SEL120(SEL120-34,SEL120-34A)

Catalog No.S8840

SEL120(SEL120-34,SEL120-34A) Chemical Structure

Molecular Weight(MW): 450.6

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.

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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

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].

Assay
Methods Test Index PMID
Western blot
CDK8 / ERK; 

PubMed: 28422713     


SEL120-34A competitively inhibits CDK8 binding to ATP -desthiobiothin probes (ActivX) in KG-1 AML cell lysate; ERK1/2 was used as a control. CDK8 and ERK1/2 proteins in precipitates were revealed by WB.

pSTAT1 pS727 / pSTAT1 pY701 / STAT1 / pSTAT5 pS726 / pSTAT5 pY694 / STAT5; 

PubMed: 28422713     


SEL120-34A inhibits serine phosphorylation of STAT1 S727 and STAT5 S726, whereas Ruxolitinib inhibits tyrosine phosphorylation of STAT1 Y701 and STAT5 Y694 in JAK2 V617F cells. SET-2 cells were treated with Ruxolitinib, SEL120-34A or vehicle DMSO (C) for 24 hours and protein levels of pS727, pY701 STAT1 and pS726, pY694 STAT5 were measured by WB.

28422713
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].

Protocol

Cell Research:

[1]

+ Expand
  • 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.


    (Only for Reference)
Animal Research:

[1]

+ Expand
  • Animal Models: SCID/beige C.B17 female mice xenografted with Colo-205 tumors
  • Formulation: water
  • Dosages: 5, 15, 30 and 60 mg/kg BID
  • Administration: oral
    (Only for Reference)

Solubility (25°C)

In vitro Water 90 mg/mL (199.73 mM)
DMSO 11 mg/mL (24.41 mM)
Ethanol Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 450.6
Formula

C15H19Br2ClN4

CAS No. 1609522-33-9
Storage powder
in solvent
Synonyms N/A

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Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

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Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

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* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

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  • Computed Result

  • C1=C0/X C1: LOG(C1):
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    C8=C7/X C8: LOG(C8):
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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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CDK Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID