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^[1][2].

In HeLa cell viability assays, treatment with KST012174 (50-200 μM; 1 day or 2 days) results in a cell viability of approximately 50% of that of the control group with no obvious concentration dependence after 1 day of treatment, while a moderate concentration-dependent decrease in cell viability occurs after 2 days of treatment^[1].
KST012174 (100 μM) reduces the VEGF mRNA level in HeLa cells, which is induced and elevated by Deferoxamine (HY-B1625) (DFO, 150 μM), to a level close to that under normoxia in real-time quantitative PCR assays^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

545.50

C₂₇H₃₄Cl₂N₆O₂

1392224-35-9

O=C(N1CCN(CC1)CC(NC2=C(Cl)C=CC=C2)=O)NCC3=NN(C(CC(C)C)=C3)C4=CC=CC=C4.Cl

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [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.