[CAS NO. 1609452-30-3] SEL120 (SEL120-34A) hydrochloride
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PRODUCTS SPECIFICATIONS [1609452-30-3]
Store
Catalog
SLK-S8840
Brand
Selleck
CAS
1609452-30-3
DESCRIPTION [1609452-30-3]
Overview
| MDL | MFCD31692363 |
|---|---|
| Molecular Weight | 450.60 |
| Molecular Formula | C15H18Br2N4.xHCl |
| SMILES | CC1=C2C3=C(C(Br)=C1Br)CCCN3C(N4CCNCC4)=N2.[H]Cl |
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
SEL120 (SEL120-34, SEL120-34A) is a novel inhibitor of with IC50 values of 4.4 nM and 10.4 nM for CDK8/Cyclin C and CDK19/CyclinC respectively.
In vitro
SEL120-34A inhibits kinase activities of CDK8/CycC and CDK19/CycC complexes with an IC50 of 4.4 nM and 10.4 nM, respectively. It does not significantly inhibit other members of the CDK family in a single point inhibition assay, namely CDK1, 2, 4, 6, 5, 7 in vitro, with the exception of CDK9, however a calculated IC50 1070 nM, indicated an over 200 fold selectivity against this kinase. SEL120-34A inhibits phosphorylation of STAT1 S727 and STAT5 S726 in cancer cells, inhibits mitogen- induced expression of immediate early response (IER) genes and IFN- responsive genes expression in vitro. In a broad panel of cancer cell lines, the compound shows the strongest activity in hematological malignancies, especially in selected acute myeloid leukemia (AML) (GI50 12 nM), acute lymphoblastic leukemia (ALL) and mantle cell lymphoma (MCL) models. SEL120−34A could alter transcriptional programs linked to differentiation of leukemia cells.
References
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