2. Signaling Pathways
  3. Cell Cycle/DNA Damage
  4. Checkpoint Kinase (Chk)
  5. Chk2 Isoform

Chk2

Checkpoint kinase Chk2 (CHEK2) is a serine/threonine kinase and key DNA damage response component that coordinates checkpoint activation, DNA repair, apoptosis, senescence, or damage tolerance after genotoxic stress[1]. Mechanistically, ATM-mediated Thr68 phosphorylation triggers CHK2 dimerization through phospho-Thr68-FHA interactions, followed by activation-loop autophosphorylation and kinase activation[2]. Activated CHK2 connects DNA damage signaling to p53 stabilization, BRCA1 phosphorylation, and cell-cycle control, therefore supporting genome integrity research in cancer models[3][4]. In disease contexts, CHK2 functions as a tumor-suppressive kinase linked to cancer susceptibility, while experimental data also show context-dependent roles in DNA damage-induced apoptosis and checkpoint arrest[5][6]. Compared with Chk1, CHK2 is structurally distinct and is activated mainly by DNA damage, whereas Chk1 has a broader role in S-phase and G2 checkpoint control[6]. For experimental applications, the selective CHK2 inhibitor CCT241533 blocks CHK2 activity in tumor cell lines after DNA damage and potentiates cytotoxicity of PARP inhibitors, supporting pathway-dissection studies rather than unsupported monotherapy claims[7].- CHK2 links ATM-driven DNA damage signaling to p53, BRCA1, apoptosis, and checkpoint control. - CHK2 differs from Chk1 in activation pattern, checkpoint dependence, and experimental inhibitor utility.

