Catalog No.
Product Name
Application
Product Information
Citations
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DYRK1A Inhibitor
Dyrk1A-IN-16 is a selective DYRK1A inhibitor that operates as an ATP-competitive antagonist with an IC50 of 53 nM. This compound exhibits strong selectivity for DYRK kinases and demonstrates nanomolar potency in biological assays. In vitro studies reveal that Dyrk1A-IN-16 effectively impairs neurosphere self-renewal, cell invasion, and EGFR stability. In vivo, it has been shown to inhibit tumor growth and extend survival, indicating its potential utility in glioblastoma research. -
EGFR/HER2/CDK9/COX-2 Inhibitor
CDK9-IN-41 is a potent inhibitor of CDK9, EGFR, HER2, and COX-2, exhibiting IC50 values of 192.81 nM, 254.03 nM, 238.81 nM, and 775 nM respectively. This compound demonstrates significant antitumor activity across various cancer cell lines, including leukemia, colon, melanoma, ovarian, and breast cancer. It serves as a valuable tool for exploring the role of these kinases in cancer biology and therapeutic applications. -
EGFR/HER2/CDK9 Inhibitor
EGFR/HER2/CDK9-IN-3 is a potent inhibitor targeting EGFR, HER2, and CDK9, exhibiting IC50 values of 191.08 nM, 132.65 nM, and 113.98 nM, respectively. This compound demonstrates significant antitumor activity, making it valuable for research in cancer therapies and signaling pathways involving these targets. Its inhibitory effects on cell proliferation in cancer models may aid in the understanding and development of targeted treatment strategies. -
EGFR/HER2/CDK9 Inhibitor
EGFR/HER2/CDK9-IN-1 is a highly active inhibitor of EGFR, HER2, and CDK9, displaying IC50 values of 90.17 nM, 131.39 nM, and 67.04 nM, respectively. This compound demonstrates significant antitumor properties, making it a valuable tool for cancer research. Its ability to target multiple kinases involved in cell proliferation and survival pathways supports investigations into therapeutic strategies for various malignancies. -
KRAS Inhibitor
KRAS G12D inhibitor 25 selectively targets the KRAS G12D mutation and HSP90α, exhibiting IC50 values of less than 0.1 μM and between 0.1-1 μM, respectively. This compound effectively inhibits the proliferation of MIA PaCa-2 and NCI-H358 cell lines, displaying EC50 values of less than 0.1 μM and between 0.1-1 μM, respectively. Additionally, KRAS G12D inhibitor 25 promotes the degradation of ERBB2 with a DC50 range of 0.1-1 μM, making it a valuable tool for cancer research focusing on KRAS-targeted therapies. -
DYRK1A Inhibitor
Dyrk1A-IN-15 is a selective, ATP-competitive inhibitor of DYRK1A with an IC50 of 19 nM. This compound demonstrates high selectivity for DYRK kinases and nanomolar potency across various kinase assays. In vitro studies reveal that Dyrk1A-IN-15 disrupts neurosphere self-renewal, inhibits cell invasion, and destabilizes EGFR. Additionally, it shows the ability to inhibit tumor growth and extend survival in vivo, indicating its potential utility in glioblastoma research. -
EGFR/CDK-2 Inhibitor
EGFR/CDK2-IN-1 is an inhibitor targeting both the epidermal growth factor receptor (EGFR) and cyclin-dependent kinase 2 (CDK2). This compound exhibits significant cytotoxicity against breast cancer MCF7 cells and liver cancer HepG2 cells, making it a valuable tool in cancer research. Its dual inhibition profile allows for exploration of synergistic effects in therapeutic strategies targeting these critical pathways in cancer proliferation and survival. -
CDK9/PARP Inhibitor
CDK9/PARP-IN-1 is a potent inhibitor of CDK9 and PARP1, demonstrating IC50 values of 118 nM and 107 nM, respectively. This dual inhibition results in significant antiproliferative effects across various cancer cell lines, making it a valuable tool for cancer research. CDK9/PARP-IN-1 is particularly relevant for studies investigating the therapeutic potential of targeting these pathways in oncology. -
PARP1/CDK12 Inhibitor
Antitumor agent-104 is a potent inhibitor of PARP1 and CDK12, targeting critical pathways in DNA damage repair in tumors. By inhibiting PARP1 enzymatic activity, it effectively reduces PAR protein levels, thus impairing the cellular mechanisms that protect tumor cells. This compound serves as a valuable tool in cancer research, especially in studies focused on understanding tumor biology and exploring novel therapeutic strategies. -
CDK-1/PARP-1 Inhibitor
UNPD139734 is a potent inhibitor of Cyclin-Dependent Kinase 1 (CDK-1) and Poly (ADP-ribose) polymerase 1 (PARP-1), forming stable complexes with both target proteins. This compound serves as a valuable lead for the structural optimization of dual-target anticancer agents, particularly in the context of breast cancer research. Its dual inhibition mechanism offers a promising avenue for investigating novel therapeutic strategies in oncology. -
Aurora-A Inhibitor
PHA-680626 is a selective inhibitor of Aurora-A kinase, disrupting its interaction with N-Myc. This compound effectively inhibits the kinase activities of both AURKA and Bcr-Abl, leading to the degradation of N-Myc. Additionally, PHA-680626 reduces phosphorylation levels of CrkL and histone H3. Its anti-proliferative and pro-apoptotic effects have been demonstrated in Imatinib-resistant chronic myeloid leukemia cell lines and primary CD34+ hematopoietic stem cells, making it a valuable tool for research in cancer therapeutics. -
CDK Inhibitor
Ryuvidine is a selective inhibitor of cyclin-dependent kinases (CDKs), specifically targeting SET domain-containing protein 8 (SETD8) with an IC50 of 0.5 µM, thereby suppressing the monomethylation of histone H4 at lysine 20 (H4K20). Additionally, Ryuvidine inhibits CDK4 with an IC50 of 6.0 µM and KDM5A, leading to the blockade of DNA synthesis. Its biological activity includes anticancer effects against various tumor types, including breast cancer, and it also demonstrates potential therapeutic benefits in arthritis research. -
CDK9/EZH2 Dual-target Inhibitor
CDK9/EZH2-IN-1 is a dual-target inhibitor designed to inhibit both CDK9 and EZH2, exhibiting IC50 values of 83.9 nM and 108.6 nM, respectively. This compound demonstrates significant biological activity by inducing apoptosis and causing DNA double-strand breaks (DSBs). It effectively inhibits the proliferation of various cancer cell lines, including MKN45, MDA-MB-453, and SW620, with IC50 values of 136.3 nM, 171.3 nM, and 315.7 nM, respectively. CDK9/EZH2-IN-1 is suitable for research applications in understanding cancer cell biology and therapeutic development. -
Nur77 Agonist
Nur77 agonist-1 is a selective agonist targeting the Nur77 receptor, promoting ferroptosis through the upregulation of Nur77 protein expression. This compound significantly elevates levels of reactive oxygen species (ROS) and lipid peroxidation while diminishing GPX4 protein expression. With a binding affinity of 13.80 μM to the ligand binding domain of Nur77, Nur77 agonist-1 demonstrates potent antiproliferative effects against various breast cancer cell lines (IC50: 2.15-3.26 μM) while exhibiting low toxicity to normal cells. It is a valuable tool for research focused on breast cancer therapies. -
CDK2/CDK5 Inhibitor
(S)-PHA533533 is an inhibitor of cyclin-dependent kinases CDK2 and CDK5, demonstrating blood-brain barrier permeability with IC50 values of 37 nM and 55 nM, respectively. This compound effectively restores UBE3A expression by downregulating UBE3A-ATS, thereby alleviating the epigenetic silencing of paternal UBE3A in mature neurons. (S)-PHA533533 is a valuable tool for research applications related to Angelman syndrome and offers insights into therapeutic strategies for this genetic disorder. -
CDK9 Autophagic Degrader
CDK9 autophagic degrader 1 is a selective autophagic degrader targeting cyclin-dependent kinase 9 (CDK9). This compound effectively degrades CDK9, leading to a significant reduction in associated Cyclin T1 levels. Demonstrating over 80% inhibition of CDK9 at a concentration of 100 nM, this reagent serves as a valuable tool for research applications focused on transcriptional regulation and cancer biology. -
G-quadruplex DNA Fluorescent Binder
N-Methylmesoporphyrin IX (NMM) is a potent fluorescent binder that targets G-quadruplex DNA, making it an effective probe for studying Aβ fibrillation. It serves as both an in situ inhibitor and an ex situ monitor of Aβ amyloidogenesis in vitro and within cellular contexts. NMM exhibits high sensitivity to G-quadruplex structures while showing negligible response to duplexes, triplexes, and single-stranded DNA. Additionally, it remains nonfluorescent in monomeric Aβ environments, producing strong fluorescence upon interaction with Aβ aggregates. -
CDK2 Inhibitor
CDK2-IN-12 is a selective inhibitor of cyclin-dependent kinase 2 (CDK2), exhibiting an IC50 of 11.6 μM. This compound also inhibits human carbonic anhydrase isoforms I, II, IX, and XII, with respective KI values of 3534, 638.4, 44.3, and 48.8 nM. CDK2-IN-12 demonstrates notable anticancer activity, making it a valuable tool for research in cancer biology and therapeutic development. -
CA/CDK2 Inhibitor
Carbonic anhydrase inhibitor 14 is a potent inhibitor of carbonic anhydrases (CAs), exhibiting Ki values of 1203 nM for hCA I, 99.7 nM for hCA II, 9.4 nM for hCA IX, and 27.7 nM for hCA XII. Additionally, it effectively inhibits cyclin-dependent kinase 2 (CDK2) with an IC50 of 20.3 μM. This compound demonstrates significant antitumor activity, making it a valuable tool for cancer research and therapeutic applications targeting both CA and CDK2 pathways. -
CDK2 Inhibitor
CDK2-IN-11 is a selective inhibitor of cyclin-dependent kinase 2 (CDK2), demonstrating an IC50 of 6.4 μM. With inhibitory constant (KI) values of 23.4 nM, 56.3 nM, and 44.3 nM for human carbonic anhydrases II, IX, and XII, respectively, it exhibits significant enzyme inhibition. CDK2-IN-11 is primarily utilized in anticancer research, making it a valuable tool for studies targeting cell cycle regulation and tumor progression. -
Chk1 Inhibitor
Isogranulatimide is a selective inhibitor of checkpoint kinase 1 (Chk1) with an IC50 value of 0.1 μM. It effectively inhibits the G2/M checkpoint, demonstrating the ability to impede the growth of p53-mutant tumor cells. This compound shows promise for research applications focused on tumors that are linked to DNA damage response mechanisms. -
CHK1 Inhibitor
BEN-28010 is a selective CHK1 inhibitor that demonstrates potent inhibitory activity with an IC50 of 4.0 nM. This compound is orally active and effectively penetrates the blood-brain barrier, making it a valuable tool in cancer research. BEN-28010 acts as a radiosensitizer and exhibits antitumor efficacy in glioblastoma models, providing a promising avenue for investigation into glioblastoma therapies. -
Chk1/Wee1 Inhibitor
PD 407824 is a selective inhibitor of checkpoint kinase Chk1 and WEE1, exhibiting IC50 values of 47 nM and 97 nM, respectively. This compound enhances the sensitivity of cells to low concentrations of BMP4, positioning it as a valuable tool for studying BMP signaling pathways and cellular responses to DNA damage. PD 407824 is applicable in cancer research and therapeutic development targeting cell cycle regulation and stress response mechanisms. -
CHK1 Inhibitor
LY2880070 is a potent, orally active CHK1 inhibitor with an IC50 of less than 1 nM. This reagent demonstrates significant biological activity in cancer cell lines, making it a valuable tool for investigating cancer therapies, particularly in combination with DNA-damaging agents. Its application in preclinical research facilitates the exploration of CHK1's role in DNA repair and cellular response to genotoxic stress. -
Chk2 Inhibitor
PV-1019 (NSC 744039) is a selective inhibitor of Chk2 with an IC50 value of 24 nM. This compound effectively inhibits Chk2 autophosphorylation induced by Topotecan, demonstrating its potential to modulate cellular responses to DNA damage. PV-1019 is valuable for research applications related to cancer biology and therapeutic strategies targeting DNA damage response mechanisms. -
ChK1 Inhibitor
GDC-0425 is a potent, oral small molecule inhibitor targeting check-point kinase 1 (ChK1). This selective inhibitor demonstrates significant activity in disrupting ChK1-mediated signaling pathways, making it valuable for research into various malignancies. Its application in cancer studies may enhance the understanding of tumor response to DNA damage and inform therapeutic strategies. -
Chk1 Inhibitor
