MKC3946, inhibitor

MKC3946

Cat. Num. AAA5764357

• Purity: 98.00%
• Synonyms: MKC3946; inhibitor

• Purity/Purification: 98.00%
• Form/Format: Solid. Powder

• Solubility: DMSO: 30mg/mL (78.85mM); (<1mg/ml refers to the product slightly soluble or insoluble)
• Formula: C21H20N2O3S
• SMILES: CN(CC1)CCN1C(c1ccc(-c(ccc2c3C=O)cc2ccc3O)s1)=O
• CAS Number: 1093119-54-0
• Cell Research: For each assay, the various numbers of cells (1,000 for cell proliferation and 10,000 for cell viability assays) are seeded in 96-well plates, followed by either vehicle (DMSO) or increasing concentrations of the drug. For detection of relative numbers of living cells, 10uL of MTT (5mg/mL) is added to each well, placed in an incubator for four hours, followed by centrifugation (1,000 rpm, 5 min); 100uL of supernatant media from each well are carefully removed and 100uL of SDS buffer (20% in water) is added to dissolve the crystals. Results are further read on the spectrophotometer machine at 570nM wavelengthours. Half maximal inhibitory concentration (IC50) is calculated using the GraphPad Prism 5. A synergy of combination of two drugs is determined using the CalcuSyn software. The extent of drug interaction between the two drugs is determined using the combination index (CI) for mutually exclusive drugs. Different CI values are obtained when solving the equation for different concentrations of drugs. A CI of 1 indicates an additive effect, whereas a CI of <1denotes synergy. All experiments are repeated at least three times [1].
• In Vitro: MKC-3946 (100mg/kg, i.p.) inhibits XBP1 splicing in a model of ER stress in vivo, associated with significant growth inhibition ofmM cells, alone or with bortezomib. MKC-3946 significantly reducesmM tumor growth in the treatment,versus the control group. Inhibition of XBP1 splicing by MKC-3946 is associated with decreasedmM growth in vivo, alone or in combination with bortezomib [3].
• Preparation and Storage: Store at -20 degree C for 3 years powder; -80 degree C for 2 years in solvent

Related Product Information for MKC3946, inhibitor

MKC3946 is an effective and soluble IRE1alpha inhibitor which triggered modest growth inhibition in multiple myeloma cell lines.

References

Sun H, et al. Inhibition of IRE1alpha-driven pro-survival pathways is a promising therapeutic application in acute myeloid leukemia. Oncotarget. 2016 Apr 5;7(14):18736-49.
Sun H, et al. Inhibition of IRE1alpha-driven pro-survival pathways is a promising therapeutic application in acute myeloid leukemia. Oncotarget. 2016 Apr 5;7(14):18736-49.
Zhang L, et al. IRE1 inhibition perturbs the unfolded protein response in a pancreatic beta-cell line expressing mutant proinsulin, but does not sensitize the cells to apoptosis. BMC Cell Biol. 2014 Jul 10;15:29.
Zhang L, et al. IRE1 inhibition perturbs the unfolded protein response in a pancreatic beta-cell line expressing mutant proinsulin, but does not sensitize the cells to apoptosis. BMC Cell Biol. 2014 Jul 10;15:29.
Mimura N, et al. Blockade of XBP1 splicing by inhibition of IRE1alpha is a promising therapeutic option in multiple myeloma. Blood. 2012 Jun 14;119(24):5772-81.
Mimura N, et al. Blockade of XBP1 splicing by inhibition of IRE1alpha is a promising therapeutic option in multiple myeloma. Blood. 2012 Jun 14;119(24):5772-81.