Cat. No. Product Name Effect Purity
  • HY-18174
    Prexasertib
    		Inhibitor 99.64%
    Prexasertib (LY2606368) is a selective, ATP-competitive second-generation checkpoint kinase 1 (CHK1) inhibitor with a Ki of 0.9 nM and an IC50 of <1 nM. Prexasertib inhibits CHK2 (IC50=8 nM) and RSK1 (IC50=9 nM). Prexasertib causes double-stranded DNA breakage and replication catastrophe resulting in apoptosis. Prexasertib shows potent anti-tumor activity.
  • HY-10992
    AZD-7762
    		Inhibitor 99.94%
    AZD-7762 is a potent ATP-competitive checkpoint kinase (Chk) inhibitor in with an IC50 of 5 nM for Chk1.
  • HY-14720
    Rabusertib
    		Inhibitor 99.98%
    Rabusertib (LY2603618) is a potent and selective inhibitor of Chk1 with an IC50 of 7 nM.
  • HY-13946
    BML-277
    		Inhibitor 99.67%
    BML-277 is a selective checkpoint kinase 2 (Chk2) inhibitor with an IC50 of 15 nM.
  • HY-18958
    CCT245737
    		Inhibitor 99.48%
    CCT245737 (SRA737) is an orally active and seletive Chk1 inhibitor, with an IC50 of 1.3 nM.
  • HY-112477A
    (E/Z)-Chk2-IN-1
    		Inhibitor
    (E/Z)-Chk2-IN-1 ((E/Z)-Hymenialdisine analogue-1) (Compound 1) is a potent and selective cell cycle kinase Chk2 inhibitor with an IC50 of 8 nM. (E/Z)-Chk2-IN-1 exhibits low inhibitory activity against other kinases (such as CK1δ, MEK1, and PKCα/βⅡ) with IC50 values both >89 nM. (E/Z)-Chk2-IN-1 can be used for the research of cancer.
  • HY-15532
    SCH900776
    		Inhibitor 99.97%
    SCH900776 (MK-8776) is a potent, selective and orally bioavailable inhibitor of checkpoint kinase1 (Chk1) with an IC50 of 3 nM. SCH900776 shows 50- and 500-fold selectivity over CDK2 and Chk2, respectively.
  • HY-14715B
    CCT241533 hydrochloride
    		Inhibitor 98.55%
    CCT241533 hydrochloride is a potent and selective CHK2 inhibitor with an IC50 of 3 nM and a Ki of 1.16 nM.
  • HY-13263
    CHIR-124
    		Inhibitor 99.05%
    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.
  • HY-10032
    PF 477736
    		Inhibitor 99.04%
    PF 477736 (PF 00477736) is a potent, selective and ATP-competitive inhibitor of Chk1, with a Ki of 0.49 nM, it is also a Chk2 inhibitor, with a Ki of 47 nM. PF 477736 shows <100-fold selectivity for Chk1 over VEGFR2, Fms, Yes, Aurora-A, FGFR3, Flt3, and Ret (IC50=8 (Ki), 10, 14, 23, 23, 25, and 39 nM, respectively). PF 477736 can enhance Gemcitabine antitumor activity in vitro and in vivo.
  • HY-18174A
    Prexasertib dihydrochloride
    		Inhibitor 99.73%
    Prexasertib dihydrochloride (LY2606368 dihydrochloride) is a selective, ATP-competitive second-generation checkpoint kinase 1 (CHK1) inhibitor with a Ki of 0.9 nM and an IC50 of <1 nM. Prexasertib dihydrochloride inhibits CHK2 (IC50=8 nM) and RSK1 (IC50=9 nM). Prexasertib dihydrochloride causes double-stranded DNA breakage and replication catastrophe resulting in apoptosis. Prexasertib dihydrochloride shows potent anti-tumor activity.
  • HY-18174E
    Prexasertib dimesylate
    		Inhibitor 98.90%
    Prexasertib dimesylate (LY2606368 dimesylate) is a selective, ATP-competitive second-generation checkpoint kinase 1 (CHK1) inhibitor with a Ki of 0.9 nM and an IC50 of <1 nM. Prexasertib dimesylate inhibits CHK2 (IC50=8 nM) and RSK1 (IC50=9 nM). Prexasertib dimesylate causes double-stranded DNA breakage and replication catastrophe resulting in apoptosis. Prexasertib dimesylate shows potent anti-tumor activity.
  • HY-125203
    PV-1019
    		Inhibitor 99.30%
    PV-1019 (NSC 744039) is a potent, selective Chk2 inhibitor with an IC50 value of 24 nM. PV-1019 inhibits the Topotecan (HY-13768)-induced Chk2 autophosphorylation. PV-1019 inhibits IR-induced apoptosis.
  • HY-153857
    Lasmotinib
    		Inhibitor 98.16%
    Lasmotinib (PHI-101) is a FLT3 and CHK2 inhibitor. Lasmotinib potently inhibits FLT3 single activating mutations (ITD or TKD mutants) and has inhibitory activity against FLT3 double (ITD/D835Y or ITD/F691L) and triple (ITD/D835Y/F691L) resistance mutations. Lasmotinib synergizes with Venetoclax (HY-15531) or Azacytidine to inhibit leukemia. Lasmotinib exhibits anticancer activity against ovarian and breast cancer.
  • HY-117102
    ANI-7
    		Activator 99.01%
    ANI-7 is an activator of aryl hydrocarbon receptor (AhR) pathway. ANI-7 inhibits the growth of multiple cancer cells, and potently and selectively inhibits the growth of MCF-7 breast cancer cells with a GI50 of 0.56 μM. ANI-7 induces CYP1-metabolizing mono-oxygenases by activating AhR pathway, and also induces DNA damage, checkpoint Kinase 2 (Chk2) activation, S-phase cell cycle arrest, and cell death in sensitive breast cancer cell lines.
  • HY-B1165
    Cyproheptadine (hydrochloride sesquihydrate)
    		Activator 99.74%
    Cyproheptadine hydrochloride sesquihydrate acts as a p38 MAP kinase activator, CHK2 activator, histamine H1 receptor inhibitor and serotonin receptor inhibitor. Cyproheptadine hydrochloride sesquihydrate mediates cell cycle arrest via G1 phase arrest, G1/S transition arrest, G0/G1 phase arrest, reduced expression of cyclins D1/D2/D3, upregulated expression of HBP1, p16, p21, p27, and decreased phosphorylation of retinoblastoma protein. Cyproheptadine hydrochloride sesquihydrate induces Apoptosis by increasing PARP and cleaved PARP, as well as activating the mitochondrial caspase pathway. Cyproheptadine hydrochloride sesquihydrate inhibits tumor growth with extremely low toxicity to normal cells. Cyproheptadine hydrochloride sesquihydrate can be used in research related to hepatocellular carcinoma, multiple myeloma and acute myeloid leukemia.
  • HY-15883
    GNE-900
    		Inhibitor 98.58%
    GNE-900 is a an ATP-competitive, selective, and orally active ChK1 inhibitor with IC50s of 0.0011, 1.5 μM for ChKl, ChK2, respectively. GNE-900 abrogates the G2-M checkpoint, enhances DNA damage, and induces Apoptosis. Gemcitabine (HY-17026) and GNE-900 administration shows anti-tumor activity.
  • HY-10992A
    AZD-7762 hydrochloride
    		Inhibitor 99.58%
    AZD-7762 hydrochloride is a potent ATP-competitive checkpoint kinase (Chk) inhibitor in with an IC50 of 5 nM for Chk1.
  • HY-14715
    CCT241533
    		Inhibitor
    CCT241533 is a potent and selective ATP competitive inhibitor of CHK2 with an IC50 of 3 nM and Ki of 1.16 nM.
  • HY-18174B
    Prexasertib Mesylate Hydrate
    		Inhibitor
    Prexasertib Mesylate Hydrate (LY2606368 Mesylate Hydrate) is a selective, ATP-competitive second-generation checkpoint kinase 1 (CHK1) inhibitor with a Ki of 0.9 nM and an IC50 of <1 nM. Prexasertib Mesylate Hydrate inhibits CHK2 (IC50=8 nM) and RSK1 (IC50=9 nM). Prexasertib Mesylate Hydrate causes double-stranded DNA breakage and replication catastrophe resulting in apoptosis. Prexasertib Mesylate Hydrate shows potent anti-tumor activity.
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity