BAMB-4

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BAMB-4

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

891025-25-5

包装与价格：

包装	价格(元)
10mM (in 1mL DMSO)	电议
5mg	电议
10mg	电议

产品介绍

化学性质

Physical Appearance	A solid
Storage	Store at -20°C
M.Wt	252.27
Cas No.	891025-25-5
Formula	C₁₅H₁₂N₂O₂
Solubility	insoluble in H2O; insoluble in EtOH; ≥7.8 mg/mL in DMSO
Chemical Name	N-(benzo[d]isoxazol-3-yl)-4-methylbenzamide
Canonical SMILES	CC1=CC=C(C(NC2=NOC3=CC=CC=C32)=O)C=C1
运输条件	蓝冰运输或根据您的需求运输。
一般建议	为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。

资料参考

BAMB-4是肌醇-1,4,5-三磷酸酯-3-激酶A（ITPKA）的抑制剂，IC50值为20 μM [1]。

ITPKA是InsP3激酶，它结合肌动蛋白丝并将它们捆绑。该蛋白质调节肌动蛋白的动态以及肌醇磷酸信号[1]。

BAMB-4几乎可以完全被H1299细胞吸收。BAMB-4不属于典型的激酶抑制剂。其具有相对较高的特异性和高细胞摄取，使之具有有效抑制体内InsP3激酶的可能性。在所有InsP3激酶抑制剂中，BAMB-4表现出最低的抑制频率。在测试的42种激酶中，BAMB-4仅对其中一种显示出抑制作用。在激酶筛选中，没有检测到BAMB-4的靶标。这些结果表明，BAMB-4不是典型的激酶抑制剂。在体外，数据表明，对于InsP3，BAMB-4增加Km，减少了Vmax。最低浓度 10 μM 的BAMB-4 将InsP3的Km增加160％。较高浓度BAMB-4没有进一步增加InsP3的Km值。BAMB-4剂量依赖性地将Vmax从75％降至50％。在抑制剂存在下，Vmax的下降和Km的增加表明BAMB-4可能属于混合型抑制剂。数据表明，BAMB-4也减少ATP的Vmax，增加Km [2]。

目前BAMB -4未应用在动物中。

参考文献：
[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.

试验操作

Cell experiment:[1]
Cell lines	KB-3-1 cells
Reaction Conditions	10 μM BAMB-4 for 12 h incubation
Applications	Inhibition of inositol-trisphosphate 3-kinase B (ITPKB) activity by BAMB-4 treatment resulted in increased ROS level, NOX activity, and cisplatin response in cancer cells. The BAMB-4 effect was abolished in cells lacking ITPKB.
Animal experiment:[1]
Animal models	Patient-derived xenograft (PDX) mouse models of ovarian cancer and lung cancer
Dosage form	10 mg/kg Administered by intraperitoneal injection twice a week after 42 days from xenograft
Applications	No obvious histopathological changes or kidney injury were observed in mice chronically exposed to BAMB-4 (10 mg/kg), cisplatin (5 mg/kg), or the combination. The combination of BAMB-4 and cisplatin significantly reduced tumor growth, tumor size, and tumor proliferation in ovarian cancer PDX and lung cancer PDX mice.
Note	The technical data provided above is for reference only.
	References: 1. Pan C, Jin L, Wang X, et al. Inositol-triphosphate 3-kinase B confers cisplatin resistance by regulating NOX4-dependent redox balance. Journal of Clinical Investigation, 2019, 129(6): 2431-2445.