Chk1-IN-5 is a potent inhibitor of checkpoint kinase 1 (Chk1), effectively blocking its phosphorylation activity. This compound demonstrates significant antitumor efficacy by inhibiting tumor growth in colon cancer xenograft models. Chk1-IN-5 is valuable for research applications focusing on cell cycle regulation and cancer therapeutics. -
Chk Inhibitor
AZD-7762 hydrochloride is a potent ATP-competitive inhibitor of checkpoint kinases, specifically demonstrating an IC50 of 5 nM for Chk1. This compound is primarily utilized in research focused on cell cycle regulation and DNA damage response mechanisms. Its ability to inhibit Chk1 makes it valuable for investigating therapeutic strategies in cancer treatment and enhancing the efficacy of DNA-damaging agents. -
CHK1 Inhibitor
CHK1-IN-7 is a selective inhibitor of checkpoint kinase 1 (CHK1), targeting key signaling pathways involved in cell cycle regulation. This compound has demonstrated the ability to enhance the antiproliferative effects of Gemcitabine in both prostate and breast cancer cell lines, indicating its potential utility in combination therapies. CHK1-IN-7 is suitable for research applications focusing on cancer biology, particularly in understanding the mechanisms of resistance to chemotherapy and improving therapeutic efficacy. -
Chk1 Inhibitor
Chk1-IN-6 is a selective checkpoint kinase 1 (Chk1) inhibitor, exhibiting an IC50 of 16.1 nM. It demonstrates notable antiproliferative activity against MV-4-11 cells and provides effective therapeutic responses in MV-4-11 xenograft mouse models. Additionally, Chk1-IN-6 has shown a synergistic anticancer effect in combination with Gemcitabine. This compound is valuable for research focused on acute myeloid leukemia and colorectal adenocarcinoma. -
CHK1 Inhibitor
MU380 is a selective CHK1 inhibitor that targets the checkpoint kinase 1 (CHK1) pathway. It demonstrates potent pro-apoptotic effects, leading to the induction of apoptosis in cancer cells. This compound is primarily utilized in cancer research to explore mechanisms of tumorigenesis and to evaluate potential therapeutic strategies aimed at enhancing the efficacy of existing treatment modalities. -
Chk1 PROTAC Degrader
PROTAC Chk1 degrader-1 is a selective Chk1-targeting PROTAC that facilitates the recruitment of the Cereblon E3 ligase to promote ubiquitination and subsequent proteasomal degradation of Chk1. This compound effectively induces Chk1 degradation in malignant melanoma cells, demonstrating a robust biological activity without exhibiting a hook effect. PROTAC Chk1 degrader-1 is suitable for research applications focused on understanding the role of Chk1 in malignant melanoma and exploring targeted degradation strategies in cancer therapy. -
Chk2 Inhibitor
VRX0466617 is a selective, ATP-competitive inhibitor of Chk2 with an IC50 of 120 nM and a Ki of 11 nM. It exhibits specificity by not inhibiting Chk1 activity. This compound is valuable for research focused on cancer mechanisms and the modulation of DNA damage repair pathways. -
Chk1/Chk2 Inhibitor
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. -
Checkpoint Kinase (Chk) Inhibitor
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. -
Chk2 Inhibitor
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. -
Chk1 Inhibitor
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. -
Chk2 Inhibitor
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. -
CHK1 Inhibitor
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. -
CHK1 Inhibitor
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. -
Chk Kinase Inhibitor
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. -
Chk2 Inhibitor
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. -
Chk2 Inhibitor
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. -
Chk1 Inhibitor
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. -
CHK1/2 Substrate
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. -
CHK2 Inhibitor
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. -
CHK1 Inhibitor
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. -
CHK1 Inhibitor
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. -
Dual Wee1/Chk1 Inhibitor
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. -
Checkpoint Kinase (Chk) Inhibitor
(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.
