Catalog No.
Product Name
Application
Product Information
Citations
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PLK1 Inhibitor
TAK-960 monohydrochloride is a selective inhibitor of polo-like kinase 1 (PLK1), exhibiting an IC50 of 0.8 nM. It also demonstrates inhibitory effects on PLK2 and PLK3 with IC50 values of 16.9 nM and 50.2 nM, respectively. This compound effectively inhibits the proliferation of various cancer cell lines and shows significant antitumor activity in multiple tumor xenograft models, making it a valuable tool for cancer research applications. -
Plk1 Inhibitor
ZK-Thiazolidinone is a potent ATP-competitive inhibitor of Polo-like kinase 1 (Plk1), exhibiting an IC50 of 19 nM. It effectively inhibits tumor cell proliferation, induces cell cycle arrest, and causes characteristic mitotic defects. The compound disrupts the recruitment of γ-tubulin and Aurora A kinase to centrosomes, leading to compromised bipolar spindle maintenance and sister chromatid cohesion. ZK-Thiazolidinone is valuable for applications in cancer research. -
PLK1 Inhibitor
PLK1-IN-7 is a highly effective inhibitor of Polo-like kinase 1 (PLK1), demonstrating an IC50 of 0.66 nM. This compound exhibits significant antiproliferative and antitumor activities, making it a valuable tool for cancer research. Its ability to modulate PLK1 activity supports investigations into cell cycle regulation and potential therapeutic applications in oncology. -
PLK1 Inhibitor
IIP0943 is a potent and selective inhibitor of PLK1 (polo-like kinase 1), exhibiting an IC50 of 5.1 nM. This compound demonstrates significant antiproliferative activity against HCT116 cancer cells, with an IC50 of 0.22 µM. IIP0943 is a valuable tool for researchers investigating cancer therapeutics and the role of PLK1 in cell cycle regulation and tumor growth. -
Polo-like Kinase (PLK) Inhibitor
Poloxin-2 is a specific inhibitor of Polo-like Kinase 1 (PLK1), effectively inducing mitotic arrest in HeLa cells with an EC50 of approximately 15 μM. It targets the Polo-box domain to disrupt protein-protein interactions, facilitating its application in cancer research. The hydrophobic tag (HT) conjugated form, Poloxin-2HT, exhibits enhanced potency by promoting selective degradation of the PLK1 protein, resulting in increased apoptosis and reduced cell viability. This highlights the potential of hydrophobic tags as a novel strategy for targeting disease-associated proteins. -
PLK Inhibitor
PLK1-IN-9 is a potent inhibitor of polo-like kinase 1 (PLK1) that shows effective inhibition of modified PLK proteins, specifically 1010pT, cdc25c, and PBIP, with IC50 values of 1.6, 0.8, and 1.4 μM, respectively. This compound exhibits significant antiproliferative effects on various cancer cell lines, including HeLa, HL60, SNU387/499, and HepG2, where it induces cytotoxicity and apoptosis. In vivo studies demonstrate that PLK1-IN-9 effectively inhibits tumor growth in a HepG2 xenograft mouse model, highlighting its potential for cancer research applications. -
PLK1 Inhibitor
CD 10899 is a potent Polo-like kinase 1 (PLK1) inhibitor, exhibiting an IC50 of 6 nM. As a hydroxylated metabolite of Volasertib, CD 10899 demonstrates significant pharmacological activity against PLK1, an important target in cancer research. This compound is valuable for studies exploring PLK1's role in cell cycle regulation and tumor progression, making it a useful tool for cancer-related investigations. -
RAD51-BRCA2 Inhibitor
Homologous recombination-IN-1 is an inhibitor of the RAD51-BRCA2 protein-protein interaction, demonstrating an EC50 of 19 μM. This compound effectively disrupts homologous recombination processes, making it a valuable tool for studying DNA repair mechanisms and the underlying biology of cancer. Researchers can utilize Homologous recombination-IN-1 to investigate the roles of RAD51 and BRCA2 in genetic stability and therapeutic responses. -
