A selective Mcl-1 inhibitor (Ki = 490 nM) that disrupts the heterodimerization of Mcl-1/Bax and Mcl-1/Bak; induces apoptosis of various pancreatic cancer cell lines (IC50s = 3.4-16.1 μM); demonstrates antitumor activity in a BxPC-3 xenograft mouse model

UMI-77 – 5 mg

Brand:
Cayman
CAS:
518303-20-3
Storage:
-20
UN-No:
De Minimis - 3077 / 9

Myeloid cell leukemia-1 (Mcl-1) is a potent anti-apoptotic protein and a member of the pro-survival Bcl-2 family. UMI-77 is a selective Mcl-1 inhibitor with a Ki value of 490 nM and exhibits selectivity over other members of the Bcl-2 family (Kis = 5.3, 23.8, 33.0, and 8.2 µM) for A1/Bfl-1, Bcl-2, Bcl-xL, and Bcl-W, respectively).{31143} It has been shown to disrupt the heterodimerization of Mcl-1/Bax and Mcl-1/Bak, thus antagonizing Mcl-1 function.{31143} UMI-77 inhibits the growth of various pancreatic cancer cell lines with IC50s values ranging from 3.4-16.1 μM, inducing apoptosis through activation of the intrinsic apoptotic pathway and/or Bax conformational change.{31143} In a BxPC-3 xenograft mouse model, 60 mg/kg UMI-77 demonstrated antitumor activity without damaging normal tissues.{31143}  

 

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Description

A selective Mcl-1 inhibitor (Ki = 490 nM) that disrupts the heterodimerization of Mcl-1/Bax and Mcl-1/Bak; induces apoptosis of various pancreatic cancer cell lines (IC50s = 3.4-16.1 μM); demonstrates antitumor activity in a BxPC-3 xenograft mouse model

Formal name: 2-[[4-[[(4-bromophenyl)sulfonyl]amino]-1-hydroxy-2-naphthalenyl]thio]-acetic acid

Synonyms: 

Molecular weight: 468.3

CAS: 518303-20-3

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors||Research Area|Cancer|Cell Death|Apoptosis

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