Catalog No.
Product Name
Application
Product Information
Citations
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PARP1/2/CDK12 Inhibitor
PARP-1/2-IN-2 is a potent inhibitor of PARP1, PARP2, and CDK12, exhibiting IC50 values of 34 nM, 30 nM, and 285 nM, respectively. This compound disrupts DNA damage repair mechanisms, leading to induced cell cycle arrest and apoptosis. Notable for its efficacy in targeted therapy, PARP-1/2-IN-2 effectively inhibits the growth of triple-negative breast cancer (TNBC) cells and demonstrates significant antitumor activity in TNBC xenograft models. This makes it a valuable tool for research in cancer biology and therapeutic development. -
Aurora-A kinase Inhibitor
LY3295668 erbumine is a potent and selective inhibitor of Aurora-A kinase, exhibiting a Ki value of 0.8 nM for AurA while demonstrating significantly lower binding affinity for AurB at 1038 nM. This compound effectively inhibits the autophosphorylation of Aurora-A, leading to mitotic arrest and apoptosis without promoting polyploidy associated with AurB inhibition. LY3295668 erbumine is valuable for research into small cell lung cancer and other conditions involving dysregulation of Aurora kinases. -
CDK1 Inhibitor
Avotaciclib sulfate is an orally bioavailable inhibitor of cyclin-dependent kinase 1 (CDK1). It effectively inhibits cell proliferation and induces apoptosis in various cancer cell lines. This compound is particularly useful for research applications focused on oncology, including the study of pancreatic and lung cancer. -
c-Myc G4 Inhibitor
c-Myc inhibitor 16 iodide is a selective inhibitor of the c-Myc G-quadruplex, effectively targeting the c-Myc gene's transcription and translation processes. It disrupts the tumor cell cycle by arresting growth in the G0/G1 phase and activates the mitochondrial apoptosis pathway, leading to early apoptosis in cancer cells. This compound has significant potential in research applications related to breast cancer. -
Aurora B Inhibitor
HOI-07 is a selective inhibitor of Aurora B kinase that interferes with the phosphorylation of histone H3 at Ser10 in lung cancer cells. This compound induces cell-cycle arrest and apoptosis, demonstrating significant antitumor activity. HOI-07 effectively suppresses tumor growth in xenograft models, including A549, 143B, and KHOS, making it a valuable tool for cancer research and therapeutic investigation. -
c-Myc Inhibitor
EP12 is a selective c-Myc inhibitor that stabilizes c-Myc G-quadruplexes. This compound induces apoptosis and causes DNA damage in multiple myeloma cells, effectively inhibiting their growth. Additionally, EP12 disrupts the nuclear translocation of P65/P50 by interfering with the NF-κB signaling pathway, highlighting its potential in cancer research and therapeutic applications. -
PKMYT1 Inhibitor
XH-30 is a potent and selective inhibitor of PKMYT1, exhibiting an IC50 of 4.1 nM. This compound effectively suppresses the proliferation of P53-mutated triple-negative breast cancer (TNBC) cells by promoting G2/M phase release, inducing DNA damage, and triggering apoptosis. Additionally, XH-30 demonstrates significant antitumor effects in MDA-MB-231 mouse models, making it a valuable tool for research focused on P53-mutated TNBC. -
CHK1 Inhibitor
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. -
CDK12/CDK13 Inhibitor
ZSQ836 is an orally active dual covalent inhibitor of CDK12 and CDK13, demonstrating an EC50 value of 32 nM for CDK12 inhibition. This compound has been shown to induce apoptosis and exhibits significant anticancer efficacy in vivo. ZSQ836 is a valuable tool for investigating the mechanisms and treatment strategies associated with ovarian cancer. -
PLK1 Inhibitor
PLK1-IN-16 is a potent and selective inhibitor of polo-like kinase 1 (PLK1) with an IC50 value of 0.25 nM. This compound is primarily utilized in cancer research due to its ability to induce G2 phase cell cycle arrest and promote apoptosis, displaying significant antiproliferative activity against various tumor cell lines. Additionally, PLK1-IN-16 has been shown to exhibit stability under simulated gastric acid conditions and presents manageable CYP 450 inhibition. Its applications extend to the study of triple-negative breast cancer (TNBC), breast cancer, and leukemia. -
PLK4 Inhibitor
Ocifisertib hydrochloride is a potent inhibitor of Polo-like kinase 4 (PLK4) with a Ki value of 0.26 nM and an IC50 of 2.8 nM. This compound demonstrates significant biological activity by inhibiting the growth of various cancer cell lines, inducing cell cycle arrest at the G2/M phase, and promoting apoptosis. Research applications include evaluating its antitumor efficacy in preclinical models, making it a valuable reagent for studying mechanisms of cancer progression and potential therapeutic strategies. -
CHK1 Inhibitor
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. -
Telomeric G-Quadruplex Ligand
Telomeric G4s ligand 1 is a telomeric G-quadruplex ligand known for its ability to stabilize telomeric G4 structures and promote R-loop formation, resulting in DNA damage responses. This compound has been shown to induce apoptosis in tumor cells and trigger immunogenic cell death (ICD), making it a valuable tool for cancer research and therapeutic applications. -
c-Myc Inhibitor
(-)-CMLD010509 is a potent c-Myc inhibitor that selectively targets the oncogenic translation program associated with multiple myeloma. This compound demonstrates significant activity, exhibiting an IC50 of less than 10 nM in various multiple myeloma cell lines, leading to the induction of apoptosis. (-)-CMLD010509 operates through a mechanism that is independent of eIF4E phosphorylation, making it a valuable tool for studying the translation control of key oncoproteins such as MYC, MDM2, CCND1, MAF, and MCL-1. -
CDK Inhibitor
R547 mesylate is a potent and selective ATP-competitive inhibitor of cyclin-dependent kinases (CDKs). It exhibits inhibitory constants of 2 nM for CDK1/cyclin B, 3 nM for CDK2/cyclin E, and 1 nM for CDK4/cyclin D1. Due to its oral bioavailability and high specificity, R547 mesylate is valuable for investigating cell cycle regulation and the role of CDKs in cancer research. -
CDK Inhibitor
Otviciclib is a potent cyclin-dependent kinase (CDK) inhibitor that demonstrates significant anti-proliferative effects against various solid tumor cell lines, including HCT116, NCIH82, and DU145. This compound effectively induces cell cycle arrest in the G2/M phase and triggers apoptosis, exhibiting a favorable toxicity profile towards normal cells. Otviciclib shows broad-spectrum anticancer activity, making it a valuable tool for research applications related to colon, pancreatic, and lung cancers. -
Aurora Kinase Inhibitor
Aurora Kinase Inhibitor-14 is a highly selective inhibitor of Aurora kinases, demonstrating IC50 values of 0.5 nM for Aurora A and 1.2 nM for Aurora B. This compound binds to the ATP-binding site of these kinases, effectively disrupting chromosome segregation during mitosis and promoting apoptosis in tumor cells. Aurora Kinase Inhibitor-14 is a valuable tool for investigating the therapeutic potential in various solid tumors and hematological malignancies, including non-small cell lung cancer, breast cancer, and acute myeloid leukemia. -
DYRK1A/DYRK1B Inhibitor
JH-XVII-10 is a highly selective inhibitor of DYRK1A and DYRK1B, exhibiting IC50 values of 3 nM and 5 nM, respectively. This compound demonstrates significant antitumor activity in head and neck squamous cell carcinoma (HNSCC) cell lines. JH-XVII-10 is suitable for research applications focusing on dysregulation of DYRK kinases in cancer. -
Wee1/HDAC Inhibitor
Wee1/HDAC-IN-1 is a dual inhibitor targeting Wee1 and histone deacetylases (HDACs). It demonstrates potent activity with an IC50 of 1.2 nM for Wee1 and varying IC50 values of 196 nM for HDAC1, 156 nM for HDAC3, and 55 nM for HDAC6. This compound displays significant antiproliferative effects in MV4-11 cells, with an IC50 of 0.076 μM, by disrupting DNA damage repair mechanisms and promoting apoptosis. Wee1/HDAC-IN-1 is suited for research on acute myeloid leukemia (AML). -
