1392224-35-9
Chemical Structure
KST012174 hydrochloride
- CAS No.: 1392224-35-9
- Formula:C27H34Cl2N6O2
- Molecular Weight:545.50
IUPAC Name: 4-(2-((2-chlorophenyl)amino)-2-oxoethyl)-N-((5-isobutyl-1-phenyl-1H-pyrazol-3-yl)methyl)piperazine-1-carboxamide hydrochloride
InChIKey: XHHMTZMVSPEWCP-UHFFFAOYSA-N
SMILES: O=C(N1CCN(CC1)CC(NC2=C(Cl)C=CC=C2)=O)NCC3=NN(C(CC(C)C)=C3)C4=CC=CC=C4.Cl
Biological Activity: KST012174 hydrochloride is a potent HIF-1α-p300/CBP interaction inhibitor with an IC50 of 107 μM. KST012174 hydrochloride completely blocks the binding of HIF-1α to p300 protein at a concentration of 100 μM, without affecting the expression stability of HIF-1α protein itself. By directly interfering with the binding between the C-terminal transactivation domain (C-TAD) of HIF-1α and the CH1 domain of p300, KST012174 inhibits the transcriptional activation function of HIF-1α, thereby significantly downregulating the mRNA expression level of its downstream target gene VEGF and exerting core activity in inhibiting tumor angiogenesis. KST012174 hydrochloride is applicable for research on cancer occurrence and development as well as hypoxia pathway-targeted strategies[1][2].
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KST012174 hydrochloride | KST012174 hydrochloride is a potent HIF-1α-p300/CBP interaction inhibitor with an IC50 of 107 μM. KST012174 hydrochloride completely blocks the binding of HIF-1α to p300 protein at a concentration of 100 μM, without affecting the expression stability of HIF-1α protein itself. By directly interfering with the binding between the C-terminal transactivation domain (C-TAD) of HIF-1α and the CH1 domain of p300, KST012174 inhibits the transcriptional activation function of HIF-1α, thereby significantly downregulating the mRNA expression level of its downstream target gene VEGF and exerting core activity in inhibiting tumor angiogenesis. KST012174 hydrochloride is applicable for research on cancer occurrence and development as well as hypoxia pathway-targeted strategies. | |||||||||||||||||||||
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- [1]. Kwon HS, et al. Inhibition of VEGF transcription through blockade of the hypoxia inducible factor-1α-p300 interaction by a small molecule. Bioorg Med Chem Lett. 2012;22(16):5249-5252. [Content Brief]
- [2]. Wei J, et al. Recent advances in the discovery of HIF-1α-p300/CBP inhibitors as anti-cancer agents[J]. Mini Reviews in Medicinal Chemistry, 2018, 18(4): 296-309.
Keywords