RAD51 Inhibitor
RAD51-IN-1 is a selective inhibitor of the RAD51 protein, which is crucial for homologous recombination and DNA repair processes. This compound has demonstrated significant anti-tumor activity and may be utilized in cancer research to explore its potential in enhancing the effectiveness of cancer therapies by targeting DNA repair mechanisms. Its application may also extend to investigations of DNA damage response pathways and their implications in cancer biology. -
RAD51 Inhibitor
RAD51-IN-5 is a selective inhibitor of RAD51, a key protein involved in homologous recombination repair of DNA double-strand breaks. This compound demonstrates potential in exploring therapeutic strategies for conditions associated with mitochondrial defects. Its activity against RAD51 may provide insights into DNA repair mechanisms and related cellular processes in various research applications. -
RAD51 Inhibitor
RAD51-IN-3 is a potent inhibitor of the RAD51 protein, which plays a crucial role in homologous recombination and DNA repair mechanisms. By targeting RAD51, this compound interferes with DNA damage response pathways, making it valuable for research in cancer biology, particularly in exploring therapeutic strategies that exploit DNA repair deficiencies. Its application extends to studies investigating the sensitivity of tumor cells to chemotherapeutic agents and the development of novel cancer treatment modalities. -
RAD51 Inhibitor
RAD51-IN-4 is a potent inhibitor of the RAD51 protein, essential for homologous recombination and DNA repair in eukaryotic cells. This compound demonstrates significant anti-proliferative activity and has potential applications in studying conditions associated with mitochondrial defects and genomic stability. Researchers may utilize RAD51-IN-4 to explore cancer biology, therapeutic resistance, and the underlying mechanisms of DNA repair processes. -
RAD51 Inhibitor
RAD51-IN-7 is a selective inhibitor of RAD51, a key protein involved in homologous recombination and DNA repair mechanisms in eukaryotic cells. This compound is valuable for investigating conditions associated with mitochondrial dysfunction and its role in cancer biology. The potential applications of RAD51-IN-7 extend to studies targeting cellular responses to genotoxic stress and the development of therapeutic strategies for genetic diseases. -
RAD51 Inhibitor
RAD51-IN-6 is a highly effective inhibitor of RAD51, a key protein involved in homologous recombination and DNA repair in eukaryotic cells. This compound demonstrates significant biological activity by interfering with RAD51-mediated processes, making it a valuable tool for studying conditions related to mitochondrial defects and other genomic instability disorders. Its application in research may provide insights into therapeutic strategies targeting RAD51-related pathways. -
RAD51/HR Inhibitor
RI(dl)-2 is a potent inhibitor of RAD51, specifically targeting its D-loop activity with an IC50 of 11.1 µM, and effectively inhibiting homologous recombination (HR) with an IC50 of 3.0 µM. This compound disrupts HR-mediated repair of DNA double-strand breaks, leading to increased sensitivity in various cancer cell lines. RI(dl)-2 serves as a valuable tool for investigating HR processes and exploring potential therapeutic strategies in cancer research. -
RAD51 Inhibitor
DIDS is a RAD51 inhibitor that disrupts RAD51-mediated homologous pairing and strand exchange reactions, thereby impacting DNA repair processes. In addition to its primary function, DIDS also inhibits ABCA1 and VDAC1, affecting anion exchange and binding to red blood cell membranes. Furthermore, it has been shown to inhibit the activation of caspase-3 and -9, making it a valuable tool for cancer research applications. -
RAD51 Inhibitor
