Chk

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.

SCH900776 is an agent targeting cell cycle checkpoint kinase 1 (Chk1) with potential radiosensitization and chemosensitization activities.

NMS-1286937 is an orally bioavailable, small-molecule Polo-like kinase 1 (PLK1) inhibitor with potential antineoplastic activity.

CHK1-IN-2 is a checkpoint kinase 1 (CHK1) inhibitor, with an IC50 of 6 nM.

RO3280 is a potent, highly selective inhibitor of Polo-like kinase 1 (PLK1) with IC50 of 3 nM.

TAK-960 is a novel, orally available, selective inhibitor of polo-like kinase 1, shows broad-spectrum preclinical antitumor activity.

PF 477736 is a selective checkpoint kinase 1 (Chk1) inhibitor (Ki values are 0.49 and 47 nM for Chk1 and Chk2 respectively).

Poloxin is a non-ATP competitive Polo-like Kinase 1 (PLK1) inhibitor that targets the polo-box domain, with an IC50 of appr 4.8 μM.

Poloxime, a hydrolysis product of poloxin, is a non-ATP-competitive Plk1 inhibitor, with moderate Plk1 inhibitory activity.

BML-277 (Chk2 Inhibitor II) is a Chk2 (checkpoint kinase 2) inhibitor.

GNE-900 is an ATP-competitive, selective, and orally bioavailable ChK1 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).

CCT245737 is a potent, selective and orally active checkpoint kinase 1 (CHK1) inhibitor. CCT245737 showed CHK1 IC50 = 1.3 nM, CHK2 IC50 = 2440 nM, G2 check point abrogation IC50 = 30 nM. Mouse F (oral)=100%.

CHK1-IN-3 is a Checkpoint Kinase 1 (CHK1) inhibitor with an IC50 of 0.4 nM.

GDC-0575 (ARRY-575, RG7741) is a potent and selective CHK1 inhibitor with an IC50 of 1.2?nM.

GDC-0575 dihydrochloride (ARRY-575 dihydrochloride) is an orally bioavailable CHK1 inhibitor, with an IC50 of 1.2 nM, and has antitumor activity.

SBE13 is a potent and selective Plk1 inhibitor, with an IC50 of 200 pM; SBE13 poorly inhibits Plk2 (IC50>66?μM) or Plk3 (IC50=875?nM).

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.

MN58b is a selective choline kinase α (CHKα) inhibitor, and results in inhibition of phosphocholine synthesis.

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.

SAR-020106 is an ATP-competitive, potent, and selective CHK1 inhibitor with an IC50 of 13.3 nM for human CHK1.

Centrinone-B (LCR-323) is a potent and highly selective PLK4 inhibitor, with a Ki of 0.59 nM.

Centrinone (LCR-263) is a selective and reversible inhibitor of polo-like kinase 4 (PLK4) with a Ki of 0.16 nM.

CHK1 inhibitor (GDC-0575 analog) is an inhibitor of CHK1.

AAPK-25 is a potent and selective Aurora/PLK dual inhibitor with anti-tumor activity, which can cause mitotic delay and arrest cells in a prometaphase, reflecting by the biomarker histone H3Ser10 phosphorylation and followed by a surge in apoptosis.

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.

SB 218078 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)

CCT244747 is a novel potent, highly selective, orally active ATP-competitive CHK1 inhibitor with potential anticancer activity,

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.

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.

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.

(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.

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-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.

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.

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.