CDK9/HDAC Dual Inhibitor
CDK9/HDAC1/HDAC3-IN-1 is a dual inhibitor targeting CDK9 and HDACs. With IC50 values of 0.17 μM for CDK9, 1.73 μM for HDAC1, and 1.11 μM for HDAC3, this compound effectively disrupts the activity of these proteins. It induces cancer cell apoptosis and causes cell cycle arrest at the G2/M phase. Additionally, CDK9/HDAC1/HDAC3-IN-1 exhibits broad-spectrum anti-cancer effects, demonstrating efficacy against various malignancies, including breast, cervical, and liver cancers, as evidenced in murine TNBC MDA-MB-231 xenograft models. -
CDK2 Inhibitor
CDK2-IN-9 is a potent inhibitor of cyclin-dependent kinase 2 (CDK2), exhibiting an IC50 of 0.63 µM. This compound demonstrates significant antiproliferative activity, inducing apoptosis and causing cell cycle arrest at the S and G2/M phases. CDK2-IN-9 is suitable for research applications focused on melanoma and the exploration of CDK2's role in cell cycle regulation and cancer biology. -
Aurora A Inhibitor
Aurora A Inhibitor 2 is a potent inhibitor of Aurora A kinase, exhibiting an IC50 value of 21.94 nM. This compound has been shown to induce caspase-dependent apoptosis in MDA-MB-231 cells, highlighting its potential as a therapeutic agent in cancer research. It is useful for studies investigating the role of Aurora A in cell cycle regulation and apoptosis. -
CDKs Inhibitor
(Rac)-Roscovitine is a selective inhibitor of cyclin-dependent kinases (CDKs), functioning by competitively binding to their active sites in place of ATP. This mechanism effectively inhibits CDK phosphorylation activity, leading to apoptosis in cancer cells. As a valuable research tool, (Rac)-Roscovitine is applicable in studies of cancer and various conditions associated with CDK dysregulation, including neurodegenerative diseases, cardiac disorders, and chronic inflammation. -
HDAC/CDK Inhibitor
CDK/HDAC-IN-2 is a dual inhibitor of histone deacetylases (HDACs) and cyclin-dependent kinases (CDKs), exhibiting IC50 values of 6.4 nM for HDAC1, 0.25 nM for HDAC2, 45 nM for HDAC3, and >1000 nM for HDAC6,8, as well as 8.63 nM for CDK1, 0.30 nM for CDK2, and >1000 nM for CDK4,6,7. This compound demonstrates significant antiproliferative effects, inducing apoptosis and causing cell cycle arrest in the G2/M phase. CDK/HDAC-IN-2 is particularly valuable in cancer research due to its potent antitumor efficacy. -
CDK9 Inhibitor
CDK9-IN-18 is a selective inhibitor of cyclin-dependent kinase 9 (CDK9), effectively obstructing its phosphorylation activity. This compound demonstrates significant anticancer properties, promoting apoptosis in various cancer cell lines while exhibiting low cellular toxicity. Its mechanism of action makes CDK9-IN-18 a valuable tool for research into cancer therapeutics and the regulation of gene expression. -
CDK2/Topo I Inhibitor
ZLHQ-5f is a dual inhibitor of Cyclin-dependent kinase 2 (CDK2) and Topoisomerase I (Topo I), exhibiting an IC50 of 0.145 μM against CDK2/CycA2. This compound effectively induces S-phase cell cycle arrest and triggers apoptosis in HCT116 cancer cells. Its favorable safety profile supports its potential applications in cancer research and therapeutic development. -
CDK2/9 Inhibitor
CDK2/9-IN-1 is an orally active dual inhibitor targeting cyclin-dependent kinases CDK2 and CDK9, with IC50 values of 0.004 μM and 0.009 μM, respectively. This compound induces apoptosis through G2/M cell cycle arrest, demonstrating notable antitumor activity. CDK2/9-IN-1 is useful for research applications focused on cancer biology and the modulation of cell cycle regulation. -
Dual PLK1/BET Inhibitor
