[CAS NO. 1093119-54-0] MKC-3946
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PRODUCTS SPECIFICATIONS [1093119-54-0]
Catalog
SLK-S8286
Brand
Selleck
CAS
1093119-54-0
DESCRIPTION [1093119-54-0]
Overview
| MDL | MFCD30496700 |
|---|---|
| Molecular Weight | 380.46 |
| Molecular Formula | C21H20N2O3S |
| SMILES | O=CC1=C2C=CC(C3=CC=C(C(N4CCN(C)CC4)=O)S3)=CC2=CC=C1O |
For research use only.
Storage
3 years,-20°C,powder
1 years,-80°C,in solvent
1 years,-80°C,in solvent
Shipping
Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)
Preparing Stock Solutions
| 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.6284 mL | 13.1420 mL | 26.2840 mL |
| 5 mM | 0.5257 mL | 2.6284 mL | 5.2568 mL |
| 10 mM | 0.2628 mL | 1.3142 mL | 2.6284 mL |
| 50 mM | 0.0526 mL | 0.2628 mL | 0.5257 mL |
Description
MKC3946 is a potent and soluble inhibitor which triggered modest growth inhibition in multiple myeloma cell lines, without toxicity in normal mononuclear cells.
Targets
| IRE1α endoribonuclease [1] |
In vitro
MKC-3946 triggers modest growth inhibition in MM cell lines, without toxicity in normal mononuclear cells. Importantly, it significantly enhances cytotoxicity induced by bortezomib or 17-AAG, even in the presence of bone marrow stromal cells or exogenous IL-6. Both bortezomib and 17-AAG induce ER stress, evidenced by induction of XBP1s, which is blocked by MKC-3946. Apoptosis induced by these agents is enhanced by MKC-3946, associated with increased CHOP. MKC-3946 treatment does not inhibit IRE1α kinase function or binding of activated IRE1α to TRAF2 and downstream JNK signaling.
In vivo
MKC-3946 inhibits XBP1 splicing in a model of ER stress in vivo, associated with significant growth inhibition of MM cells.
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