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HA14-1

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Chemical Structure| 65673-63-4 同义名 : -
CAS号 : 65673-63-4
货号 : A350244
分子式 : C17H17BrN2O5
纯度 : 98%
分子量 : 409.231
MDL号 : MFCD00218213
存储条件：

粉末 Keep in dark place,Sealed in dry,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 50 mg/mL(122.18 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
靶点

  • Bcl-2

    Bcl-2, IC50:9 μM
描述 Bcl-2 (B-cell lymphoma 2) is an integral outer mitochondrial membrane protein that regulates cell death by inhibiting Bax, thus controlling the mitochondrial membrane permeability. Bcl-2 could engage a group of proapoptotic Bcl-2 family members, the BH3-only proteins like Bid and Bim, by physically sequestering them from directly activating Bax. Bcl-2 could also interact with Bax directly[3]. HA14-1 is an inhibitor of Bcl-2. In a binding assay, HA14-1 was found to bind the designated pocket on Bcl-2 with the IC50 of ≈ 9 μM in competing with the bcl-2 binding of Flu-BakBH3[4]. In a MTT assay, the lethal concentration 50% (LC50) values of HA14-1 to HF1A3, HF4.9 and HF28RA cells when incubated for 20h were 4.5 μM, 12.6 μM and 8.1 μM, respectively[5]. Treatment with 50 μM HA14-1 by 3h induced apoptosis in HL-60 cells as evidenced by DNA ladders[4]. In a BeGBM xenograft model established in nude mice, HA14-1 was injected once weekly for 4 weeks at the concentration of 400 nM in 100 μl volume at the site of cell injection. This dose of HA14-1 increased the effect of etoposide on tumor growth[3].
作用机制 HA14-1 is an inhibitor of Bcl-2. In a binding assay, HA14-1 was found to bind the designated pocket on Bcl-2 with the IC50 of ≈ 9 μM in competing with the bcl-2 binding of Flu-BakBH3[4].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.44mL

0.49mL

0.24mL

12.22mL

2.44mL

1.22mL

24.44mL

4.89mL

2.44mL
参考文献

[1]Skommer J, Wlodkowic D, et al. HA14-1, a small molecule Bcl-2 antagonist, induces apoptosis and modulates action of selected anticancer drugs in follicular lymphoma B cells. Leuk Res. 2006 Mar;30(3):322-31.

[2]Wang JL, Liu D, et al. Structure-based discovery of an organic compound that binds Bcl-2 protein and induces apoptosis of tumor cells. Proc Natl Acad Sci U S A. 2000 Jun 20;97(13):7124-9.

[3]Manero F, Gautier F, Gallenne T, Cauquil N, Grée D, Cartron PF, Geneste O, Grée R, Vallette FM, Juin P. The small organic compound HA14-1 prevents Bcl-2 interaction with Bax to sensitize malignant glioma cells to induction of cell death. Cancer Res. 2006 Mar 1;66(5):2757-64.

[4]Wang JL, Liu D, Zhang ZJ, Shan S, Han X, Srinivasula SM, Croce CM, Alnemri ES, Huang Z. Structure-based discovery of an organic compound that binds Bcl-2 protein and induces apoptosis of tumor cells. Proc Natl Acad Sci U S A. 2000 Jun 20;97(13):7124-9.

[5]Skommer J, Wlodkowic D, Mättö M, Eray M, Pelkonen J. HA14-1, a small molecule Bcl-2 antagonist, induces apoptosis and modulates action of selected anticancer drugs in follicular lymphoma B cells. Leuk Res. 2006 Mar;30(3):322-31.