WNY0824 is a dual inhibitor targeting Polo-like kinase 1 (PLK1) and the Bromodomain and Extra-Terminal (BET) protein family. It demonstrates potent inhibitory activity, with IC50 values of 22 nmol/L for PLK1 and varying efficacy against BRD2, BRD3, BRD4, and BRDT. WNY0824 induces cell cycle arrest and apoptosis by disrupting AR- and MYC-mediated transcriptional processes, making it valuable for research in cancer biology. Furthermore, it has shown effectiveness in inhibiting tumor growth in Enzalutamide-resistant castration-resistant prostate cancer (CRPC) xenograft models, highlighting its potential in overcoming treatment resistance. -
CDK2 Inhibitor
CDK2-IN-55 is a selective CDK2 inhibitor with an IC50 value of 4.7 nM, also exhibiting significant inhibitory action on CDK1 (IC50 = 26.3 nM), alongside moderate inhibition of Aurora A (IC50 = 92.0 nM) and CDK9 (IC50 = 288 nM). Its weak inhibitory profile on CDK4, CDK6, DYRK1A, and GSK3β (IC50 > 1000 nM) highlights its specificity. CDK2-IN-55 demonstrates potent anti-proliferative effects against various cancer cell lines, effectively inducing cell cycle arrest and apoptosis, making it a valuable tool for research related to colorectal, lung, and cervical cancers. -
Cdk1 Inhibitor
BMI-1026 is a potent cyclin-dependent kinase 1 (Cdk1) inhibitor with an IC50 of 2.3 nM. This compound effectively induces apoptosis by interfering with cell cycle progression, specifically by causing a G2-M phase arrest. Its ability to modulate Cdk1 activity makes BMI-1026 valuable for research applications focused on cell division, cancer biology, and therapeutic strategies targeting cell cycle dysregulation. -
Nur77 Antagonist
Nur77 Antagonist 1 is a selective antagonist of the Nur77 receptor, with a binding affinity of KDSPR Nur77 = 91 nM. This compound has demonstrated the ability to induce apoptosis in cancer cells, showcasing significant antitumor activity against triple-negative breast cancer (TNBC) cells. It serves as a valuable tool for research in cancer biology and therapeutic development targeting Nur77 pathways. -
CDK1 Inhibitor
CDK1-IN-8 is a potent inhibitor of Cyclin-dependent kinase 1 (CDK1), primarily targeting the regulation of cell cycle progression. This compound effectively inhibits cell migration, induces apoptosis, and causes cell cycle arrest at the G2/M phase. Notably, CDK1-IN-8 leads to significant downregulation of CDK1 protein levels in HepG2 cells, making it a valuable tool for investigating mechanisms in hepatocellular carcinoma research. -
c-Myc G-quadruplex Stabilizer
Y502-2304 is a potent c-Myc G-quadruplex stabilizer that exhibits significant antiproliferative activity in multiple myeloma (MM) cells. It effectively downregulates both c-Myc mRNA and protein expression, leading to the induction of apoptosis characterized by increased γH2AX levels and elevated reactive oxygen species (ROS). Additionally, Y502-2304 disrupts mitochondrial function and demonstrates a marked inhibition of tumor growth in xenograft models of MM. This compound is suitable for various research applications focused on elucidating the molecular mechanisms underlying multiple myeloma. -
PKMYT1 Inhibitor
PD-166285 is a potent inhibitor of PKMYT1, exhibiting an IC50 value of 17 nM. This compound demonstrates significant antiproliferative activity against CCNE1-amplified cancer cell lines, including OVCAR3 (IC50 = 0.14 μM) and HCC1569 (IC50 = 0.21 μM). In addition to its antiproliferative effects, PD-166285 induces apoptosis and effectively arrests CCNE1-amplified HCC1569 cells in the G1/S phase of the cell cycle. This reagent serves as a valuable tool for exploring PKMYT1-targeted therapies in the context of CCNE1-amplified malignancies. -
CDK7 Inhibitor
SY-5102 is a potent and selective inhibitor of cyclin-dependent kinase 7 (CDK7) with a Kd of 0.03 nM. This compound exhibits significant anti-proliferative activity in HCC70 cells, with an EC50 of 9 nM, and effectively modulates CDK7-mediated functions, including downregulation of CDK2 Thr160 and RNA polymerase II Ser5 phosphorylation. SY-5102 induces G2/M cell cycle arrest and decreases c-Myc oncogene expression, leading to enhanced apoptosis in cancer cells. It is particularly relevant for research focused on triple-negative breast cancer (TNBC). -
