UMI-77 |
Catalog No.GC15805
One-Click Copy Product Info
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Mcl-1 inhibitor, novel
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 518303-20-3
Sample solution is provided at 25 µL, 10mM.
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UMI-77 is a novel small-molecule inhibitor of Mcl-1 with Ki and IC50 values of 0.49 μM and 0.31 μM [1].
Myeloid cell leukemia-1 (Mcl-1) is a member of the prosurvival Bcl-2 family and is a potent anti-apoptotic protein. Mcl-1 acts as an important survival factor in a broad range of human cancers [1].
UMI-77 is a novel small-molecule Mcl-1 inhibitor. In FP-based binding assays, UMI-77 potently and selectively displaced fluorescent labeled BID-BH3 peptide from Mcl-1 protein with Ki value of 0.49μM and bound to the BH3 binding pocket of Mcl-1 protein. UMI-77 bound to A1/Bfl-1, Bcl-w, Bcl-2 and Bcl-xL with Ki values of 5.33, 8.19, 23.83 and 32.99μM. In a pull-down assay, UMI-77 at 10 μM effectively and dose-dependently inhibited the interactions between BL-Noxa and cellular Mcl-1. It was reported that Mcl-1 regulates pro-apoptotic Bax and Bak proteins and preventing their pro-apoptotic activity. UMI-77 dose-dependently inhibited the binding of Mcl-1 to Bax with IC50 value of 1.43μM. In PC cells, UMI-77 inhibited cell growth and induced apoptosis in a time and dose-dependent way [1].
In BxPC-3 xenografted SCID mice model, UMI-77 exhibited robust anti-tumor efficacy with no toxicity. Also, UMI-77 decreased the anti-apoptotic protein survivin, which potently inhibited apoptosis by antagonizing caspase activity [1].
Reference:
[1]. Abulwerdi F, Liao C, Liu M, Azmi AS, et al. A novel small-molecule inhibitor of mcl-1 blocks pancreatic cancer growth in vitro and in vivo. Mol Cancer Ther, 2014, 13(3): 565-575.
| 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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| Cas No. | 518303-20-3 | SDF | |
| Chemical Name | 2-[4-[(4-bromophenyl)sulfonylamino]-1-hydroxynaphthalen-2-yl]sulfanylacetic acid | ||
| Canonical 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 |
| Solubility | ≥ 23.4mg/mL in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.1352 mL | 10.676 mL | 21.352 mL |
| 5 mM | 427 μL | 2.1352 mL | 4.2704 mL |
| 10 mM | 213.5 μL | 1.0676 mL | 2.1352 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >97.50% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 4 reference(s) in Google Scholar.)