A Chk2 inhibitor (IC50 = 13.5 nM); selective for Chk2 over Chk1 (IC50 = 220.4 nM); inhibits Chk2 autophosphorylation at Ser516 in non-cancerous 184B5 cells that contain wild-type p53 and in MDA-MB-231 cells that contain mutated p53 at 0.1-30 µM; enhances survival of 184B5

Chk2 Inhibitor – 1 mg

Brand:
Cayman
CAS:
724708-21-8
Storage:
-20
UN-No:
Non-Hazardous - /

Chk2 inhibitor is an inhibitor of checkpoint kinase 2 (Chk2; IC50 = 13.5 nM).{48513} It is selective for Chk2 over Chk1 (IC50 = 220.4 nM). It inhibits Chk2 autophosphorylation at the serine in position 516 in non-cancerous 184B5 cells that contain wild-type p53 and in MDA-MB-231 cells that contain mutated p53 when used at concentrations ranging from 0.1 to 30 µM. Chk2 inhibitor enhances survival of 184B5, but not MDA-MB-231, cells following ionizing radiation and inhibits cell cycle arrest at the G2 stage induced by ionizing radiation in 184B5 cells. It also inhibits the production of IL-2 in Jurkat cells stimulated by phorbol 12-myristate 13-acetate (PMA; Item No. 10008014) and the production of TNF-α in LPS-stimulated THP-1 cells (IC50s = 3.5 and 8.2 µM, respectively).{48514} Chk2 inhibitor also inhibits the growth of CEM leukemia T cells (GI50 = 1.73 µM).  

 

Out of stock

Add to quotes
SKU: 21184 - Category:

Description

A Chk2 inhibitor (IC50 = 13.5 nM); selective for Chk2 over Chk1 (IC50 = 220.4 nM); inhibits Chk2 autophosphorylation at Ser516 in non-cancerous 184B5 cells that contain wild-type p53 and in MDA-MB-231 cells that contain mutated p53 at 0.1-30 µM; enhances survival of 184B5, but not MDA-MB-231, cells following ionizing radiation; inhibits PMA-induced production of IL-2 in Jurkat cells and LPS-induced TNF-α production in THP-1 cells (IC50s = 3.5 and 8.2 µM, respectively); inhibits the growth of CEM leukemia T cells (GI50 = 1.73 µM)

Formal name: (5Z)-5-(2-amino-1,5-dihydro-5-oxo-4H-imidazol-4-ylidene)-3,4,5,10-tetrahydro-azepino[3,4-b]indol-1(2H)-one

Synonyms:  SC-203885

Molecular weight: 295.3

CAS: 724708-21-8

Purity: ≥95%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|Checkpoint Kinases||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Cell Cycle|G2/M||Research Area|Cancer|Cell Cycle|G2/S||Research Area|Cancer|Cell Signaling|p53 Signaling||Research Area|Cancer|Transcription Factors|p53||Research Area|Cell Biology|Cell Cycle||Research Area|Cell Biology|Cell Death|Apoptosis||Research Area|Immunology & Inflammation|Adaptive Immunity||Research Area|Immunology & Inflammation|Innate Immunity

Related products

  • A zwitterionic glycerophospholipid commonly used in the formation of lipid monolayers

    1,2-Dipalmitoyl-sn-glycero-3-PC – 50 mg

    1,2-Dipalmitoyl-sn-glycero-3-PC (DPPC) is a zwitterionic glycerophospholipid commonly used in the formation of lipid monolayers, bilayers, and liposomes for use in a variety of applications.{14480,24261,14478,14479} It has been used in the formation of proteoliposomes for implantation of γ-glutamyl transpeptidase into human erythrocyte membranes.{14478} Incorporation of glycosphingolipid antigens into DPPC-containing liposomes increases the immunogenicity of the antigens in mice.{14479}  

     

    Brand:
    Cayman
    SKU:10009473 - 50 mg

    Available on backorder

    Add to quotes
    View product page
  • A potent inhibitor of Cdk2/cyclin E with an IC50 value of 0.1 µM; also inhibits Cdk7/cyclin H

    (R)-Roscovitine – 500 µg

    Cyclin-dependent kinases (CDKs) are key regulators of cell cycle progression and are therefore promising targets for cancer therapy. (R)-Roscovitine is a potent inhibitor of Cdk2/cyclin E with an IC50 value of 0.1 µM.{14988} It also inhibits Cdk7/cyclin H, Cdk5/p35, and cell division cycle (cdc)/cyclin B with IC50 values of 0.49, 0.16, and 0.65 µM, respectively.{14987,14988,14991} (R)-Roscovitine inhibits the growth of rapidly proliferating cells with an average IC50 value of 15.2 µM against a panel of 19 human tumor cell lines.{14988} In murine models of polycystic kidney disease, (R)-roscovitine effectively inhibited disease progression at doses of 50-100 mg/kg.{14564}  

     

    Brand:
    Cayman
    SKU:10009569 - 500 µg

    Available on backorder

    Add to quotes
    View product page
  • A potent inhibitor of Cdk2/cyclin E with an IC50 value of 0.1 µM; also inhibits Cdk7/cyclin H

    (R)-Roscovitine – 10 mg

    Cyclin-dependent kinases (CDKs) are key regulators of cell cycle progression and are therefore promising targets for cancer therapy. (R)-Roscovitine is a potent inhibitor of Cdk2/cyclin E with an IC50 value of 0.1 µM.{14988} It also inhibits Cdk7/cyclin H, Cdk5/p35, and cell division cycle (cdc)/cyclin B with IC50 values of 0.49, 0.16, and 0.65 µM, respectively.{14987,14988,14991} (R)-Roscovitine inhibits the growth of rapidly proliferating cells with an average IC50 value of 15.2 µM against a panel of 19 human tumor cell lines.{14988} In murine models of polycystic kidney disease, (R)-roscovitine effectively inhibited disease progression at doses of 50-100 mg/kg.{14564}  

     

    Brand:
    Cayman
    SKU:10009569 - 10 mg

    Available on backorder

    Add to quotes
    View product page
  • A small molecule activator of stem cell renewal that allows the propagation of OG2 mES cells for at least 10 passages in an undifferentiated state; activity is mediated by the combined inhibition of RasGAP and ERK1 with Kd values of 98 and 212 nM

    SC-1 – 10 mg

    The maintenance of embryonic stem cells in culture typically requires feeder cells and various exogenous factors found in serum. Murine embryonic stem (mES) cells can be maintained in the absence of feeder cells and serum but require the leukemia inhibitor factor (LIF) and bone morphogenic protein (BMP) to prevent differentiation and promote self-renewal. SC-1 is a small molecule activator of stem cell renewal that allows the propagation of OG2 mES cells for at least 10 passages in an undifferentiated state.{14533} The activity of SC-1 is mediated by the combined inhibition of RasGAP and ERK1 with Kd values of 98 and 212 nM, respectively.{14533} Inhibition of RasGAP increases Ras signaling via the PI3-kinase pathway which promotes self-renewal, whereas inhibition of ERK blocks differentiation.  

     

    Brand:
    Cayman
    SKU:10009557 - 10 mg

    Available on backorder

    Add to quotes
    View product page