MKC3946 Inhibitor

Solid. Powder

98.00%

Store at -20 degree C for 3 years powder
-80 degree C for 2 years in solvent

380.46

DMSO: 30mg/mL (78.85mM)
(<1mg/ml refers to the product slightly soluble or insoluble)

C21H20N2O3S

CN(CC1)CCN1C(c1ccc(-c(ccc2c3C=O)cc2ccc3O)s1)=O

1093119-54-0

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].

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].