13585831301
021-59541103 021-60443211
3004967995
13585831301021-59541103 021-604432113004967995
聯系人:高小姐
電話:021-59541103 021-60443211
手機:13585831301
Q Q： 3004967995
Email:3004967995@qq.com
詳細地址：上海嘉定區嘉羅公路1661
化學性質：
| 規格 | 10mM (in 1mL DMSO) 10mg 50mg |
| CAS | 509102-00-5 |
| 別名 |
|
| 化學名 | 4-((E)-(((Z)-2-(cyclohexylimino)-4-methylthiazol-3(2H)-yl)imino)methyl)benzene-1,2,3-triol |
| 分子式 | C17H21N3O3S |
| 分子量 | 347.43 |
| 溶解度 | ≥ 12.15mg/mL in DMSO |
| 儲存條件 | 4°C, protect from light |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice |
產品描述：
MIM1 effectively competed with FITC-MCL-1 SAHBA and FITC-BID BH3 for MCL-1ΔNΔC binding with IC50 values of 4.7 and 4.8 mM, respectively. And MIN1 shows a combination of favorable biophysical and biological properties including its solubility, stability, nonreactivity, MCL-1 binding potency and selectivity, compatibility with and activity in a BAX-mediated liposomal release assay and relatively little to no toxicity in Bax-/-Bak-/- MEFs [1].
As an MCL-1 inhibitor, MIM1 selectively targets the BH3-binding groove of MCL-1, neutralizes its biochemical lockhold on apoptosis, and induces caspase activation and leukemia cell death in the specific context of MCL-1 dependence.
The activity and specificity of MIM1 in cancer cells was dependable for assessing MCL-1 and BCL-XL dependence by employing murine BCRABL (p185)-transformed, Arf null, B-lineage acute lymphoblastic leukemia cells. Comparing to the effect of ABT-737 on p185+Arf-/-/Mcl-1-deleted B-ALL cells, MIM1 had the exact opposite effect, impacting the viability of the MCL-1-dependent cells (IC50, 4.2 mM), including dose-dependent induction of caspase 3/7 activity, but having no effect on the BCL-XL-dependent cells. A combination of MIM1 (IC50, 10.6 mM) and ABT-737 (IC50, 5.1 mM) resulted in synergistic cytotoxicity. Strikingly, when the MIM1/ABT-737 combination was applied to MCL-1-reconstituted p185+Arf-/-/Mcl-1-deleted B-ALL cells, the addition of ABT-737 had little effect [1].
MIM1 emerged as a potent and selective small molecule inhibitor of MCL-1 DNDC, capable of targeting the canonical BH3-binding point of MCL-1 and blocking MCL-1-mediated suppression of tBID-induced BAX activation in vitro. MIM1 may serve as a prototype for the development of next generation small molecules that effectively reduce the apoptotic threshold in cancers specifically driven by antiapoptotic MCL-1 [1].
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原創作者：上海莼試生物技術有限公司
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普票匯款信息
賬 戶 名：上海生物
開 戶 行：中國銀行山東省分行營業部
賬 號：2169 2341 6278
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