Home Cell Cycle CDK inhibitor SEL120 (SEL120-34A) hydrochloride For research use only.

SEL120 (SEL120-34A) hydrochloride

Synonyms: SEL120-34

SEL120 (SEL120-34, SEL120-34A) is a novel inhibitor of Cyclin-dependent kinase 8 (CDK8) with IC50 values of 4.4 nM and 10.4 nM for CDK8/Cyclin C and CDK19/CyclinC respectively.

SEL120 (SEL120-34A) hydrochloride Chemical Structure

SEL120 (SEL120-34A) hydrochloride Chemical Structure

CAS No. 1609452-30-3

Purity & Quality Control

SEL120 (SEL120-34A) hydrochloride Related Products

Signaling Pathway

CDK Signaling Pathways

CDK Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HL60 Growth inhibition assay Growth inhibition of human HL60 cells by alamar blue assay, GI50<1μM 29266937
SKNO1 Growth inhibition assay Growth inhibition of human SKNO1 cells by alamar blue assay, GI50<1μM 29266937
KG1 Growth inhibition assay Growth inhibition of human KG1 cells by alamar blue assay, GI50<1μM 29266937
MOLM16 Growth inhibition assay Growth inhibition of human MOLM16 cells by alamar blue assay, GI50<1μM 29266937
MV4-11 Growth inhibition assay Growth inhibition of human MV4-11 cells by alamar blue assay, GI50<1μM 29266937
OCI-AML2 Growth inhibition assay Growth inhibition of human OCI-AML2 cells by alamar blue assay, GI50<1μM 29266937
OCI-AML3 Growth inhibition assay Growth inhibition of human OCI-AML3 cells by alamar blue assay, GI50<1μM 29266937
MOLM6 Growth inhibition assay Growth inhibition of human MOLM6 cells by alamar blue assay, GI50<1μM 29266937
Click to View More Cell Line Experimental Data

Biological Activity

Description SEL120 (SEL120-34, SEL120-34A) is a novel inhibitor of Cyclin-dependent kinase 8 (CDK8) with IC50 values of 4.4 nM and 10.4 nM for CDK8/Cyclin C and CDK19/CyclinC respectively.
Targets
CDK8 [1]
(Cell-free assay)		 CDK19 [1]
(Cell-free assay)
4.4 nM 10.4 nM
In vitro
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[1]. 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[2].
Cell Research Cell lines HCT-116 cells
Concentrations 0.1, 0.25, 0.5, 1, 2.5, 5 μM
Incubation Time 5 h
Method

HCT-116 are seeded onto 6-well plates at 2.5×105/well. On the following day, cells are synchronized for 24 h by 0.5% FBS starvation, pretreated with 0.1% DMSO or SEL120-34A at the indicated concentration for 1 h and then supplemented with either 10% FBS, IFNg or IFNa in the presence of the inhibitor (4h). Cells are centrifuged at 1300 rpm for 5 min at 4°C, washed once with 1 ml of ice-cold PBS and stored at -80°C.
Experimental Result Images Methods Biomarkers Images PMID
Western blot CDK8 / ERK pSTAT1 pS727 / pSTAT1 pY701 / STAT1 / pSTAT5 pS726 / pSTAT5 pY694 / STAT5 28422713
In Vivo
In vivo

SEL120-34A has favorable pharmacodynamics to be sufficient to affect expression of CDK8 and CDK19- dependent genes in vivo. SEL120-34A treatment causes specific alterations in interferon- responsive genes and inhibits the proliferation of AML cell lines in vivo. SEL120-34A does not affect normal hematopoiesis[1]. SEL120−34A effectively inhibits tumor growth in subcutaneous responder AML and MCL models when administered orally[2].
Animal Research Animal Models SCID/beige C.B17 female mice xenografted with Colo-205 tumors
Dosages 5, 15, 30 and 60 mg/kg BID
Administration oral

Chemical Information & Solubility

Molecular Weight Formula

C15H18Br2N4.xHCl
CAS No. 1609452-30-3 SDF --
Smiles CC1=C2C3=C(CCCN3C(=N2)N4CCNCC4)C(=C1Br)Br
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

Water : 90 mg/mL

DMSO : 1 mg/mL ( Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : ˂1 mg/mL


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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