactivation in human HeLa cells assessed as CAT expression after 2 days	[PMID: 18926711]
L132	CC₅₀	> 10 μM Compound: 81; SB203580	Cytotoxicity against human L132 cells Cytotoxicity against human L132 cells	[PMID: 33539089]
PBMC	IC₅₀	0.34 μM Compound: SB-203580	Antiinflammatory activity in human PBMCs assessed as inhibition of LPS-induced IL1-beta release incubated for 15 mins prior to LPS challenge measured after 24 hrs by HTRF assay Antiinflammatory activity in human PBMCs assessed as inhibition of LPS-induced IL1-beta release incubated for 15 mins prior to LPS challenge measured after 24 hrs by HTRF assay	[PMID: 23411072]
PBMC	IC₅₀	1 μM Compound: SB-203580	Antiinflammatory activity in human PBMCs assessed as inhibition of LPS-induced TNFalpha release incubated for 15 mins prior to LPS challenge measured after 24 hrs by HTRF assay Antiinflammatory activity in human PBMCs assessed as inhibition of LPS-induced TNFalpha release incubated for 15 mins prior to LPS challenge measured after 24 hrs by HTRF assay	[PMID: 23411072]
PBMC	IC₅₀	160 nM Compound: 4	Inhibition of staphylococcal enterotoxin B(SEB) stimulated tumor necrosis factor alpha (TNF-alpha) production by human peripheral blood mononuclear cells(PBMCs) Inhibition of staphylococcal enterotoxin B(SEB) stimulated tumor necrosis factor alpha (TNF-alpha) production by human peripheral blood mononuclear cells(PBMCs)	[PMID: 9784093]
PBMC	IC₅₀	25 nM Compound: 4	Inhibition of LPS-stimulated TH+NF-alphs production by human peripheral blood mononuclear cells (PBMCs) Inhibition of LPS-stimulated TH+NF-alphs production by human peripheral blood mononuclear cells (PBMCs)	[PMID: 9784093]
PBMC	IC₅₀	48 nM Compound: 4	Inhibition of LPS-induced IL1-beta production in human peripheral blood mononuclear cells(PBMCs) Inhibition of LPS-induced IL1-beta production in human peripheral blood mononuclear cells(PBMCs)	[PMID: 9784093]
PBMC	IC₅₀	> 10 μM Compound: SB-203580	Antiinflammatory activity in human PBMCs assessed as inhibition of LPS-induced IL6 release incubated for 15 mins prior to LPS challenge measured after 24 hrs by HTRF assay Antiinflammatory activity in human PBMCs assessed as inhibition of LPS-induced IL6 release incubated for 15 mins prior to LPS challenge measured after 24 hrs by HTRF assay	[PMID: 23411072]
Peritoneal macrophage cell	IC₅₀	0.22 μM Compound: 10, SB-203580	Antiinflammatory activity in BALB/c mouse peritoneal macrophages assessed as inhibition of LPS-induced TNFalpha production treated 1 hr before LPS challenge measured after 24 hrs by ELISA Antiinflammatory activity in BALB/c mouse peritoneal macrophages assessed as inhibition of LPS-induced TNFalpha production treated 1 hr before LPS challenge measured after 24 hrs by ELISA	[PMID: 22647219]
Platelet	IC₅₀	200 nM Compound: K00038	Inhibition of collagen-induced human platelet aggregation Inhibition of collagen-induced human platelet aggregation	[PMID: 18077363]
RBL-1	IC₅₀	58 μM Compound: 2	Inhibitory activity against 5-lipoxygenase enzyme from RBL-1 cells Inhibitory activity against 5-lipoxygenase enzyme from RBL-1 cells	10.1016/0960-894X(95)00189-Z
SW1353	IC₅₀	0.05 μM Compound: 1	Compound was evaluated for its ability to inhibit IL-6 production in SW1353 cells treated with cytokines IL-1 and TNF Compound was evaluated for its ability to inhibit IL-6 production in SW1353 cells treated with cytokines IL-1 and TNF	[PMID: 10999467]
SW1353	IC₅₀	50 nM Compound: 1	Inhibition of TNF and IL-1 induced IL-6 production in human chondro-sarcoma SW 1353 cells Inhibition of TNF and IL-1 induced IL-6 production in human chondro-sarcoma SW 1353 cells	[PMID: 10999468]
SW1353	IC₅₀	50 nM Compound: 1	Inhibition of IL-6 production by SW1353 cells treated with both cytokines IL-1 and TNF-alpha. Inhibition of IL-6 production by SW1353 cells treated with both cytokines IL-1 and TNF-alpha.	[PMID: 11140741]
Sf9	IC₅₀	0.035 μM Compound: SB203580	Inhibition of recombinant human full-length N-terminal GST-tagged P38 alpha MAPK expressed in baculovirus infected Sf9 insect cells using p38 peptide as substrate preincubated for 15 mins followed by substrate addition and measured after 60 mins in presence of ATP by ADP-Glo kinase assay Inhibition of recombinant human full-length N-terminal GST-tagged P38 alpha MAPK expressed in baculovirus infected Sf9 insect cells using p38 peptide as substrate preincubated for 15 mins followed by substrate addition and measured after 60 mins in presence of ATP by ADP-Glo kinase assay	[PMID: 31445234]
Sf9	IC₅₀	10 nM Compound: 2, SB-203580	Inhibition of full-length FLAG-6His-TEV tagged human RIP2 expressed in Sf9 cells assessed as reduction in autophosphorylation pre-incubated for 30 mins followed by incubation with ATP for 2 hrs by ADP-Glo assay Inhibition of full-length FLAG-6His-TEV tagged human RIP2 expressed in Sf9 cells assessed as reduction in autophosphorylation pre-incubated for 30 mins followed by incubation with ATP for 2 hrs by ADP-Glo assay	[PMID: 26455654]
Sf9	IC₅₀	200 nM Compound: 2, SB-203580	Inhibition of full-length FLAG-6His-TEV tagged human RIP2 expressed in Sf9 cells by fluorescent polarization assay Inhibition of full-length FLAG-6His-TEV tagged human RIP2 expressed in Sf9 cells by fluorescent polarization assay	[PMID: 26455654]
THP-1	EC₅₀	60 nM Compound: 1	Inhibition of LPS-induced tumor necrosis factor-alpha (TNF-alpha) production in THP-1 cells Inhibition of LPS-induced tumor necrosis factor-alpha (TNF-alpha) production in THP-1 cells	[PMID: 12086485]
THP-1	IC₅₀	0.016 μM Compound: SB-203580	Inhibition of LPS-induced TNFalpha production in human THP1 cells Inhibition of LPS-induced TNFalpha production in human THP1 cells	[PMID: 18325768]
THP-1	IC₅₀	0.07 μM Compound: SB-203580	Inhibition of tumor necrosis factor alpha release by THP-1 cells Inhibition of tumor necrosis factor alpha release by THP-1 cells	[PMID: 15658855]
THP-1	IC₅₀	20 nM Compound: SB 203580	Inhibition of LPS-induced TNFalpha production in human THP1 cells incubated for 1 hr followed by LPS stimulation and measured after 4 hrs by TR-FRET method Inhibition of LPS-induced TNFalpha production in human THP1 cells incubated for 1 hr followed by LPS stimulation and measured after 4 hrs by TR-FRET method	[PMID: 31520926]
THP-1	IC₅₀	50 nM Compound: K00038	Inhibition of LPS-stimulated IL1 production in human THP1 cells Inhibition of LPS-stimulated IL1 production in human THP1 cells	[PMID: 18077363]
THP-1	IC₅₀	50 nM Compound: K00038	Inhibition of LPS-stimulated TNFalpha production in human THP1 cells Inhibition of LPS-stimulated TNFalpha production in human THP1 cells	[PMID: 18077363]
THP-1	IC₅₀	72 nM Compound: SB-203580	Inhibitory activity against TNF-alpha production using lipopolysaccharide stimulated human monocytic cells Inhibitory activity against TNF-alpha production using lipopolysaccharide stimulated human monocytic cells	[PMID: 12729637]
THP-1	IC₅₀	72 nM Compound: SB-203580	Inhibitory activity against LPS-stimulated TNF-alpha production in human monocytic cells (THP-1) Inhibitory activity against LPS-stimulated TNF-alpha production in human monocytic cells (THP-1)	[PMID: 15139749]
THP-1	IC₅₀	72 nM Compound: SB-203580	Inhibitory activity against lipopolysaccharide stimulated TNF-alpha production in THP-1 cells (human monocytic cells) Inhibitory activity against lipopolysaccharide stimulated TNF-alpha production in THP-1 cells (human monocytic cells)	[PMID: 15837310]
THP-1	IC₅₀	72 nM Compound: SB-203580	Inhibition of LPS-stimulated TNFalpha production in THP1 cells Inhibition of LPS-stimulated TNFalpha production in THP1 cells	[PMID: 16750367]
THP-1	IC₅₀	72 μM Compound: SB-203580	Concentration required to inhibit production of Tumor necrosis factor, alpha in LPS-stimulated human monocytic cells (THP-1) Concentration required to inhibit production of Tumor necrosis factor, alpha in LPS-stimulated human monocytic cells (THP-1)	[PMID: 15341957]

