Catalog No.
Product Name
Application
Product Information
Citations
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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. -
PLK1 PBD Inhibitor
MCC1019 is a selective inhibitor of the Polo-like kinase 1 (PLK1) phosphopeptide-binding domain (PBD), exhibiting an IC50 of 16.4 μmol/L. This compound effectively inactivates the AKT signaling pathway in cancer cells, leading to the induction of apoptosis, necroptosis, and autophagy. MCC1019 demonstrates significant anticancer activity against lung and prostate cancer, making it a valuable tool for cancer research and therapeutic studies. -
CDK6/9 Inhibitor
CDK6/9-IN-2 is a potent dual inhibitor of cyclin-dependent kinases CDK6 and CDK9, with reported IC50 values of 15 nM and 22 nM, respectively. This compound exhibits selectivity for CDK2, CDK8, and CDK11. CDK6/9-IN-2 effectively inhibits the proliferation of HaCaT cells stimulated by IFN-γ and TNF-α, while also suppressing the STAT3 signaling pathway and the expression of inflammatory factors. Its ability to alleviate psoriatic dermatitis makes CDK6/9-IN-2 valuable for research in psoriasis and related inflammatory conditions. -
KRAS Inhibitor
BBO-11818 is a highly selective non-covalent pan-KRAS inhibitor, targeting the Switch-II/Helix 3 pocket with an IC50 range of 28-120 nM. This compound effectively disrupts the KRAS:RAF1 interaction, leading to inhibition of the MAPK signaling pathway, resulting in significant anti-tumor effects. It demonstrates the ability to not only inhibit cell proliferation and induce apoptosis but also promote tumor regression in xenograft models. BBO-11818 is particularly valuable in research focused on KRAS mutation-related malignancies, including pancreatic cancer, non-small cell lung cancer, and colorectal cancer, and exhibits synergistic effects when used in combination with other therapeutic agents. -
CDK Inhibitor
AS2863619 free base is a selective inhibitor of cyclin-dependent kinases 8 and 19 (CDK8 and CDK19), demonstrating IC50 values of 0.61 nM and 4.28 nM, respectively. This compound drives the conversion of antigen-specific effector and memory T cells into Foxp3+ regulatory T (Treg) cells, thereby offering potential therapeutic approaches for various immunological conditions. The inhibition of CDK8/19 by AS2863619 enhances STAT5 activation, leading to the upregulation of the Foxp3 gene and promoting Treg cell development. -
CDK3 Inhibitor
Vanicoside B is a potent inhibitor of cyclin-dependent kinase 8 (CDK8), derived from the herb Persicaria dissitiflora. This compound demonstrates significant anti-tumor activity by disrupting CDK8-mediated signaling pathways and reducing the levels of proteins associated with epithelial-mesenchymal transition. As a result, Vanicoside B induces cell cycle arrest and apoptosis, making it a valuable reagent for cancer research and therapeutic investigations targeting CDK8 pathways. -
ROCK2 Inhibitor
ROCK2-IN-12 is a selective ROCK2 inhibitor, demonstrating an IC50 of 7.0 nM for ROCK2 relative to ROCK1. This compound exhibits potent antifibrotic effects by modulating the TGF-β/Smad and ROCK2/STAT3 signaling pathways, effectively reducing collagen deposition and reversing fibrosis in Bleomycin-induced pulmonary fibrosis mouse models. ROCK2-IN-12 is suitable for investigating lung diseases, particularly pulmonary fibrosis. -
ROCK2 Inhibitor
ROCK2-IN-7 is a selective inhibitor of the Rho-associated protein kinase 2 (ROCK2). It effectively disrupts ROCK2/pSTAT3 signaling pathways, leading to decreased systemic immune activation and reduced inflammation. This compound is particularly valuable in studies related to autoimmune conditions, such as psoriasis, as it provides insights into the modulation of immune responses and inflammatory processes. -
CDK8/19 Inhibitor
CDK8/19-IN-2 is a potent and orally active inhibitor of cyclin-dependent kinases 8 and 19, exhibiting IC50 values of 2.08 nM and 2.49 nM, respectively. This compound is crucial for research focusing on acute myeloid leukemia (AML), breast cancer, and lymphoma, where inhibition of CDK8 and CDK19 can influence tumor proliferation and survival. Its selectivity and efficacy make it a valuable tool in studying the role of these kinases in various oncogenic pathways. -
PLK Inhibitor
Poloxipan is a pan-specific inhibitor targeting polo-like kinases (PLKs), specifically interfering with the Polo-box domain at the C-terminus. It demonstrates IC50 values of 3.2 μM, 1.7 μM, and 3.0 μM against PLK-1, PLK-2, and PLK-3, respectively. Additionally, Poloxipan inhibits various phospho-tyrosine binding domains, including the forkhead-associated domain of CHK-2 and the WW domain of peptidyl-prolyl cis/trans isomerase (PIN1). This compound is valuable for applications in cancer research, particularly in studies involving PLK pathways and associated cellular processes. -
