CHDI-390576
Based on 1 publication(s) in Google Scholar
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.
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- Purity: 98.10%
- CAS No.: 1629729-98-1
- 화학식: C19H13F4N3O2
- 분자량:391.32
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보관:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) CHDI-390576
More
Biological Activity
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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) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A549 | IC50 |
>30 μM
Compound: 22
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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
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[PMID: 30463802] |
| A549 | IC50 |
17 μM
Compound: 22
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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
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[PMID: 30463802] |
| CAL-27 | IC50 |
12.8 μM
Compound: CHDI0039
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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
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[PMID: 37979441] |
| CAL-27 | IC50 |
9.69 μM
Compound: CHDI0039
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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
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[PMID: 37979441] |
| HEK293 | IC50 |
6.2 μM
Compound: 22
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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
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[PMID: 30463802] |
| Jurkat | IC50 |
>50 μM
Compound: 22
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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
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[PMID: 30463802] |
| Jurkat | IC50 |
0.069 μM
Compound: 22
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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
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[PMID: 30463802] |
| Jurkat | IC50 |
0.069 μM
Compound: 22
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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
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[PMID: 30463802] |
| Sf9 | IC50 |
>50 μM
Compound: 22
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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
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[PMID: 30463802] |
| Sf9 | IC50 |
0.031 μM
Compound: 22
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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
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[PMID: 30463802] |
| Sf9 | IC50 |
0.05 μM
Compound: 22
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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
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[PMID: 30463802] |
| Sf9 | IC50 |
0.06 μM
Compound: 22
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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
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[PMID: 30463802] |
| Sf9 | IC50 |
39.7 μM
Compound: 22
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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
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[PMID: 30463802] |
| Sf9 | IC50 |
9.1 μM
Compound: 22
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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
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[PMID: 30463802] |
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.
Chemical Information
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CAS No. 1629729-98-1
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Appearance Solid
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분자량 391.32
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화학식 C19H13F4N3O2
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Color White to off-white
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SMILES
O=C(NO)C(C1=C(F)C=CC=C1)C2=CC=C(C3=NC=C(C(F)(F)F)C=N3)C=C2
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Synonyms
CHDI00390576
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Publications (1)
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Journal Impact Factor
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Most Recent
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Adv Sci (Weinh)
The Probiotic Parabacteroides johnsonii Ameliorates Metabolic Disorders Through Promoting BCAAs to BSCFAs Conversion. [Abstract]2025 Aug 7:e02624. PMID: 40772426
용액&용해도
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
순도&문서
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Data Sheet (274 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
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.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.5555 mL | 12.7773 mL | 25.5545 mL | 63.8863 mL |
| 5 mM | 0.5111 mL | 2.5555 mL | 5.1109 mL | 12.7773 mL | |
| 10 mM | 0.2555 mL | 1.2777 mL | 2.5555 mL | 6.3886 mL | |
| 15 mM | 0.1704 mL | 0.8518 mL | 1.7036 mL | 4.2591 mL | |
| 20 mM | 0.1278 mL | 0.6389 mL | 1.2777 mL | 3.1943 mL | |
| 25 mM | 0.1022 mL | 0.5111 mL | 1.0222 mL | 2.5555 mL | |
| 30 mM | 0.0852 mL | 0.4259 mL | 0.8518 mL | 2.1295 mL | |
| 40 mM | 0.0639 mL | 0.3194 mL | 0.6389 mL | 1.5972 mL | |
| 50 mM | 0.0511 mL | 0.2555 mL | 0.5111 mL | 1.2777 mL | |
| 60 mM | 0.0426 mL | 0.2130 mL | 0.4259 mL | 1.0648 mL | |
| 80 mM | 0.0319 mL | 0.1597 mL | 0.3194 mL | 0.7986 mL | |
| 100 mM | 0.0256 mL | 0.1278 mL | 0.2555 mL | 0.6389 mL |
CHDI-390576 Related Classifications
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