chk 1

CHK1-IN-3 is an inhibitor of checkpoint kinase 1 (CHK1; IC50: 0.4 nM).

CHK-IN-1 is a dual inhibitor of CHK1 and CHK2 with antiproliferative activity.

CHK1-IN-4 hydrochloride is a potent inhibitor of checkpoint kinase 1 (chk1). CHK1-IN-4 hydrochloride potently inhibits chk1 phosphorylation in the tumor cells. CHK1-IN-4 hydrochloride has anti-tumor activity.

CHK1-IN-2 is an inhibitor of checkpoint kinase 1 (CHK1; IC50: 6 nM).

CHK1-IN-4 is a potent inhibitor of checkpoint kinase 1 (chk1) and potently inhibits chk1 phosphorylation in the tumor cells with anti-tumor activity.

Chk1-IN-5 is a highly effective inhibitor of checkpoint kinase 1 (Chk1), which hinders the phosphorylation of Chk1 and effectively suppresses tumor growth in a colon cancer xenograft model[1].

Chk1-IN-6 is a potent, selective, and orally bioavailable [CHK1] inhibitor candidate.

Compound 18, also known as FLT3/CHK-IN-1, is a dual inhibitor targeting FLT3 and CHK1, exhibiting over 1700-fold selectivity towards c-KIT and significantly diminishing hERG affinity, with an IC50 of 58.4 μM. It demonstrates efficacy in suppressing tumor growth in mouse xenotransplantation models implanted with MV-4-11 cells [1].

CHK1-IN-12 (Compound example 1-5) is a highly selective and orally active checkpoint kinase 1 (CHK1) inhibitor, demonstrating an in vitro enzyme IC50 of ≤10 nM and a cellular IC50 of ≤50 nM. This compound suppresses the phosphorylation activity of CHK1 kinase, disrupts DNA damage response pathways, and induces tumor cell cycle arrest and apoptosis. CHK1-IN-12 shows promise for cancer research applications.

CHK1-IN-11 (Compound 1) is an orally active inhibitor of checkpoint kinase 1 (CHK1). It is utilized in research focused on cancers with oncogene amplification.

FLT3/CHK1-IN-2 (Compound 30) is a dual inhibitor targeting FLT3 and CHK1, with IC50 values of 25.63 nM for CHK1, 16.39 nM for FLT3-WT, and 22.80 nM for FLT-D835Y. It displays favorable oral pharmacokinetic properties and kinase selectivity. FLT3/CHK1-IN-2 is applicable in acute myeloid leukemia (AML) research.

CHK1-IN-9 (compound 11) is an orally active CHK1 inhibitor with an IC50 of 0.55 nM. It enhances the effects of DNA-damaging agents on tumor cells and exhibits synergistic anticancer activity with Gemcitabine.

CHK1-IN-13 (Compound 38) is an inhibitor of checkpoint kinase 1 (Chk1) with an IC50 ranging from 10 to 50 nM. It exhibits antitumor activity and can be utilized in research studies focused on cancers such as breast, ovarian, and prostate cancer.

CHK1-IN-8 (example 3-2) is an inhibitor of Chk1, exhibiting an IC50 of less than 10 nM against human Chk1. It is applicable for cancer research.

CHK1-IN-14 is a free base form of a CHK1 inhibitor. It is utilized in research focused on resistance to chemotherapy and radiotherapy.

PROTACFLT3/CHK1 Degrader-1 is a PROTAC agent targeting FLT3 and CHK1, with DC50 values of 5.88 nM (FLT3) and 4.17 nM (CHK1). It inhibits the phosphorylation of downstream signaling effectors STAT5(Tyr694), AKT(Ser473), and ERK(Tyr204) of FLT3, reduces c-Myc protein levels, and maintains p53 protein expression. Additionally, PROTACFLT3/CHK1 Degrader-1 induces apoptosis in MV-4-11 cells and demonstrates significant antitumor activity in mice with MV-4-11 xenografts. This compound is applicable in acute myeloid leukemia (AML) research.

FLT3/CHK1 ligand-1 is a PROTAC target protein ligand used in the synthesis of PROTACs, such as [PROTAC FLT3/CHK1 Degrader-1]. [PROTAC FLT3/CHK1 Degrader-1] functions as a potent FLT3/CHK1 PROTAC degrader with antitumor activity.

CHK1-IN-15 (compound 9a) is an ATP-competitive inhibitor of checkpoint kinase 1 (CHK1), exhibiting a binding rate of 95% at a concentration of 1.0 µM. It also acts as a Chk1 target protein ligand of MA203 and is applicable for tumor-related research.

Compound PROTAC-2, also known as PROTAC Chk1 degrader-1, is a potent degrader of Chk1, exhibiting a DC50 of 1.33 μM. It is utilized in cancer research [1].

Prexasertib (LY2606368) is a selective checkpoint kinase 1 (CHK1) inhibitor (Ki 0.9 nM, IC50<1 nM). Prexasertib causes double-stranded DNA breaks and replication mutations, leading to apoptosis. Prexasertib has antitumor activity.

CCT241533 is an effective and selective ATP competitive inhibitor of CHK2 (Ki: 1.16 nM; IC50: 3 nM).

MBM-55S is an effective inhibitor of Nek2 with an IC50 of 1 nM. MBM-55S indecus cell cycle arrest and apoptosis thereby inhibiting the proliferation of cancer cells. MBM-55S shows antitumor activities.

Tuvusertib (M1774) is an orally available ataxia telangiectasia and Rad3-related (ATR) kinase inhibitor (Ki< 1 µΜ) with selective and potentially antitumor activity.Tuvusertib selectively inhibits ATR activity and blocks downstream phosphorylation of serine/threonine protein kinase checkpoint kinase 1 (CHK1), thereby inhibits DNA damage checkpoint activation, disrupting DNA damage repair and inducing apoptosis in tumor cells.

CCT241533 hydrochloride is an effective and selective ATP competitive inhibitor of CHK2 (Ki: 1.16 nM; IC50: 3 nM).