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BAMB-4 Sale

(Synonyms: ITPKA-IN-C14) 目录号 : GC14668

BAMB-4 (ITPKA-IN-C14) 是一种特异性且可透过膜的 ITPKA 抑制剂。 BAMB-4 具有很高的稳定性和膜通透性,并能对抗 1,4,5-三磷酸肌醇 (ITPKA) 的 1,4,5-三磷酸肌醇 (InsP3) 激酶活性,IC50 值为 20微米。 BAMB-4可用于肺癌转移的研究。

BAMB-4 Chemical Structure

Cas No.:891025-25-5

规格 价格 库存 购买数量
10mM (in 1mL DMSO)
¥1,995.00
现货
5mg
¥2,310.00
现货
10mg
¥3,518.00
现货

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Sample solution is provided at 25 µL, 10mM.

产品文档

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产品描述

BAMB-4 is an inhibitor of inositol-1,4,5-trisphosphate-3-kinase A (ITPKA) with an IC50 value of 20 µM [1].

ITPKA is an InsP3 kinase. It binds to actin filaments and bundles them. This protein regulates actin dynamics as well as inositol phosphate signaling [1].

BAMB-4 was almost completely taken up by H1299 cells. BAMB-4 did not belong to typical kinase inhibitors. Its relatively high specificity and high cellular uptake provide the possibility to effectively inhibit InsP3 kinase in vivo. Among InsP3Kinase inhibitors, BAMB-4 exhibit the lowest inhibition frequency. BAMB-4 showed an inhibitory effect only in 1 from 42 tested targets. There was no detected BAMB-4 target in kinase screens. These results indicated that BAMB-4 is not a typical kinase inhibitor. In vitro, data showed that BAMB-4 increased Km and reduced Vmax with respect to InsP3. BAMB-4 at the lowest concentration (10 µM) increased the Km-value for InsP3 by 160%. BAMB-4 at elevated concentrations did not further rise the Km-value for InsP3. BAMB-4 dose-dependently decreased Vmax from 75% to 50%. Decreased Vmax and increased Km in presence of inhibitor indicated that BAMB-4 might belong to mixed type inhibitors. Data showed that BAMB-4 also reduced Vmax and increased Km with respect to ATP [2].

There is still no any available result of the application of BAMB-4 in animals.

References:
[1].  Schrder D, Tdter K, Gonzalez B, et al. The new InsP 3 Kinase inhibitor BIP-4 is competitive to InsP 3 and blocks proliferation and adhesion of lung cancer cells. Biochemical pharmacology, 2015, 96(2): 143-150.
[2].  Schrder D, Rehbach C, Seyffarth C, et al. Identification of a new membrane-permeable inhibitor against inositol-1, 4, 5-trisphosphate-3-kinase A. Biochemical and biophysical research communications, 2013, 439(2): 228-234.

Chemical Properties

Cas No. 891025-25-5 SDF
别名 ITPKA-IN-C14
化学名 N-(benzo[d]isoxazol-3-yl)-4-methylbenzamide
Canonical SMILES CC1=CC=C(C(NC2=NOC3=CC=CC=C32)=O)C=C1
分子式 C15H12N2O2 分子量 252.27
溶解度 ≥ 7.8mg/mL in DMSO 储存条件 Store at -20°C
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1 mg 5 mg 10 mg
1 mM 3.964 mL 19.82 mL 39.6401 mL
5 mM 0.7928 mL 3.964 mL 7.928 mL
10 mM 0.3964 mL 1.982 mL 3.964 mL
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