UMI-77|UMI77|Mcl-1 inhibitor

Cas No.:	518303-20-3
Chemical Name:	2-[4-[(4-bromophenyl)sulfonylamino]-1-hydroxynaphthalen-2-yl]sulfanylacetic acid
Synonyms:	UMI 77，UMI77
SMILES:	C1=CC=C2C(=C1)C(=CC(=C2O)SCC(=O)O)NS(=O)(=O)C3=CC=C(C=C3)Br
Formula:	C₁₈H₁₄BrNO₅S₂
M.Wt:	468.34
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:	UMI-77 is a selective Mcl-1 inhibitor, which shows high binding affinity to Mcl-1 (IC50=0.31 μM). UMI-77 binds to the BH3 binding groove of Mcl-1 with Ki of 490 nM, showing selectivity over other members of anti-apoptotic Bcl-2 members.
In Vivo:	UMI-77 exhibits moderate metabolic stability with a half-life of 45 minutes.The maximum tolerated dose (MTD) of UMI-77 in SCID mice is determined. Administered 60 mg/kg i.v. for 5 consecutive days per week for two weeks does not cause any loss in the animal weight and there is no obvious sign of toxicity during the course of the treatment. Increasing the dose to 80 mg/kg show severe animal weight loss (>20%), therefore 60 mg/kg is used as a therapeutic dose for the in vivo efficacy studies. Daily treatment with UMI-77 for 5 consecutive days a week for two weeks results in statistically significant tumor growth inhibition by 65% and 56% in comparison with the controls in day 19 (p<0.0001) and day 22 (p<0.003) respectively[1].
In Vitro:	Competitive binding curve of UMI-77 against Mcl-1 is obtained by FP based binding assay using fluorescent labeled Bid BH3 peptide with an IC50 of 1.87±0.22 μM. UMI-77 potently inhibits the cell growth of BxPC-3 and Panc-1 cell lines with IC50 values of 3.4 μM and 4.4 μM respectively, and shows 3 to 5 times less potency in inhibition of the cell growth of two other tested cell lines MiaPaCa-2 (12.5 μM) and AsPC-1 (16.1 μM). The cell growth inhibition potency of UMI-77 correlates with the highest expression of Mcl-1 and Bak, and lowest expression of Bcl-xL in the sensitive cell lines, BxPC-3 and Panc-1. Capan-2 cells are showing similar sensitivity to UMI-77 (IC50 of 5.5 μM) as BxPC-3 and Panc-1, although has low Mcl-1 levels[1].

Cat. No.	Product name	Field of application
DC7950	UMI-77	UMI-77 is a selective Mcl-1 inhibitor with Ki of 490 nM, showing selectivity over other members of Bcl-2 family.
DC5005	tw-37	TW-37 is a novel nonpeptide inhibitor to recombinant Bcl-2, Bcl-xL and Mcl-1 with Ki of 0.29 μM, 1.11 μM and 0.26 μM, respectively.
DC10965	SW076956	SW076956 is a small molecule that selectively disrupt Beclin 1/Bcl-2 binding as compared to Bax/Bcl-2 and Bim/Bcl-2 binding and induces autophagic flux at concentrations with minimal cytotoxicity.
DC8128	Pyridoclax(MR29072)	Pyridoclax(MR-29072) is a potent Mcl-1 inhibitor with Kd value of 25 nM.
DC10133	Gambogic Acid	Gambogic Acid activates caspases with EC50 of 0.78-1.64 μM and competitively inhibits Bcl-xl, Bcl-2, Bcl-w, Bcl-B, Bfl-1 and Mcl-1 with IC50 of 1.47 μM, 1.21 μM, 2.02 μM, 0.66 μM, 1.06 μM and 0.79 μM, respectively.
DC10447	FX1	FX1 is a novel specific inhibitor of the B cell lymphoma 6 (BCL6).
DC9955	BCL6 inhibitor(CID5721353)	CID5721353 is a B-Cell Lymphoma 6 Inhibitor (BCL6 inhibitor).
DC9695	BH3I-1	BH3I-1 is a cell permeable BH3 mimetic that binds to Bcl-xL. BH3I-1 is an inhibitor of Bcl-xL.
DC1022	ABT-737	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, respectively.
DC4127	ABT-263 (Navitoclax)	ABT-263 (Navitoclax) is a potent inhibitor of Bcl-xL, Bcl-2 and Bcl-w with Ki of ≤ 0.5 nM, ≤1 nM and ≤ 1 nM, respectively.