Réactifs et instruments pour l'immunologie, la biologie cellulaire et la biologie moléculaire.
 
> CHDI-390576 [1629729-98-1]

CHDI-390576 [1629729-98-1]

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Référence HY-119939-5mg

Conditionnement : 5mg

Marque : MedChemExpress

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Description

CHDI-390576, a potent, cell permeable and CNS penetrant class IIa histone deacetylase (HDAC) inhibitor with IC50s of 54 nM, 60 nM, 31 nM, 50 nM for class IIa HDAC4, HDAC5, HDAC7, HDAC9, respectively, shows >500-fold selectivity over class I HDACs (1, 2, 3) and ~150-fold selectivity over HDAC8 and the class IIb HDAC6 isoform[1].

IC50 & Target[1]

HDAC4

54 nM (IC50)

HDAC5

60 nM (IC50)

HDAC7

31 nM (IC50)

hHDAC9

50 nM (IC50)

HDAC1

39.7 μM (IC50)

HDAC3

25.8 μM (IC50)

HDAC8

9.1 μM (IC50)

hHDAC6

6.2 μM (IC50)

Cellular Effect
Cell Line Type Value Description References
A549 IC50
>30 μM
Compound: 22
Inhibition of HDAC class 1 in human A549 cells using histone H4K12 as substrate measured after 4 hrs by Western blot analysis
Inhibition of HDAC class 1 in human A549 cells using histone H4K12 as substrate measured after 4 hrs by Western blot analysis
[PMID: 30463802]
A549 IC50
17 μM
Compound: 22
Inhibition of HDAC6 in human A549 cells using tubulin as substrate measured after 4 hrs by Western blot analysis
Inhibition of HDAC6 in human A549 cells using tubulin as substrate measured after 4 hrs by Western blot analysis
[PMID: 30463802]
CAL-27 IC50
12.8 μM
Compound: CHDI0039
Antiproliferative activity against human CAL-27 cells overexpressing HDAC4 assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
Antiproliferative activity against human CAL-27 cells overexpressing HDAC4 assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
[PMID: 37979441]
CAL-27 IC50
9.69 μM
Compound: CHDI0039
Antiproliferative activity against human CAL-27 cells without HDAC4 expression assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
Antiproliferative activity against human CAL-27 cells without HDAC4 expression assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
[PMID: 37979441]
HEK293 IC50
6.2 μM
Compound: 22
Inhibition of recombinant human HDAC6 expressed in HEK293 cells using Lys-Ac-AMC as substrate measured after 60 mins by fluorescence assay
Inhibition of recombinant human HDAC6 expressed in HEK293 cells using Lys-Ac-AMC as substrate measured after 60 mins by fluorescence assay
[PMID: 30463802]
Jurkat IC50
>50 μM
Compound: 22
Inhibition of HDAC class 1/2b in human Jurkat cells using Boc-Lys-Ac as substrate preincubated for 2 hrs followed by substrate addition and measured after 3 hrs by fluorescence assay
Inhibition of HDAC class 1/2b in human Jurkat cells using Boc-Lys-Ac as substrate preincubated for 2 hrs followed by substrate addition and measured after 3 hrs by fluorescence assay
[PMID: 30463802]
Jurkat IC50
0.069 μM
Compound: 22
Inhibition of HDAC class 2a in human Jurkat cells using Boc-Lys-TFA as substrate preincubated for 2 hrs followed by substrate addition and measured after 3 hrs by fluorescence assay
Inhibition of HDAC class 2a in human Jurkat cells using Boc-Lys-TFA as substrate preincubated for 2 hrs followed by substrate addition and measured after 3 hrs by fluorescence assay
[PMID: 30463802]
Jurkat IC50
0.069 μM
Compound: 22
Inhibition of HDAC class 2a/HDAC8 in human Jurkat cells using Boc-Lys-TFA as substrate preincubated for 2 hrs followed by substrate addition and measured after 3 hrs by fluorescence assay
