Chk

Cat. No.

A40224

CAS No.

1174664-88-0

VER-00158411

VER-00158411 is a potent inhibitor of checkpoint kinase 1 (CHK1) and CHK2, exhibiting IC50 values of 4.4 nM and 4.5 nM, respectively. This compound is a valuable tool for studying cell cycle regulation and DNA damage response mechanisms. Its inhibitory effects on CHK1 and CHK2 make it suitable for research applications in cancer biology, particularly in combination therapies targeting replication stress in tumor cells.

Cat. No.

A40225

CAS No.

2120398-41-4

CHK1-IN-4

CHK1-IN-4 is a selective inhibitor of checkpoint kinase 1 (Chk1), effectively blocking Chk1 phosphorylation in tumor cells. This compound demonstrates significant anti-tumor activity, making it a valuable tool for cancer research. Its ability to disrupt cell cycle regulation positions CHK1-IN-4 as a potential candidate for investigating therapeutic strategies in oncology.

Cat. No.

A40226

CAS No.

1093793-10-2

PV1115

PV1115 is a highly selective Chk2 inhibitor with a low IC50 of 0.14 nM, demonstrating significant potency against Chk2 while exhibiting much weaker activity against Chk1 and RSK2 (IC50s of 66000 nM and >100000 nM, respectively). This compound operates by binding within the ATP-binding pocket of Chk2, making it an invaluable tool for research involving DNA damage response and cancer therapeutics. PV1115 is suitable for studies investigating Chk2's role in cell cycle regulation and its implications in tumor biology.

Cat. No.

A40227

CAS No.

622856-21-7

PD-321852

PD-321852 is a selective Chk1 inhibitor with an IC50 of 5 nM. It effectively interferes with checkpoint kinase 1 activity, promoting cell cycle arrest and apoptosis in cancerous cells. This reagent is valuable for anti-cancer research, particularly in studies exploring the modulation of DNA damage response and therapeutic susceptibility in tumor cells.

Cat. No.

A40228

CAS No.

2984543-29-3

Chk2-IN-2

Chk2-IN-2 is a selective inhibitor of CHK2, a key regulator in the DNA damage response pathway. This compound exhibits potent anticancer activity by hindering cell cycle progression in response to DNA damage. It is primarily utilized in research applications focused on cancer cell biology and the development of targeted therapies for tumors with defective DNA repair mechanisms.

Cat. No.

A40229

CAS No.

2309309-69-9

MCL1020

MCL1020 is a potent CHK1 inhibitor, characterized by an IC50 of 1.61 μM. This compound effectively occupies the ATP binding pocket through interactions with multiple sites on the CHK1 kinase. MCL1020 is useful for investigating mechanisms in hematologic malignancies, facilitating research into potential therapeutic strategies targeting this protein.

Cat. No.

A40231

CAS No.

3017958-71-0

CHK1-IN-11

CHK1-IN-11 is a selective checkpoint kinase 1 (CHK1) inhibitor that exhibits oral bioactivity. This compound demonstrates significant potential in targeting cancers characterized by oncogene amplification. CHK1-IN-11 may be employed in research to explore the mechanisms of tumor cell proliferation and response to therapeutic agents in cancer models.

Cat. No.

A40232

CAS No.

1351804-17-5

CBP501 Affinity Peptide

CBP501 Affinity Peptide is a Chk kinase inhibitor that effectively disrupts G2 cell cycle arrest triggered by DNA-damaging agents. This reagent is valuable for cancer research, enabling studies on cell cycle regulation and therapeutic responses to genotoxic stress. Its application can facilitate the investigation of DNA damage repair pathways and their implications in oncogenesis.

Cat. No.

A40233

CAS No.

66748-43-4

NSC 109555 ditosylate

NSC 109555 ditosylate is a selective, ATP-competitive inhibitor of checkpoint kinase 2 (Chk2) with an IC50 of 240 nM. This compound is primarily utilized in cancer research to investigate mechanisms of cell cycle regulation and DNA damage response. Its specificity towards Chk2 makes it valuable in studying potential therapeutic strategies for cancer treatment.

Cat. No.

A40234

CAS No.

724708-21-8

Chk2-IN-1

Synonyms: Hymenialdisine analogue-1

Chk2-IN-1 is a selective inhibitor of checkpoint kinase 2 (Chk2), demonstrating an IC50 of 13.5 nM for Chk2 and 220.4 nM for Chk1. This compound effectively enhances ATM-dependent Chk2-mediated radioprotection, making it a valuable tool for studying DNA damage response mechanisms. Chk2-IN-1 is applicable in cancer research, particularly in investigations of cell cycle regulation and therapeutic resistance.

