HDAC-IN-57
CAS No. 2716217-79-5
HDAC-IN-57( —— )
Catalog No. M36851 CAS No. 2716217-79-5
HDAC-IN-57 is an orally active pan-inhibitor of histone deacetylase (HDAC), inhibiting HDAC1, HDAC2, HDAC6, and HDAC8 with IC50 values of 2.07 nM, 4.71 nM, 2.4 nM, and 107 nM, respectively.
Purity : >98% (HPLC)
COA
Datasheet
HNMR
HPLC
MSDS
Handing Instructions
| Size | Price / USD | Stock | Quantity |
| 2MG | 296 | Get Quote |
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| 5MG | 409 | Get Quote |
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| 10MG | 604 | Get Quote |
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| 25MG | 908 | Get Quote |
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| 50MG | 1251 | Get Quote |
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| 100MG | 1647 | Get Quote |
|
| 500MG | 3312 | Get Quote |
|
| 1G | Get Quote | Get Quote |
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Biological Information
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Product NameHDAC-IN-57
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NoteResearch use only, not for human use.
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Brief DescriptionHDAC-IN-57 is an orally active pan-inhibitor of histone deacetylase (HDAC), inhibiting HDAC1, HDAC2, HDAC6, and HDAC8 with IC50 values of 2.07 nM, 4.71 nM, 2.4 nM, and 107 nM, respectively.
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DescriptionHDAC-IN-57 is an orally active inhibitor of histone deacetylases (HDAC), with IC50s of 2.07 nM, 4.71 nM, 2.4 nM and 107 nM for HDAC1, HDAC2, HDAC6, HDAC8, respectively. HDAC-IN-57 can inhibits LSD1, with IC50 of 1.34 μΜ.HDAC-IN-57 induces apoptosis, and has anti-tumor activity.
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In VitroWestern Blot Analysis Cell Line:MGC-803 cells, HCT-116 cells Concentration:1.5 μM Incubation Time:48 hours Result:Inhibited cellular LSD1 and HDACs. Upregulated the expression of apoptotic markers, including cytochrome C, Bax, cleaved caspase-3/7/9, and cleaved PARP, while downregulating the expression of anti-apoptotic protein Bcl-2. Apoptosis Analysis Cell Line:MGC-803 cells, HCT-116 cells Concentration:1.0 μM, 2.5 μM, 5.0 μM Incubation Time:48 hours Result:Triggered MGC-803 and HCT116 cells apoptosis in a dose-dependent manner.Induced about 55.4% and 51.5% MGC-803 cell apoptosis at a concentration of 5 μM.Cell Migration Assay Cell Line:MGC-803 cells, HCT-116 cells Concentration:1.0 μM, 2.0 μM, 4 μM Incubation Time:48 hours Result:Reduced the number of migrated of MGC-803 and HCT-116 cells. Inhibited the migration and invasion of cancer cells.Cell Cycle Analysis Cell Line:MGC-803 cells, HCT-116 cells Concentration:1.0 μM, 2.5 μM, 5.0 μM Incubation Time:48 hours Result:Induced G2/M cycle arrest in MGC-803 and HCT-116 cells.
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In Vivo——
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Synonyms——
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PathwayCell Cycle/DNA Damage
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TargetHDAC
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RecptorHDAC | Apoptosis
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Research Area——
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Indication——
Chemical Information
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CAS Number2716217-79-5
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Formula Weight377.39
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Molecular FormulaC21H19N3O4
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Purity>98% (HPLC)
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Solubility——
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SMILESC(NCC1=CC=C(C(NO)=O)C=C1)(=O)C=2C=C(N=CC2)C3=CC=C(OC)C=C3
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Chemical Name——
Shipping & Storage Information
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Storage(-20℃)
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ShippingWith Ice Pack
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Stability≥ 2 years
Reference
1. Duan Y, et al. Discovery of novel, potent, and orally bioavailable HDACs inhibitors with LSD1 inhibitory activity for the treatment of solid tumors. Eur J Med Chem. 2023 Jun 5;254:115367.?
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