2244714-37-0
Chemical Structure
HDAC/HSP90-IN-1
- CAS No.: 2244714-37-0
- Formula:C25H33N3O6
- Molecular Weight:471.55
IUPAC Name: N1-(4-(2,4-dihydroxy-5-isopropyl-N-methylbenzamido)phenyl)-N8-hydroxyoctanediamide
InChIKey: NRTQVEBKTMOYBI-UHFFFAOYSA-N
SMILES: O=C(NC1=CC=C(N(C(C2=CC(C(C)C)=C(O)C=C2O)=O)C)C=C1)CCCCCCC(NO)=O
Biological Activity: HDAC/HSP90-IN-1 (compound 20) is a potent dual inhibitor of HDAC (IC50 = 194 nM) and HSP90 (HSP90α IC50 = 153 nM). HDAC/HSP90-IN-1 induces HSP70 expression, downregulates HSP90 client proteins, and promotes acetylation of α-tubulin and histone H3 in cancer cells. HDAC/HSP90-IN-1 reduces PD-L1 expression in IFN-γ treated H1975 cells. HDAC/HSP90-IN-1 can be used for cancer research, such as lung and colon cancer[1].
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HDAC/HSP90-IN-1 | HDAC/HSP90-IN-1 (compound 20) is a potent dual inhibitor of HDAC (IC50 = 194 nM) and HSP90 (HSP90α IC50 = 153 nM). HDAC/HSP90-IN-1 induces HSP70 expression, downregulates HSP90 client proteins, and promotes acetylation of α-tubulin and histone H3 in cancer cells. HDAC/HSP90-IN-1 reduces PD-L1 expression in IFN-γ treated H1975 cells. HDAC/HSP90-IN-1 can be used for cancer research, such as lung and colon cancer. | |||||||||||||||||||||
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References
- [1]. Mehndiratta S, et al. N-alkyl-hydroxybenzoyl anilide hydroxamates as dual inhibitors of HDAC and HSP90, downregulating IFN-γ induced PD-L1 expression. Eur J Med Chem. 2020 Jan 1;185:111725. doi: 10.1016/j.ejmech.2019.111725. Epub 2019 Sep 24. Erratum in: Eur J Med Chem. 2020 Aug 1;199:112406. [Content Brief]
