UMI-77
UMI-77 (CAS 518303-20-3) is a small-molecule inhibitor targeting the anti-apoptotic protein Myeloid cell leukemia-1 (Mcl-1), a member of the Bcl-2 protein family implicated in apoptotic regulation and cell survival signaling. Biochemical assays demonstrate that UMI-77 binds selectively to the BH3-binding groove of Mcl-1 protein, competing effectively against pro-apoptotic BH3 peptides (Ki = 0.49 μM). Additionally, UMI-77 disrupts the interaction of Mcl-1 with pro-apoptotic factors such as Bax (IC50 = 1.43 μM), promoting apoptosis in cancer cells. Preclinical studies on pancreatic cancer cell lines and BxPC-3 xenograft mouse models show that UMI-77 suppresses tumor growth and induces apoptotic cell death, highlighting its value as a research tool for studying apoptosis-related oncogenic pathways.
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 468.34 |
| Cas No. | 518303-20-3 |
| Formula | C18H14BrNO5S2 |
| Solubility | ≥23.4 mg/mL in DMSO; insoluble in H2O; ≥7.2 mg/mL in EtOH |
| Chemical Name | 2-[4-[(4-bromophenyl)sulfonylamino]-1-hydroxynaphthalen-2-yl]sulfanylacetic acid |
| SDF | Download SDF |
| Canonical SMILES | C1=CC=C2C(=C1)C(=CC(=C2O)SCC(=O)O)NS(=O)(=O)C3=CC=C(C=C3)Br |
| Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
| General tips | We do not recommend long-term storage for the solution, please use it up soon. |
| Cell experiment [1]: | |
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Cell lines |
Pancreatic cancer (PC) cells |
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Preparation method |
Limited solubility. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
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Reaction Conditions |
~24 h |
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Applications |
UMI-77 inhibits growth of PC cells, especially for the BxPC-3 and Panc-1 cell line with highest potency. In Panc-1 cells, UMI-77 also effectively induces apoptosis in a time-dependent and dose-dependent manner. Moreover, it leads to a dose-dependent release of cytochrome c and Smac from mitochondria. In addition, the growth inhibition and apoptosis effects of UMI-77 is abrogated by knocking down Mcl-1 expression |
| Animal experiment [1]: | |
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Animal models |
BxPC-3 xenograft model in SCID mice |
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Dosage form |
60 mg/kg i.v. |
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Applications |
UMI-77 treatment for 5 consecutive days a week for two weeks significantly inhibits the tumor growth by 65% and 56%. UMI-77 also markedly increases the positive apoptotic cells of tumor sections comparing with the control cohorts. |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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References: 1. Abulwerdi F, Liao C, Liu M et al. A novel small-molecule inhibitor of mcl-1 blocks pancreatic cancer growth in vitro and in vivo. Mol Cancer Ther. 2014 Mar;13(3):565-75. |
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