[CAS NO. 438190-29-5] SMI-4a
Please click "REQUEST A QUOTE" button if you need other sizes or
custom synthesis
request a quote
If there is no stock, or you need other sizes or custom synthesis,
please:
PRODUCTS SPECIFICATIONS [438190-29-5]
Catalog
SLK-S8005
Brand
Selleck
CAS
438190-29-5
DESCRIPTION [438190-29-5]
Overview
| MDL | MFCD01152003 |
|---|---|
| Molecular Weight | 273.23 |
| Molecular Formula | C11H6F3NO2S |
| SMILES | O=C(NC/1=O)SC1=C/C2=CC=CC(C(F)(F)F)=C2 |
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.)
Description
SMI-4a (TCS PIM-1 4a) is a potent inhibitor of Pim1 with IC50 of 17 nM, modestly potent to Pim-2, does not significantly inhibit any other serine/threonine- or tyrosine-kinases.
Features
SMI-4a (5μM) synergizes with rapamycin (5 nM) to cause significant growth inhibition of leukemic cells.
Targets
| Pim1 [1] (Cell-free assay) |
| 17 nM |
In vitro
SMI-4a is an ATP competitive inhibitor of Pim1 with IC50 of 17 nM. SMI-4a shows high selectivity for Pim1 against a panel of kinases. SMI-4a inhibits the in vitro phosphorylation by Pim-1 of the known substrate, the translational repressor 4E-BP1. SMI-4a (5μM) inhibits pancreatic and leukemic cells growth. SMI-4a reduces phosphorylation of the Pim target Bad in prostate and hematopoietic cells. SMI-4a causes cell cycle arrest and reverses the antiapoptotic activity of Pim-1. SMI-4a increases the amount of p27Kip1 in the nucleus. SMI-4a treatment of pre-T-LBL inhibits the mTOR pathway. SMI-4a reduces MYC protein expression in pre-T-LBL. SMI-4a treatment induces up-regulation of MAPK pathway.
In vivo
SMI-4a (60 mg/Kg) treatment twice daily significantly reduce tumor size and is well tolerated. Tumors harvested 1 hour after the final oral gavage of SMI-4a demonstrates decreased phosphorylation of p70 S6K compared with tumors from mice treated with vehicle, whereas in comparison total p70 S6K expression isunchanged.
References
Powered by Arctom Copyright © 2025 Arctom.
All rights reserved.