Catalog No.
Product Name
Application
Product Information
Citations
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Chk1 Inhibitor
CHK1-IN-8 is a selective Chk1 inhibitor with an IC50 value of less than 10 nM for human Chk1. This compound is valuable for investigating the role of Chk1 in cell cycle regulation and DNA damage response mechanisms in cancer research. Its potent inhibition of Chk1 makes it a useful tool for exploring therapeutic strategies in cancer treatment. -
Chk2 Inhibitor
PV1162 is a selective Chk2 inhibitor that functions by preventing ATP binding to Chk2, specifically targeting the gatekeeper-dependent hydrophobic pocket situated behind the ATP-binding site. With an IC50 of 0.29 nM, PV1162 effectively inhibits the phosphorylation activity of Chk2. This compound demonstrates significant potential for research applications in cancer therapy, particularly in the study of checkpoint regulation and tumor progression. -
Checkpoint Kinase (Chk) Inhibitor
CHK-IN-1 is a selective inhibitor of checkpoint kinases CHK1 and CHK2, which play crucial roles in the DNA damage response and cell cycle regulation. This compound exhibits anti-proliferative activity, making it a valuable tool for cancer research and therapeutic studies targeting tumor cell growth and survival. Its ability to regulate cellular checkpoint pathways provides a basis for exploring its efficacy in combination therapies and enhancing the understanding of cancer cell biology. -
CHK1 Inhibitor
SCH900776 is an agent targeting cell cycle checkpoint kinase 1 (Chk1) with potential radiosensitization and chemosensitization activities. -
PLK inhibitor
NMS-1286937 is an orally bioavailable, small-molecule Polo-like kinase 1 (PLK1) inhibitor with potential antineoplastic activity. -
PLK inhibitor
SBE 13 HCl is a selective inhibitor of PLK1 (IC50 values are 200 pM, 875 nM and 66 μM for PLK1, PLK3 and PLK2 respectively). -
Chk1 inhibitor
GDC-0575 (ARRY-575, RG7741) is a potent and selective CHK1 inhibitor with an IC50 of 1.2?nM. -
CHK1 inhibitor
GDC-0575 dihydrochloride (ARRY-575 dihydrochloride) is an orally bioavailable CHK1 inhibitor, with an IC50 of 1.2 nM, and has antitumor activity. -
PLK1 inhibitor
TAK-960 hydrochloride is an orally available, selective inhibitor of polo-like kinase 1 (PLK1), with an IC50 of 0.8 nM at 10 μM ATP; TAK-960 hydrochloride also shows inhibitory activities against PLK2 and PLK3, with IC50s of 16.9 and 50.2 nM, respectively. -
ATP-competitive CHK1 inhibitor
Prexasertib (LY2606368) is an ATP-competitive CHK1 inhibitor with a Ki value of 0.9 nmol/L. For CHK2 and RSK, its IC50 values are 8 nM and 9 nM respectively in cell-free assay. -
CHK1 inhibitor
SAR-020106 is an ATP-competitive, potent, and selective CHK1 inhibitor with an IC50 of 13.3 nM for human CHK1. -
PLK4 inhibitor
Centrinone-B (LCR-323) is a potent and highly selective PLK4 inhibitor, with a Ki of 0.59 nM. -
PLK4 inhibitor
Centrinone (LCR-263) is a selective and reversible inhibitor of polo-like kinase 4 (PLK4) with a Ki of 0.16 nM. -
Chk2 inhibitor
CCT241533 Hcl is a potent serine/threonine checkpoint kinase (Chk2) inhibitor with IC50 of 3 nM; shows minimal cross-reactivity against a panel of kinases at 1 uM. -
CHK1 Inhibitor
Prexasertib dimesylate is a selective checkpoint kinase 1 (CHK1) inhibitor that functions as an ATP-competitive agent. With a Ki of 0.9 nM and an IC50 of less than 1 nM, it effectively inhibits CHK2 and RSK1, exhibiting IC50 values of 8 nM and 9 nM, respectively. This compound induces double-stranded DNA breaks and replication catastrophe, leading to apoptosis. Prexasertib dimesylate demonstrates significant anti-tumor activity, making it a valuable tool for cancer research and therapeutic development. -