Cat. No.

A40235

CAS No.

1196504-54-7

GDC0575 hydrochloride

Synonyms: ARRY-575 hydrochloride; RG7741 hydrochloride

GDC0575 hydrochloride is a highly selective and orally active inhibitor of Chk1, with an IC50 of 1.2 nM. This compound exhibits significant activity in disrupting cell cycle regulation and DNA damage response pathways. GDC0575 is primarily utilized in research related to colitis-associated cancer (CAC) and provides a valuable tool for studying the mechanisms underlying colitis and its implications in oncogenesis.

Cat. No.

A40236

CAS No.

289652-77-3

Chktide

Chktide is a synthetic peptide substrate specific for the kinases CHK1 and CHK2. This substrate plays a crucial role in the investigation of DNA damage response pathways by enabling the assessment of kinase activity in biochemical assays. Chktide is widely utilized in research applications focused on cancer biology and cellular stress responses, facilitating the study of cell cycle regulation and checkpoint signaling.

Cat. No.

A40237

CAS No.

1962925-28-5

CCT241533 dihydrochloride

CCT241533 dihydrochloride is a highly selective ATP-competitive inhibitor of CHK2, exhibiting an IC50 of 3 nM and a Ki of 1.16 nM. This compound has significant potential in cancer research due to its ability to modulate DNA damage responses and cell cycle regulation. It is particularly valuable for studies investigating the role of CHK2 in tumor biology and therapeutic sensitivity.

Cat. No.

A40238

CAS No.

2120398-52-7

CHK1-IN-13

CHK1-IN-13 is a selective checkpoint kinase 1 (CHK1) inhibitor with an IC50 range of 10-50 nM. This compound exhibits significant anticancer activity, making it a valuable tool for research focused on various cancers, including breast, ovarian, and prostate cancers. Its role in modulating the cell cycle checkpoint pathways provides insights into the mechanisms of cancer cell proliferation and therapeutic resistance.

Cat. No.

A40239

CAS No.

1803106-00-4

CHK1-IN-14

CHK1-IN-14 is a potent CHK1 inhibitor that selectively disrupts checkpoint kinase 1 activity. This compound is primarily utilized in research focused on understanding mechanisms of resistance to chemotherapy and radiotherapy in cancer cells. Its application provides valuable insights into potential therapeutic strategies aimed at improving the efficacy of cancer treatments.

Cat. No.

A40240

CAS No.

622855-60-1

DB07006

DB07006 is a potent dual inhibitor targeting Wee1 and Chk1 kinases. It exhibits ATP-competitive inhibition, with IC50 values of 0.030 μM for Wee1 and 0.018 μM for Chk1. This compound effectively abrogates the G2/M checkpoint when used in conjunction with DNA-damaging agents in cellular models, making it a valuable tool for cancer research and therapeutic strategies aimed at enhancing the efficacy of DNA-damage response inhibitors.

Cat. No.

A40241

CAS No.

1489389-23-2

(S)-CCT245737

Synonyms: (S)-SRA737

(S)-CCT245737 is a selective inhibitor of checkpoint kinase 1 (CHK1), primarily targeting cell cycle regulation. This compound exhibits potent inhibitory activity, making it a valuable tool for studying the role of CHK1 in DNA damage response and replication stress. Its applications extend to cancer research, particularly in investigating therapeutic strategies for tumors with defective DNA repair mechanisms.

Cat. No.

A40242

CAS No.

631864-00-1

XL-844

Synonyms: EXEL-9844

XL-844 is an inhibitor of checkpoint kinases Chk1 and Chk2, leading to the induction of apoptosis in tumor cells by disrupting cell cycle arrest. Additionally, XL-844 demonstrates inhibitory effects on vascular endothelial growth factor receptors VEGFR1 and VEGFR3. This compound is primarily applied in anti-cancer research to explore its potential in enhancing therapeutic efficacy against various malignancies.

Cat. No.

A40243

CAS No.

2871057-47-3

CHK1-IN-8

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.

Cat. No.

A40244

CAS No.

1093793-11-3

PV1162

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.

Cat. No.

A40245

CAS No.

1278405-51-8

CHK-IN-1

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.