BVT948

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

BVT948 是一种蛋白酪氨酸磷酸酶 (PTP) 抑制剂。它还可以抑制赖氨酸甲基转移酶 SETD8 (KMT5A) 和几种细胞色素 P450 (P450) 亚型。

BVT948 is a protein tyrosine phosphatase (PTP) inhibitor.It can also inhibit lysine methyltransferase SETD8 (KMT5A) and several cytochrome P450 (P450) isoforms.(In Vitro):BVT948 inhibits TPA-induced MMP-9 up-regulation in a dose-dependent manner. BVT948 does not affect the MAPK phosphorylation by TPA. Treatment with BVT948 diminishes the TPA-induced cell invasion by 50%. BVT948 appears to be an effective inhibitor of both protein tyrosine phosphatases (PTP activity and P450 activity). BVT948 efficiently and selectively suppresses cellular H4 lysine 20 (H4K20me1) at doses lower than 5 μM within 24 h. Results show that the effect of BVT948 (BVT.948) is to strengthen the insulin signal and has no effects on the duration of the signal. The cells treated with BVT948 recapitulate cell-cycle-arrest phenotypes similar to what are reported for knocking down SETD8 by RNAi. Treatment of MCF-7 cells with 0.5, 1 or 5 μM of BVT948 for 24 h does not cause any significant changes in cell viability. Treatment with BVT948 inhibits TPA-stimulated NF-κB binding activity, but not AP-1 binding activity.(In Vivo):Compare with vehicle-treated controls, BVT948 (BVT.948, 3 μmol/kg) significantly enhances glucose clearance from the blood stream in response to insulin.

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Metabolic Enzyme/Protease

Phosphatase

tryptaminic receptor

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39674-97-0

241.246

C14H11NO3

>98% (HPLC)

In Vitro:?DMSO : 100 mg/mL (414.52 mM)

CC1(C)C(=O)N=C2C1=C(O)C(=O)c1ccccc21

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(-20℃)

With Ice Pack

≥ 2 years