RAD51-IN-9 is a potent inhibitor of RAD51, effectively disrupting the binding of RAD51 to single-stranded DNA with an IC50 of 17.85 μM. This compound demonstrates an LD50 against HEK293 cells of 40.21 μM and is capable of sensitizing cells to the cytotoxic effects of Mitomycin C. RAD51-IN-9 is a valuable tool for research focused on DNA repair mechanisms and the therapeutic targeting of cancer cells. -
BRCA2-RAD51 Inhibitor
BRCA2-RAD51-IN-1 is a specific inhibitor of the BRCA2-RAD51 complex, demonstrated to have an EC50 value of 28 μM. This compound exhibits notable antitumor activity, making it a valuable tool for research into cancer treatments targeting DNA repair mechanisms. Its application in studies of BRCA-mediated tumorigenesis helps elucidate potential therapeutic strategies for cancers associated with BRCA2 mutations. -
PKMYT1 Inhibitor
Lunresertib (RP-6306) is a potent and selective inhibitor of PKMYT1, demonstrating an IC50 of 14 nM. This compound exhibits high selectivity for PKMYT1 in cellular binding assays, making it an effective tool for studying the role of this kinase in cancer biology. Lunresertib's anticancer properties highlight its potential applications in cancer research and therapeutic development. -
Wee1 Inhibitor
Azenosertib is a highly selective orally active Wee1 inhibitor, with an IC50 of 3.9 nM. It demonstrates significant antitumor activity, making it a valuable tool for cancer research. Azenosertib is utilized in studies investigating cell cycle regulation and DNA damage response pathways, contributing to the development of novel therapeutic strategies against various malignancies. -
WEE1 Inhibitor
WEE1-IN-14 is a selective WEE1 inhibitor, exhibiting an IC50 of 0.5 nM in L-RB-FEP calculations and 1.0 nM in the ADP-Glo kinase assay. By inhibiting WEE1, this compound disrupts the G2-M checkpoint in cancer cells, effectively removing cell cycle regulatory controls. The resulting early onset of mitotic failure triggers apoptosis in tumor cells, making WEE1-IN-14 a valuable reagent for research in cancer biology and therapeutic development. -
PKMYT1 Inhibitor
GSK-1520489A is a selective inhibitor of PKMYT1, an active protein kinase involved in cell cycle regulation. It exhibits an IC50 of 115 nM and a Ki value of 10.94 nM, demonstrating significant potency in inhibition. This compound is useful for exploring the role of PKMYT1 in tumorigenesis and cell proliferation, making it a valuable tool in cancer research and therapeutic discovery. -
Wee1 Kinase Inhibitor
WEE1-IN-4 is a potent inhibitor of the Wee1 kinase, exhibiting an IC50 of 0.011 μM. By targeting and inhibiting Wee1, this compound effectively abrogates the G2/M checkpoint, thereby promoting cell cycle progression in cancer cells. WEE1-IN-4 serves as a valuable tool for research in cancer biology and therapeutics, particularly in studies focused on cell cycle regulation and the development of combination therapies. -
Myt1 Inhibitor
(Rac)-lunresertib is a potent inhibitor of the membrane-associated tyrosine and threonine-specific cdc2-inhibitory kinase (Myt1), with an IC50 of less than 10 nM. This compound demonstrates significant anticancer activity, making it a valuable reagent for research focused on targeting cell cycle regulation and kinase activity in cancer biology. Its precise inhibition of Myt1 positions it as a key tool for investigating therapeutic strategies in oncology. -
WEE1 DUBTAC
LEB-03-146 is a WEE1 deubiquitinase-targeting chimera (DUBTAC) that conjugates the potent inhibitor AZD1775 (Adavosertib) with the recruiter EN523 via a PEG2 linker. This compound effectively stabilizes WEE1 in HEP3B hepatoma cancer cells, making it a valuable tool for research into cell cycle regulation and cancer therapy. Its unique mechanism of action offers potential for novel therapeutic strategies in oncology. -
Wee1/2 Inhibitor