Inhibition of HDAC class 2a/HDAC8 in human Jurkat cells using Boc-Lys-TFA as substrate preincubated for 2 hrs followed by substrate addition and measured after 3 hrs by fluorescence assay
[PMID: 30463802]
Sf9 IC50
>50 μM
Compound: 22
Inhibition of human full length C-terminal FLAG-tagged HDAC2 expressed in baculovirus infected Sf9 insect cells using Ac-Arg-Gly-Lys(Ac) as substrate measured after 60 mins by fluorescence assay
Inhibition of human full length C-terminal FLAG-tagged HDAC2 expressed in baculovirus infected Sf9 insect cells using Ac-Arg-Gly-Lys(Ac) as substrate measured after 60 mins by fluorescence assay
[PMID: 30463802]
Sf9 IC50
0.031 μM
Compound: 22
Inhibition of human N-terminal GST-tagged HDAC7 (518 to end residues) expressed in baculovirus infected Sf9 insect cells using Boc-Lys-TFA as substrate measured after 60 mins by fluorescence assay
Inhibition of human N-terminal GST-tagged HDAC7 (518 to end residues) expressed in baculovirus infected Sf9 insect cells using Boc-Lys-TFA as substrate measured after 60 mins by fluorescence assay
[PMID: 30463802]
Sf9 IC50
0.05 μM
Compound: 22
Inhibition of human C-terminal His-tagged HDAC9 (604 to 1066 residues) expressed in baculovirus infected Sf9 insect cells using Boc-Lys-TFA as substrate measured after 60 mins by fluorescence assay
Inhibition of human C-terminal His-tagged HDAC9 (604 to 1066 residues) expressed in baculovirus infected Sf9 insect cells using Boc-Lys-TFA as substrate measured after 60 mins by fluorescence assay
[PMID: 30463802]
Sf9 IC50
0.06 μM
Compound: 22
Inhibition of human C-terminal His-tagged HDAC5 catalytic domain (656 to 1122 residues) expressed in baculovirus infected Sf9 insect cells using Boc-Lys-TFA as substrate measured after 60 mins by fluorescence assay
Inhibition of human C-terminal His-tagged HDAC5 catalytic domain (656 to 1122 residues) expressed in baculovirus infected Sf9 insect cells using Boc-Lys-TFA as substrate measured after 60 mins by fluorescence assay
[PMID: 30463802]
Sf9 IC50
39.7 μM
Compound: 22
Inhibition of human full length C-terminal FLAG/His-tagged HDAC1 expressed in baculovirus infected Sf9 insect cells using Lys-Ac-AMC as substrate measured after 60 mins by fluorescence assay
Inhibition of human full length C-terminal FLAG/His-tagged HDAC1 expressed in baculovirus infected Sf9 insect cells using Lys-Ac-AMC as substrate measured after 60 mins by fluorescence assay
[PMID: 30463802]
Sf9 IC50
9.1 μM
Compound: 22
Inhibition of human full length C-terminal His-tagged HDAC8 expressed in baculovirus infected Sf9 insect cells using Boc-Lys-TFA as substrate measured after 60 mins by fluorescence assay
Inhibition of human full length C-terminal His-tagged HDAC8 expressed in baculovirus infected Sf9 insect cells using Boc-Lys-TFA as substrate measured after 60 mins by fluorescence assay
[PMID: 30463802]
In Vitro

The affinity (Kd) of CHDI-390576 to the catalytic domain of immobilized HDAC4 is 80 nM[1].
CHDI-390576 inhibits class I HDACs (1, 3, 8) and class IIb HDAC6 isoforms with IC50s of 39.7μM, 25.8 μM, 9.1 μM, 6.2 μM, respectively[1].

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

CHDI-390576 Related Antibodies

Solvant et solubilité
In Vitro: 

DMSO : 250 mg/mL (638.86 mM; Need ultrasonic; 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 2.5555 mL 12.7773 mL 25.5545 mL
5 mM 0.5111 mL 2.5555 mL 5.1109 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.08 mg/mL (5.32 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.08 mg/mL (5.32 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
Pureté et documentation
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