CDK8/19 Inhibitor
CDK8-IN-16 is a potent dual inhibitor of cyclin-dependent kinases 8 and 19, demonstrating IC50 values of 5.1 nM and 5.6 nM, respectively. This compound effectively inhibits phospho-STAT1SER727 with an IC50 of 17.9 nM in SW620 cells and modulates the WNT signaling pathway with an IC50 of 7.2 nM in 7dF3 cells. CDK8-IN-16 exhibits favorable pharmacokinetic properties, including an oral bioavailability of 57% in rat models, making it a valuable tool for research in cancer biology and therapeutic development. -
KRAS G12D Inhibitor
KRAS G12D-IN-30 is a selective inhibitor of the KRAS G12D mutant, targeting the KRAS oncogene involved in various cancers. By inhibiting the activation of the downstream MAPK signaling cascade, specifically the Raf1-MEK-ERK pathway, this compound provides valuable insights into oncogenic signaling mechanisms. KRAS G12D-IN-30 is suitable for cancer research applications, particularly in studies focusing on KRAS-driven tumor biology and therapeutic strategies. -
KRAS Inhibitor
KRAS inhibitor-27 is a specific inhibitor targeting KRAS mutations, particularly effective against KRAS G12D and G12V variants. It demonstrates potent biological activity with IC50 values of 378 nM and 0.6 nM in AsPC-1 and SW620 cell lines, respectively, while showing a markedly reduced effect on wildtype KRAS HT-29 cells (IC50 3230 nM). This compound effectively inhibits ERK phosphorylation and reduces DUSP4 expression, thereby disrupting the MAPK signaling pathway. KRAS inhibitor-27 is valuable for research applications focusing on cancer biology and therapeutic strategies against KRAS-driven tumors. -
G-quadruplex Ligand
SYUIQ-5 is a G-quadruplex ligand that specifically stabilizes G-quadruplex structures, thereby inducing cellular senescence. This compound inhibits the activity of the c-myc gene promoter, which is critical in tumorigenesis. Additionally, SYUIQ-5 promotes autophagy in cancer cells by causing telomere damage through the delocalization of TRF2 from telomeric regions, making it a valuable tool for investigating pathways related to cancer and aging. -
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. -
KRASG12C Inhibitor
KRASG12C IN-19 is a selective inhibitor that targets the KRASG12C mutation. It demonstrates potent antiproliferative effects against KRASG12C-mutant non-small cell lung cancer (NSCLC) cell line H358, with an IC50 of 7.6 nM, and effectively inhibits downstream ERK phosphorylation (IC50 = 24.06 nM). KRASG12C IN-19 shows minimal inhibitory activity against KRASG12V and KRASG12D mutants, with IC50 values exceeding 10,000 nM. This reagent forms a covalent bond with KRASG12V-GDP and provides a robust tool for research on KRASG12C-driven malignancies, including NSCLC, pancreatic cancer, and colorectal cancer. -
c-Myc Inhibitor
KSI-3716 is a potent c-Myc inhibitor that disrupts the binding of c-Myc to MAX, preventing the transcription of target genes. This compound serves as an effective agent in intravesical chemotherapy for bladder cancer, demonstrating significant antitumor activity. Its ability to modulate c-Myc signaling makes it a valuable tool for research into cancer biology and potential therapeutic interventions. -
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. -
Telomeric G-quadruplex Ligand
Telomeric G4s Ligand 2 is a selective ligand that targets telomeric G-quadruplex (G4) structures, exhibiting an IC50 value of 0.4 μM. This compound binds to dimeric telomeric G4 and inhibits the functions of DHX36 and BLM helicases. It activates both cGAS-STING and TERRA-ZBP1 pathways, leading to induction of autophagy and G2/M cell cycle arrest, demonstrating significant antiproliferative effects across various cancer cell lines. This reagent is useful for investigating mechanisms underlying colorectal cancer. -
PROTAC CDK9 Degrader
PROTAC CDK9 degrader-12 is a selective CDK9 degrader that utilizes the E3 ubiquitin ligase-mediated proteasomal pathway for the degradation of CDK9, exhibiting a DC50 of 23 nM. This compound effectively inhibits CDK9-mediated transcriptional elongation of HIV-1, subsequently reducing HIV-1 RNA synthesis. PROTAC CDK9 degrader-12 is designed for research applications focused on HIV-1 infection and the study of transcriptional regulation. -
CDK Degrader
TR-213 is a potent molecular glue degrader that specifically targets Cyclin K (CDK). At a concentration of 1 μM, TR-213 demonstrates a significant inhibition of CDK12 and Cyclin levels, leading to decreases of 91% and 56%, respectively. This compound effectively inhibits RNA polymerase II activity and modulates alternative polyadenylation (APA), making it a valuable tool for cancer research and investigations into CDK-related pathways. -
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.
