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抑制剂/激活剂

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凋亡与自噬

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VE-821

VE-821(ATR inhibitor IV)是一种有效的，选择性的，ATP竞争性ATR抑制剂，在无细胞试验中Ki/IC50为13 nM/26 nM，抑制H2AX磷酸化，对PIKKs ATM， DNA-PK， mTOR和PI3Kγ具有很低的抑制活性。

货号：
TK0279
规格：

5mg

10mg

25mg
价格：
￥0.00

产品参数

CAS No.	1232410-49-9
生物活性	VE-821 is a potent ATP-competitive inhibitor of ATR with Ki/IC50 of 13 nM/26 nM.
分子式	C18H16N4O3S
分子量	368.41
储存条件	Powder -20℃ 3 years
溶解性数据	DMSO : 50 mg/mL (135.72 mM; Need ultrasonic) H2O : < 0.1 mg/mL (ultrasonic;warming;heat to 60°C) (insoluble)
体外研究	VE-821 shows excellent selectivity for ATR with minimal cross-reactivity against the related PIKKs ATM, DNA-PK, mTOR and PI3Kγ (Kis of 16 μM, 2.2 μM, >1 μM and 3.9 μM, respectively) and against a large panel of unrelated protein kinases. VE-821 (compound 27) also inhibits ATM and DNA-PK wirh IC50 of >8 μM, and 4.4 μM, respectively. VE-821 significantly enhances the sensitivity of PSN-1, MiaPaCa-2 and primary PancM pancreatic cancer cells to radiation and Gemcitabine under both normoxic and hypoxic conditions. ATR inhibition by VE-821 leads to inhibition of radiation-induced G2/M arrest in cancer cells. In both PSN-1 and MiaPaCa-2 cells, 1 µM VE-821 inhibits phosphorylation of Chk1 (Ser 345) after treatment with Gemcitabine (100 nM), radiation (6 Gy) or both, at 2 h post-irradiation.
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纯度及产品资料	98%

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