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

Checkpoint Kinase (Chk) Inhibitor

Checkpoint Kinase (Chk) Inhibitors (15):

Cat. No. Product Name Effect Purity
  • HY-P99032
    Monalizumab
    		Inhibitor 99.08%
    Monalizumab (IPH2201) is an immune checkpoint inhibitor targeting Natural Killer Group 2A (NKG2A). Monalizumab, a humanized anti-NKG2A blocking mAb, increases IFN-γ production, thereby promoting NK cell effector functions. Monalizumab can be used for the research of head and neck squamous cell carcinoma (HNSCC).
  • HY-112167
    GDC-0575
    		Inhibitor 99.50%
    GDC-0575 (ARRY-575, RG7741) is a highly-selective oral small-molecule Chk1 inhibitor with an IC50 of 1.2 nM.
  • HY-148962
    LY2880070
    		Inhibitor 98.01%
    LY2880070 is an orally active CHK1 inhibitor, IC50 ＜ 1 nM. LY2880070 can be used as an anticancer agent for combination with DNA damaging agents.
  • HY-103367
    CHK1-IN-7
    		Inhibitor ≥98.0%
    CHK1-IN-7 (Compound 10c) is a potent human CHK1 inhibitor. CHK1-IN-7 shows no single agent effect, potentiates the antiproliferative effect of Gemcitabine HY-17026 in both prostate and breast cancer cell lines. CHK1-IN-7 can be used for the research of cancer.
  • HY-112927
    MU380
    		Inhibitor
    MU380 is a potent and selective CHK1 inhibitor that induces apoptosis and has anticancer activity.
  • HY-124122
    BPTQ
    		Inhibitor
    BPTQ is a potent inhibitor against VEGFR1/Flt-1 and CHK2 with IC50 values of 0.54 and 1.70 µmol/L, respectively. BPTQ is also an intercalator of DNA with anticancer activities. BPTQ inhibits the proliferation of HL-60 cells by arresting cells at S and G2/M phase with an IC50 value of 12 µmol/L. BPTQ also activates the mitochondria-mediated Apoptosis pathway by a decrease in mitochondrial membrane potential, increase in the Bax:Bcl-2 ratio and activation of caspases.
  • HY-106009
    VRX0466617
    		Inhibitor 99.91%
    VRX0466617, a selective Chk2 inhibitor, inhibits the phosphorylation of Chk2 Ser 19 and Ser33-35. VRX0466617 can be used in the study of cancer.
  • HY-128766A
    CHK1-IN-4 hydrochloride
    		Inhibitor
    CHK1-IN-4 hydrochloride (Compound 3) is a potent checkpoint kinase 1 (chk1) inhibitor, and potently inhibits chk1 phosphorylation in the tumor cells. CHK1-IN-4 hydrochloride has anti-tumor activity.
  • HY-123597
    NSC 109555
    		Inhibitor
    NSC 109555 (DDUG; NCI C04808) is an ATP-competitive inhibitor of checkpoint kinase 2 (Chk2; IC50=200 nM). NSC 109555 also inhibits Brk, c-Met, IGFR, and LCK with IC50 values ??of 210, 6,000, 7,400, and 7,100 nM, respectively. NSC 109555 inhibits Chk2 autophosphorylation and phosphorylation of the Chk2 substrate histone H1 in vitro (IC50=240 nM), and also inhibits the growth of L1210 leukemia cells and induces autophagy in vitro. NSC 109555 enhances Gemcitabine (HY-17026)-induced reactive oxygen species (ROS) production in MIA PaCa-2 cells.
  • HY-161622
    K1586
    		Inhibitor
    K1586 is an amidine derivative that efficiently targets Chk1. K1586 enhances the degradation of Chk1 that sensitizes colorectal cancer cells to ionizing radiation. K1586 shows anticancer effects.
  • HY-P4978
    CBP501 Affinity Peptide
    		Inhibitor
    CBP501 Affinity Peptide is a Chk kinase inhibitor that can abrogate G2 arrest induced by DNA-damaging agents. CBP501 Affinity Peptide can be used in cancer research.
  • HY-151559
    Zn-DPA-maytansinoid conjugate 1
    		Inhibitor
    Zn-DPA-maytansinoid conjugate 1 is a small molecule-based maytansinoid conjugate targeting immune checkpoint. Zn-DPA-maytansinoid conjugate 1 induces lasting regression of tumor growth and rejuvenates tumor microenvironment (TME) to an "inflamed hot tumor" .
  • HY-162367
    FLT3/CHK1-IN-2
    		Inhibitor
    FLT3/CHK1-IN-2 (Compound 30) is a dual inhibitor of FLT3 and CHK1, with IC50s of 25.63, 16.39, 22.80 nM for CHK1, FLT3-WT, and FLT-D835Y respectively. FLT3/CHK1-IN-2 has favorable oral PK properties and kinase selectivity. FLT3/CHK1-IN-2 can be used for research of acute myeloid leukemia (AML).
  • HY-119699
    PV1115
    		Inhibitor
    PV1115 is a potent and highly selective Chk2 inhibitor with an IC50 of 0.14 nM, 66000 nM, >100000 nM for Chk2, Chk1 and RSK2, respectively. PV1115 is situated within the ATP-binding pocket of Chk2.
  • HY-103366
    NSC 109555 ditosylate
    		Inhibitor
    NSC 109555 ditosylate is a potent, selective, ATP-competitive checkpoint kinase 2 (Chk2) inhibitor with an IC50 of 240 nM. NSC 109555 ditosylate can be used for the research of cancer.