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BPTES

BPTES 是一种特异性 GlutamiN/Ase GLS1 (KGA) 抑制剂，IC50=0.16 μM。

CAS号

314045-39-1

分子式

C24H24N6O2S3

主要靶点

Glutaminase|transporter

仅限科研使用

Cat No : CM04268

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Synonyms

验证数据展示

  • CAS No.: 314045-39-1

    BPTES
    CAS#: 314045-39-1

产品信息

BPTES(IC50 of 0.16 μM) is an effective and specific GlutamiN/Ase GLS1 (KGA) inhibitor.

CAS号 314045-39-1
分子式 C24H24N6O2S3
主要靶点 Glutaminase|transporter
主要通路 代谢|蛋白酶体
分子量 524.68
纯度 95.83%， 此纯度可做参考，具体纯度与批次有关系，可咨询客服
储存条件 Powder: -20°C for 3 years | In solvent: -80°C for 1 year
别名

靶点活性

Glutaminase GLS1 (KGA):0.16 μM

体内活性

In LAP/MYC mice, BPTES (12.5 mg/kg, i.p.) prolongs survival with no significant effects on MYC, GLS, or GLS2 levels. BPTES (200 μg/mouse, i.p.) also inhibits tumor cell growth in mice harboring P493 tumor xenografts. [3]

体外活性

BI-9564 with EC50 of 800 nM.BRD7 implied as a tumor suppressor and is down-regulated in cancer cells, BI-9564 shows Kd of 73 nM for it, and is >10-fold more selective for BRD9 over the high homologues bromodomain. BI-9564 (<5 μM) shows no activity against 324 kinases, when BI-9564 at 10 μM, an inhibition >40% is observed for only 2 out of 55 GPCRs.

溶解度

DMSO:10.5 mg/mL (20 mM)

细胞实验

BPTES is dissolved in DMSO. Cells are plated at a density of 500 cells/well in a 96-well black clear bottom plate. At 24 hrs, media is changed to the appropriate media (DMEM with 4.5 g/L, 1.5 g/L or 0.1 g/L glucose, 10% FBS, pencillin/streptomycin, and 4 mM glutamine with or without doxycyline). 48 hours after plating, compounds or DMSO are added. Media and alamarBlue is added to a volume of 200 μL in each well. Fluorescence is measured at 48 hrs or 72 hrs (EGCG) using a Victor3 plate-reader.

参考文献

1.Newcomb R. 2002. U.S. Pat. 6,451,828 B1.
2.Seltzer MJ, et al. Cancer Res. 2010, 70(22), 8981-81987.
3.Xiang Y, et al. J Clin Invest. 2015, 125(6), 2293-2306.
4.Lee JS, et al. Dual targeting of glutaminase 1 and thymidylate synthase elicits death synergistically in NSCLC. Cell Death Dis. 2016 Dec 8;7(12):e2511.

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