ML-291 |
Catalog No.GC13034
One-Click Copy Product Info
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ML-291 is a UPR (unfolded protein response)-inducing sulfonamidebenzamide. ML-291 overwhelms the adaptive capacity of the UPR and induces apoptosis in a variety of solid cancer models. ML-291 can activate the PERK/eIF2a/CHOP (apoptotic) arm of the UPR and reduce leukemic cell burden.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1523437-16-2
Sample solution is provided at 25 µL, 10mM.
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ML-291 is an apoptosis inducer.
Apoptosis, a process of programmed cell death, occurs in multi-cellular organisms. Biochemical events result in characteristic cell changes (morphology) and death. These changes include cell shrinkage, nuclear fragmentation, blebbing, chromatin condensation, chromosomal DNA fragmentation, as well as global mRNA decay.
In vitro: ML-291 was identified as a novel activator of the apoptotic arm of the unfolded protein response (UPR), but not the adaptive arm. Specifically, ML-291 could activate signaling via PERK/eIF2α/CHOP with EC50 value of 762 nM but not through IRE1/XBP1. Moreover, ML-291 induced apoptosis in mouse embryonic fibroblasts overexpressing CHOP, but not in wild-type or CHOP knockout cells. ML-291 showed minimal activity against a panel of 67 receptors, ion channels, as well as transporters, with the exception of the dopamine transporter with 68% inhibition. In addition, ML-291 showed greater cytotoxicity than average antitumor cell cytotoxicity against colon, melanoma, and renal cancer cell lines in an NCI-60 panel [1].
In vivo: Up to now, there is no animal in vivo data reported.
Clinical trial: So far, no clinical study has been conducted.
Reference:
[1] Flaherty, D. P.,Golden, J.E.,Liu, C., et al. Selective small molecule activator of the apoptotic arm of the UPR. Probe Reports from the NIH Molecular Libraries Program (2012).
| Cas No. | 1523437-16-2 | SDF | |
| Chemical Name | N-[4-[(4-chloro-1-piperidinyl)sulfonyl]phenyl]-5-nitro-2-furancarboxamide | ||
| Canonical SMILES | ClC1CCN(S(C2=CC=C(NC(C3=CC=C([N+]([O-])=O)O3)=O)C=C2)(=O)=O)CC1 | ||
| Formula | C16H16ClN3O6S | M.Wt | 413.8 |
| Solubility | ≤1mg/ml in DMSO;10mg/ml in dimethyl formamide | 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 | 2.4166 mL | 12.0831 mL | 24.1663 mL |
| 5 mM | 483.3 μL | 2.4166 mL | 4.8333 mL |
| 10 mM | 241.7 μL | 1.2083 mL | 2.4166 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: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 9 reference(s) in Google Scholar.)