HIF-1α inhibitor LW6 | HIF-1α inhibitor, MDH2 inhibitor

Chemical Structure : HIF-1α inhibitor LW6

CAS No.: 934593-90-5

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HIF-1α inhibitor LW6 (LW6)

货号: PC-24681Not For Human Use, Lab Use Only.

HIF-1α inhibitor LW6 is a specific small compound malate dehydrogenase 2 (MDH2) that inhibits the accumulation of HIF-1α, decreases HIF-1α protein expression without affecting HIF-1β expression, has IC50 of 2.6 uM in HIF-1-mediated cell-based reporter assay in Hep3B cells.

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5 mg	￥580	In stock
10 mg	￥880	In stock
25 mg	￥1380	In stock
50 mg	￥2180	In stock
100 mg		Get quote

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生物&药学活性

HIF-1α inhibitor LW6 is a specific small compound malate dehydrogenase 2 (MDH2) that inhibits the accumulation of HIF-1α, decreases HIF-1α protein expression without affecting HIF-1β expression, has IC50 of 2.6 uM in HIF-1-mediated cell-based reporter assay in Hep3B cells.

LW6 inhibits malate dehydrogenase 2 (MDH2), binds to MDH2 to block the TCA cycle.

LW6 promoted the degradation of wild type HIF-1α, but not of a DM-HIF-1α with modifications of P402A and P564A, at hydroxylation sites in the oxygen-dependent degradation domain (ODDD).

LW6 does not affect the activity of prolyl hydroxylase (PHD), but induced the expression of von Hippel-Lindau (VHL), which interacts with prolyl-hydroxylated HIF-1α for proteasomal degradation.

LW6 demonstrated strong anti-tumor efficacy in vivo and caused a decrease in HIF-1α expression in frozen-tissue immunohistochemical staining in mice carrying xenografts of human colon cancer HCT116 cells.

物理化学性质&存储条件

分子量	435.52
分子式	C26H29NO5
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	Methyl 3-(2-(4-(adamantan-1-yl)phenoxy)acetamido)-4-hydroxybenzoate

参考文献

1. Lee K, et al. Biochem Pharmacol. 2010 Oct 1;80(7):982-9.

2. Naik R, et al. J Med Chem. 2014 Nov 26;57(22):9522-38.

HIF-1α inhibitor LW6 (LW6)

生物&药学活性

物理化学性质&存储条件

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HIF-1α inhibitor LW6 (LW6)

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