CDKs Inhibitor
ZLWT-37 is a potent, orally active inhibitor of cyclin-dependent kinases (CDKs), specifically exhibiting IC50 values of 0.002 μM against CDK9 and 0.054 μM against CDK2. This compound effectively induces apoptosis and arrests the cell cycle at the G2/M phase in HCT116 cells. ZLWT-37 is valuable for researching CDK-related pathways and investigating therapeutic strategies in cancer treatment. -
CDK4 Inhibitor
ZDLD13 is a selective inhibitor of Cyclin-Dependent Kinase 4 (CDK4) with an IC50 of 0.38 μM. This β-carboline compound demonstrates potent anti-cancer activity against HCT116 cells, effectively inhibiting colony formation, invasion, and migration, while also inducing apoptosis and G1 phase cell cycle arrest. Additionally, ZDLD13 significantly inhibits tumor growth in HCT116 tumor xenograft models, making it a valuable tool for cancer research. -
CDK1 Inhibitor
CGP-74514 hydrochloride is a highly selective inhibitor of cyclin-dependent kinase 1 (CDK1) with an IC50 of 25 nM. By inhibiting the CDK1/cyclin B complex, it effectively induces cell cycle arrest at the G2/M phase and promotes apoptosis in tumor cells. This compound shows potential for use in research related to bladder cancer and other malignancies driven by CDK1 deregulation. -
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. -
PDE2/CDK2 Inhibitor
Aristolochic acid D is a selective inhibitor of PDE2 with an IC50 of 4.673 μM and CDK2 with an IC50 of 25 μM, derived from Aristolochia indica L. This compound demonstrates significant anti-inflammatory properties while exhibiting a non-carcinogenic and non-nephrotoxic profile. Aristolochic acid D is valuable for research applications focused on inflammation and tumor-related diseases, offering insights into therapeutic strategies. -
SHP2/CDK4 Inhibitor
SHP2/CDK4-IN-1 is a potent dual inhibitor of SHP2 and CDK4, exhibiting IC50 values of 4.3 nM and 18.2 nM, respectively. This compound effectively induces G0/G1 phase cell cycle arrest, thereby inhibiting the proliferation of triple-negative breast cancer (TNBC) cell lines. In preclinical studies, SHP2/CDK4-IN-1 demonstrated significant antitumor efficacy in the EMT6 syngeneic mouse model, making it a valuable tool for research on TNBC. -
CDK1/CDK2 Inhibitor
K00546 is a highly selective inhibitor of cyclin-dependent kinases CDK1 and CDK2, exhibiting IC50 values of 0.6 nM and 0.5 nM, respectively, for CDK1/cyclin B and CDK2/cyclin A complexes. In addition, K00546 effectively inhibits CDC2-like kinases CLK1 and CLK3, with IC50 values of 8.9 nM and 29.2 nM, respectively. This compound is valuable for research focused on cell cycle regulation and the mechanistic study of kinase activity in cancer biology. -
Aurora/VEGF/PDGF Inhibitor
Ilorasertib hydrochloride is a potent, orally active inhibitor targeting Aurora kinases, with IC50 values of 116 nM, 5 nM, and 1 nM for Aurora A, B, and C, respectively. Additionally, it exhibits significant inhibition of VEGF and PDGF pathways. This compound is valuable for research related to acute myeloid leukemia (AML) and myelodysplastic syndrome (MDS), facilitating studies into the mechanisms of these hematologic malignancies. -
CDK Inhibitor
GW297361 is an oxindole compound identified as a cyclin-dependent kinase (CDK) inhibitor with a selective action on Pho85 in cellular systems. It demonstrates significant inhibitory effects on yeast Cdk1 and Pho85, exhibiting IC50 values of 20 nM and 400 nM, respectively. This compound is valuable for research applications focused on cell cycle regulation and the study of kinase signaling pathways. -
DYRK1A Inhibitor
GNF2133 is a potent and selective inhibitor of DYRK1A, exhibiting an IC50 of 0.0062 µM for DYRK1A, with minimal activity against GSK3β (>50 µM). This compound has demonstrated significant proliferation potency and efficacy in both rat and human primary β-cells. GNF2133 notably enhances glucose disposal capacity and stimulates insulin secretion, making it a valuable reagent for research into type 1 diabetes.
