BCL-2-targeting small molecule inhibitor venetoclax won FDA approval for chronic lymphocytic leukemia and acute myeloid leukemia. Interests in developing BCL-XL-selective inhibitors arise as BCL-XL overexpression is implicated in venetoclax resistance. However, these efforts failed in clinical development ...
recommend using the Bcl-xL-selective inhibitor A-1155463 (A115), which is >800-fold selective for Bcl-xL over the BCL-2 family members Bcl-2 and Mcl-1, resulting in low cytotoxicity in most mammalian cell lines andin vivo(Tao et al., 2014) (Fig. 1B)....
ABT-737 is a BH3 mimetic inhibitor of Bcl-xL, Bcl-2 and Bcl-w with EC50 of 78.7 nM, 30.3 nM and 197.8 nM in cell-free assays, respectively; no inhibition observed against Mcl-1, Bcl-B or Bfl-1.A selective inhibitor of Bcl-2 关联靶点(人) 关联靶点(其它种属) 作用机制 名称和识别...
The development of the dual Bcl-2/Bcl-xL inhibitor ABT-263 ended up in vain due to thrombopenia resulted from Bcl-xL inhibition. However, the Bcl-xL-selective inhibitors A-1155463 and A-1331862 demonstrated tolerability and efficacy in preclinical solid tumor models14. Mcl-1 is a short-...
WEHI-539 hydrochloride is a selective inhibitor of Bcl-XL with an IC50 of 1.1 nM. IC50 & Target[1] Bcl-xL 1.1 nM (IC50) 体外研究(In Vitro) WEHI-539 hydrochloride is a selective inhibitor of Bcl-XL. WEHI-539 augments NSC 241240 induced caspase 3/7 activity, PARP cleavage and annexi...
ABT-263: a potent and orally bioavailable Bcl-2 family inhibitor. Cancer Res. 68, 3421–3428 (2008). Article CAS PubMed Google Scholar Souers, A. J. et al. ABT-199, a potent and selective BCL-2 inhibitor, achieves antitumor activity while sparing platelets. Nat. Med. 19, 202–208 ...
XL-784价格:￥3304/支产品详情:XL-784 is a selective matrix metalloproteinases (MMP) inhibitor, with IC50s of ~1900, 0.81, 120, 10.8, 18, 0.56 nM for M... 纯度:98% 包装规格:5 mg 用途:科学研究、研发 货号:C110598 品牌:ChemeGen
还披露了在其中Bcl2/BclxL的抑制提供益处的疾病和病症(像癌症)的治疗中使用这些Bcl2/BclxL抑制剂的方法. Also disclosed in which the Bcl-2 / Bcl-xL inhibition provide benefits diseases and conditions (such as cancer) treatment using these Bcl-2 / Bcl-xL inhibitor method....
et al. Structure-guided design of a selective BCL-X(L) inhibitor. Nat. Chem. Biol. 9, 390–397 (2013). Article CAS Google Scholar Heller, R. S. et al. Expression patterns of Wnts, Frizzleds, sFRPs, and misexpression in transgenic mice suggesting a role for Wnts in pancreas and ...
To further dissect the contribution of BCL-XL or BCL-2 inhibition, since Navitoclax is able to inhibit both proteins in cells, we investigated both selective BCL-XL inhibitor A-1331852 and selective BCL-2 inhibitor Venetoclax in combination with the BAX activator BTSA1.2. We evaluated a set of...