In Vitro

Adezmapimod (SB 203580) (preincubated with 0-30 μM for 1 h and cultured for 24 h in the presence of 20 ng/mL IL-2) prevents the IL-2-induced proliferation of primary human T cells, murine CT6 T cells, or BAF F7 B cells with an IC₅₀ of 3-5 μM^[1].
SB203580 blocks PKB phosphorylation (IC₅₀ 3-5 μM). SB203580 inhibitsthe phosphorylation of Ser473 in a dose-dependent manner in both CT6 and activated human T cells and IL-2-responsive BA/F3 F7 B cells^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay^[1]

Cell Line:	CT6, BA/F3 cell line F7, and PBMC/T cells
Concentration:	0-30 μM
Incubation Time:	Preincubated with 0-30 μM SB203580 for 1 h and cultured for 24 h in the presence of 20 ng/mL IL-2
Result:	Prevented the IL-2-induced proliferation of primary human T cells, murine CT6 T cells, or BAF F7 B cells with an IC₅₀ of 3-5 μM.

Western Blot Analysis^[1]

Cell Line:	CT6 cells, activated human T cells, and BA/F3 F7 cells
Concentration:	0-30 μM
Incubation Time:	Preincubated with 0-30 μM SB203580 for 1 h before stimulating with 20 ng/mL IL-2 for 5 min
Result:	Inhibited the phosphorylation of PKB at Ser473 in a dose-dependent manner.

In Vivo

Adezmapimod (SB 203580) (5 mg/kg/day; intra peritoneal injected daily for 16 consecutive days, in female atymic Nu/Nu mice) treatment, p38WT tumors show a significantly smaller tumor burden when compared with p38TM tumors that were treated in parallel^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Six-week-old female atymic Nu/Nu mice CAL27 p38WT and p38TM tumors^[1]
Dosage:	5 mg/kg/day
Administration:	Intra peritoneal injected daily for 16 consecutive days
Result:	After 2 weeks treatment, CAL27 p38WT tumors were significantly smaller; CAL27 p38TM tumors were not affected by the p38 inhibitor (n=10).

Masse moléculaire

377.43

Formule

C₂₁H₁₆FN₃OS

CAS No.

152121-47-6

Appearance

Solid

Color

White to light yellow

SMILES

O=S(C1=CC=C(C2=NC(C3=CC=C(F)C=C3)=C(C4=CC=NC=C4)N2)C=C1)C

Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvant et solubilité

In Vitro:

DMSO : 20 mg/mL (52.99 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.6495 mL	13.2475 mL	26.4950 mL
5 mM	0.5299 mL	2.6495 mL	5.2990 mL
10 mM	0.2649 mL	1.3247 mL	2.6495 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 5% DMSO 40% PEG300 5% Tween-80 50% Saline
Solubility: ≥ 2.5 mg/mL (6.62 mM); Clear solution
Protocol 2

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: 2 mg/mL (5.30 mM); Clear solution; Need ultrasonic

This protocol yields a clear solution of 2 mg/mL.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 3

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2 mg/mL (5.30 mM); Clear solution; Need ultrasonic

This protocol yields a clear solution of 2 mg/mL.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 4

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: 2 mg/mL (5.30 mM); Clear solution; Need ultrasonic

This protocol yields a clear solution of 2 mg/mL. If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.0 mg/mL) to 900 μL Corn oil, and mix evenly.
Protocol 5

Add each solvent one by one: 2% DMSO 40% PEG300 5% Tween-80 53% Saline
Solubility: ≥ 1 mg/mL (2.65 mM); Clear solution
Protocol 6

Add each solvent one by one: 2% DMSO 98% (20% SBE-β-CD in Saline)
Solubility: ≥ 1 mg/mL (2.65 mM); Clear solution

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 50% PEG300 50% Saline
Solubility: 10 mg/mL (26.49 mM); Suspended solution; Need ultrasonic
Protocol 2

Add each solvent one by one: 0.5% CMC-Na/saline water
Solubility: 16.67 mg/mL (44.17 mM); Suspended solution; Need ultrasonic

Pureté et documentation

Purity: 99.91%

Fiche technique (281 KB) SDS (393 KB)

COA (252 KB) HNMR (176 KB) LCMS (122 KB) Elemental Analysis Report (110 KB)

Instruction de manipulation (2659 KB)

Références

[1]. Davies SP, et al. Specificity and mechanism of action of some commonly used protein kinase inhibitors. Biochem J. 2000 Oct 1;351(Pt 1):95-105. [Content Brief]

[2]. Lali FV, et al. The pyridinyl imidazole inhibitor SB203580 blocks phosphoinositide-dependent protein kinase activity, protein kinase B phosphorylation, and retinoblastoma hyperphosphorylation in interleukin-2-stimulated T cells independently of p38 mitogen-activated protein kinase. J Biol Chem. 2000 Mar 10;275(10):7395-402. [Content Brief]

[3]. Leelahavanichkul K, et al. A role for p38 MAPK in head and neck cancer cell growth and tumor-induced angiogenesis and lymphangiogenesis. Mol Oncol. 2014 Feb;8(1):105-18. [Content Brief]

Vous serez peut-être également intéressé par les produits suivants :

Référence

Description

Cond.

Prix HT

HY-10492-5mg

Dinaciclib [779353-01-4]

5mg

HY-12057-50mg

Vemurafenib [918504-65-1]

50mg

HY-14660-10mg

Dabrafenib [1195765-45-7]

10mg

Adezmapimod [152121-47-6]

Référence HY-10256-10mg

Contactez votre distributeur local :

Marque : MedChemExpress

Contactez votre distributeur local :

Adezmapimod Related Antibodies

Vous serez peut-être également intéressé par les produits suivants :