CAS NO: | 891025-25-5 |
包装 | 价格(元) |
10mM (in 1mL DMSO) | 电议 |
5mg | 电议 |
10mg | 电议 |
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。 |
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.
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. |