CHKα Inhibitor
ICL-CCIC-0019 is a potent inhibitor of choline kinase α (CHKα), a key enzyme involved in phosphatidylcholine synthesis and cellular signaling. This compound has been shown to induce a G1 phase cell cycle arrest and promote endoplasmic reticulum stress-mediated apoptosis in various cancer cell lines. ICL-CCIC-0019 is valuable for research applications focused on cancer biology, specifically in studies exploring cell cycle regulation and mechanisms of apoptosis in tumor cells. -
CK1/CHK1 Inhibitor
MRT00033659 is a selective inhibitor targeting casein kinase 1 (CK1) and checkpoint kinase 1 (CHK1), with IC50 values of 0.9 μM and 0.23 μM, respectively. As a pyrazolo-pyridine analogue, MRT00033659 activates the p53 signaling pathway and causes destabilization of E2F-1. This compound is valuable for research investigating cell cycle regulation, DNA damage response, and therapeutic strategies in cancer biology. -
Chk2 Inhibitor
(E/Z)-Chk2-IN-1 is a potent and selective inhibitor of the cell cycle kinase Chk2, with an IC50 of 8 nM. This compound demonstrates minimal inhibitory activity against other kinases, including CK1δ, MEK1, and PKCα/βⅡ, with IC50 values greater than 89 nM. (E/Z)-Chk2-IN-1 is suitable for research applications in cancer biology, particularly in elucidating the role of Chk2 in cell cycle regulation and tumorigenesis. -
Dual FLT3/CHK1 Inhibitor
FLT3/CHK1-IN-1 is a dual inhibitor targeting both FLT3 and CHK1, demonstrating significant selectivity for c-KIT over other kinases. With an IC50 value of 58.4 μM, it shows reduced affinity for the hERG channel, minimizing potential cardiac side effects. FLT3/CHK1-IN-1 has exhibited efficacy in inhibiting tumor growth in mouse xenotransplantation models with MV-4-11 cells, making it a valuable tool for cancer research and therapeutic development. -
CHK1 Inhibitor
CHK1-IN-12 is a potent and selective checkpoint kinase 1 (CHK1) inhibitor that exerts its effects by significantly reducing CHK1 phosphorylation activity, thereby disrupting the DNA damage response pathway. With an in vitro enzyme IC50 of up to 10 nM and a cellular IC50 of 50 nM, CHK1-IN-12 effectively induces cell cycle arrest and apoptosis in tumor cells. This compound holds potential for cancer research, particularly in studies focused on cell cycle regulation and DNA repair mechanisms. -
CHK1 Inhibitor
Prexasertib lactate is a selective ATP-competitive inhibitor of checkpoint kinase 1 (CHK1), with a Ki value of 0.9 nM and an IC50 of less than 1 nM. It also inhibits CHK2 and RSK1 with IC50 values of 8 nM and 9 nM, respectively. By inducing double-stranded DNA breaks and leading to replication catastrophe, Prexasertib lactate promotes apoptosis in cancer cells. Its potent anti-tumor efficacy makes it a valuable tool for cancer research and therapeutic development. -
Chk1 Inhibitor
Graviquinone is a selective Chk1 inhibitor that demonstrates potent cytotoxic effects across multiple cancer cell lines. This compound is particularly notable for its ability to circumvent ABCB1-mediated multidrug resistance while selectively inducing DNA damage in cancer cells. Additionally, Graviquinone enhances its cytotoxic potential by elevating reactive oxygen species (ROS) levels, making it a valuable tool for studying mechanisms of cancer treatment and DNA damage response. Its unique properties position Graviquinone as an effective reagent for cancer research applications.
