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    Checkpoint Kinase (Chk)

    Checkpoint Kinases (Chk) are protein kinases that are involved in cell cycle control. Two checkpoint kinase subtypes have been identified, Chk1 and Chk2. Chk1 is a central component of genome surveillance pathways and is a key regulator of the cell cycle and cell survival. Chk1 is required for the initiation of DNA damage checkpoints and has recently been shown to play a role in the normal (unperturbed) cell cycle. Chk1 impacts various stages of the cell cycle including the S phase, G2/M transition and M phase. In addition to mediating cell cycle checkpoints, Chk1 also contributes to DNA repair processes, gene transcription, embryo development, cellular responses to HIV infection and somatic cell viability. Chk2 is a protein kinase that is activated in response to DNA damage and is involved in cell cycle arrest. In response to DNA damage and replication blocks, cell cycle progression is halted through the control of cell cycle regulators. The protein encoded by this gene is a cell cycle checkpoint regulator and putative tumor suppressor.

    Products

    Catalog No. Name Description
    GY01128 Special AZD7762 AZD-7762 is a potent ATP-competitive checkpoint kinase (Chk) inhibitor in with IC50 of 5 nM for Chk1.
    GY01196 Special SCH900776 SCH900776 is a potent, selective and orally bioavailable inhibitor of checkpoint kinase1 (Chk1) with IC50 of 3 nM, and has much greater selectivity than Chk2 (IC50=1500 nM) and cyclin-dependent kinase CDK2 (IC50=160 nM).
    GY02280 Special LY2606368 LY2606368 is a potent and selective ATP competitive inhibitor of the Chk1 protein kinase, with IC50s of <1 nM and 8 nM for CHK1 and CHK2, respectively, and a Ki of 0.9 nM against purified CHK1.
    GY02503 Special CCT244747 CCT244747 is a potent, orally bioavailable and highly selective CHK1 inhibitor, with an IC50 of 7.7 nM; also abrogates G2 checkpoint with an IC50 of 29 nM.
    GY01252 LY2603618 LY2603618 is a potent and selective inhibitor of Chk1 protein kinase activity in vitro with IC50 of 7 nM.
    GY01339 CHIR-124 CHIR-124 is a potent and selective Chk1 inhibitor with IC50 of 0.3 nM, and also potently targets PDGFR and FLT3 with IC50s of 6.6 nM and 5.8 nM.
    GY01354 PF 477736 PF 477736 is a potent, selective ATP-competitive inhibitor of Chk1, with a Ki of 0.49 nM, 100-fold selectivity versus Chk2 (Ki, 47 nM).
    GY02281 Prexasertib (LY2606368) 2HCl LY2606368 dihydrochloride is a potent and selective ATP competitive inhibitor of the Chk1 protein kinase, with IC50s of <1 nM and 8 nM for CHK1 and CHK2, respectively, and a Ki of 0.9 nM against purified CHK1.
    GY02328 CCT241533 CCT241533 is a potent and selective ATP competitive inhibitor of CHK2 with an IC50 of 3 nM and Ki of 1.16 nM.
    GY02560 CCT241533 HCl CCT241533 hydrochloride is a potent and selective ATP competitive inhibitor of CHK2 with an IC50 of 3 nM and Ki of 1.16 nM.
    GY02620 CCT245737 CCT245737 is a orally active and seletive Chk1 inhibitor, with an IC50 of 1.3 nM; shows much less activity against Chk2, with an IC50 of 2440 nM.
    GY03334 BML-277 BML-277 is a selective checkpoint kinase 2 (Chk2) inhibitor with an IC50 of 15 nM.
    GY03898 GDC0575 GDC0575(ARRY-575,RG7441)is a small molecule inhibitor of cell cycle checkpoint kinase 1 (Chk1), with potential chemosensitization activity.
    GY03968 SB218078 SB218078 is an inhibitor of checkpoint kinase 1 (Chk1) that displays selectivity over other protein kinases (IC50 values are 15, 250 and 1000 nM for Chk1, cdc2 and PKC respectively).
    GY05062 VRX-0466617 A potent and selective Chk2 inhibitor with Ki/IC50 of 11 nM/120 nM.
    GY05110 NSC-109555 ditosylate A potent, selective, reversible, ATP-competitive Chk2 inhibitor with IC50 of 0.2 uM.
    GY05117 XL-844 A potent, specific, orally available, ATP‑competitive inhibitor of Chk1 and Chk2 with Ki of 2.2 nM and 0.07 nM, respectively.
    GY05217 BAY-1816032 BAY-1816032 is a highly potent, selective, orally active BUB1 mitotic checkpoint serine/threonine kinase with IC50 of 7 nM, displays excellent selectivity on a panel of 395 kinases.
    GY05222 SAR-020106 A potent, selective, ATP-competitive Chk1 inhibitor with IC50 of 13.3 nM.
    GY05345 GDC-0425 A potent, selective and orally active Chk1 inhibitor.
    GY05346 GNE-900 GNE-900 (GNE900) is a potent, selective, ATP-competitive, and orally bioavailable Chk1 inhibitor with IC50 of <1 nM.
    GY05347 GDC-0575 GDC-0575 (ARRY-575, RG-7741) is a potent, selective and orally bioavailable Chk1 inhibitor with IC50 of 1.2 nM.
    GY05355 VER-158411 A potent, selective, ATP-competitive Chk1 and Chk2 inhibitor with IC50 of 4.4 nM and 4.5 nM, respectively.
    GY05639 VER-250840 A potent, selective, orally active Chk1 inhibitor with IC50 of < 1 nM, Ki=69 pM.
    GY05644 PV-1019 A potent, ATP-competitive and highly selective Chk2 inhibitor with IC50 of 138 nM.
    GY06979 PD-321852 A potent, reasonably selective Chk1 inhibitor with cell IC50 of 5 nM
    GY06980 Debromohymenialdisine A marine sponge alkaloid that inhibits Chk1 and Chk2 with IC50 of 3 and 3.5 uM, respectively
    GY07052 MU 380 A novel potent, selective CHK1 inhibitor 2 nM, >80-fold selectivity over CHK2