927823-01-6
Chemical Structure
KCN1
- CAS No.: 927823-01-6
- Formula:C26H27NO5S
- Molecular Weight:465.56
IUPAC Name: N-((2,2-dimethyl-2H-chromen-6-yl)methyl)-3,4-dimethoxy-N-phenylbenzenesulfonamide
InChIKey: IPZJNJPAVPZHJM-UHFFFAOYSA-N
SMILES: O=S(C1=CC=C(C(OC)=C1)OC)(N(C2=CC=CC=C2)CC3=CC4=C(C=C3)OC(C)(C)C=C4)=O
Biological Activity: KCN1 is a p300/HIF-1α interaction inhibitor with a Kd value of 345 nM for p300-CH1. KCN1 binds to the CH1 domain of p300, blocks the assembly of the p300/HIF-1α complex, and disrupts the HIF-1α-p300/CBP interaction. KCN1 inhibits cancer cell growth, induces cancer cell cycle arrest and apoptosis. KCN1 inhibits β-galactosidase activity and downregulates the expression of VEGF, Glut1, CA9 and CAIX. KCN1 exerts anticancer activity in mouse tumor xenograft models. KCN1 can be used in research related to malignant glioma, pancreatic cancer and metastatic uveal melanoma[1][2][3].
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KCN1 | KCN1 is a p300/HIF-1α interaction inhibitor with a Kd value of 345 nM for p300-CH1. KCN1 binds to the CH1 domain of p300, blocks the assembly of the p300/HIF-1α complex, and disrupts the HIF-1α-p300/CBP interaction. KCN1 inhibits cancer cell growth, induces cancer cell cycle arrest and apoptosis. KCN1 inhibits β-galactosidase activity and downregulates the expression of VEGF, Glut1, CA9 and CAIX. KCN1 exerts anticancer activity in mouse tumor xenograft models. KCN1 can be used in research related to malignant glioma, pancreatic cancer and metastatic uveal melanoma. | |||||||||||||||||||||
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- [1]. Shi Q, et al. Binding Model for the Interaction of Anticancer Arylsulfonamides with the p300 Transcription Cofactor. ACS medicinal chemistry letters. 2012 Aug 09;3(8):620-5. [Content Brief]
- [2]. Wang W, et al. KCN1, a novel synthetic sulfonamide anticancer agent: in vitro and in vivo anti-pancreatic cancer activities and preclinical pharmacology. PloS one. 2012;7(9):e44883. [Content Brief]
- [3]. Yin S, et al. Arylsulfonamide KCN1 inhibits in vivo glioma growth and interferes with HIF signaling by disrupting HIF-1α interaction with cofactors p300/CBP. Clin Cancer Res. 2012 Dec 15;18(24):6623-33. [Content Brief]
Keywords