Bosutinib isomer is a potent inhibitor of the cell cycle regulators Wee1 and Wee2, exhibiting high binding affinities with Kd values of 43.7 ± 10.0 nM and 4.7 ± 2.3 nM, respectively. This compound is utilized in research applications aimed at understanding cell cycle modulation and exploring therapeutic strategies in cancer treatment, particularly in tumors with aberrant cell cycle regulation. -
Wee1 Inhibitor
WEE1-IN-3 is a potent inhibitor of Wee1 kinase, demonstrating an IC50 of less than 10 nM. This compound exhibits significant anticancer activity, making it a valuable tool for research in cancer biology. Its ability to modulate cell cycle regulation positions WEE1-IN-3 as a useful reagent for exploring therapeutic strategies against various cancer types. -
PKMYT1 Inhibitor
PKMYT1-IN-8 is a specific inhibitor of PKMYT1, demonstrating an IC50 of 9 nM. In addition to its primary target, it also inhibits several receptor tyrosine kinases, including EPHB3, EPHA1, KIT, EPHB1, EPHA2, EPHA3, and EPHB2, with varying IC50 values ranging from 1.79 to 10.9 μM. This compound effectively reduces the proliferation of the OVCAR3 cancer cell line, exhibiting a GI50 of 2.02 μM. PKMYT1-IN-8 is useful for research focused on cancer biology and targeted therapies. -
WEE1 Inhibitor
WEE1-IN-10 is a selective inhibitor of WEE1 kinase, a critical regulator of the cell cycle. It demonstrates potent inhibitory activity against LOVO cancer cell growth, with an IC50 of 0.524 μM. This compound is applicable in research focusing on diseases associated with aberrant WEE1 activity, providing insights into cell cycle regulation and potential therapeutic strategies. -
myt1 Inhibitor
(R)-lunresertib is a selective inhibitor of the myt1 kinase (PKMYT1), exhibiting an IC50 of 1360 nM. This compound is valuable for investigating Myt1-mediated signaling pathways and related oncogenic processes. Its application in cancer research highlights the potential for therapeutic interventions targeting Myt1 activity in tumor biology. -
Myt1 Inhibitor
Myt1-IN-3 is a potent inhibitor of Myt1, a membrane-associated kinase that specifically targets tyrosine and threonine residues and inhibits cdc2 activity. With an IC50 of less than 10 nM, it effectively modulates Myt1 activity, making it a valuable tool for investigating cell cycle regulation. This compound is suitable for research applications focused on cancer biology, cell proliferation, and kinase signaling pathways. -
Myt1 Inhibitor
Myt1-IN-1 is a potent inhibitor of Myt1 (PKMYT1), a membrane-associated kinase that specifically targets tyrosine and threonine residues with an IC50 of less than 10 nM. This compound exhibits significant anticancer activity, making it a valuable tool for research focused on cell cycle regulation and cancer therapeutics. Myt1-IN-1 is useful for studies investigating the role of Myt1 in tumor progression and offers insights into potential treatment strategies for various cancers. -
WEE1/PKMYT1 Inhibitor
WEE1/PKMYT1-IN-1 is a potent inhibitor targeting WEE1 and PKMYT1 kinases. This compound exhibits significant antiproliferative activity, making it suitable for research applications in cancer biology. It can be utilized to investigate cell cycle regulation and the mechanistic pathways involved in tumor cell proliferation. -
PKMYT1 Inhibitor
PKMYT1-IN-1 is a selective inhibitor of the membrane-associated tyrosine and threonine kinase, PKMYT1, demonstrating an IC50 of 8.8 nM. This reagent effectively inhibits the proliferation of HCC1569 tumor cells with an IC50 of 42 nM, making it a valuable tool for research into cancer biology and therapeutic interventions targeting PKMYT1 pathways. Its specificity and potency offer significant potential for studying the role of PKMYT1 in oncogenic processes. -
Myt1 Inhibitor
Myt1-IN-2 is a potent inhibitor of the membrane-associated cdc2-inhibitory kinase, Myt1 (Gene name: PKMYT1), demonstrating an IC50 of less than 10 nM. This compound exhibits significant antitumor activity, making it a valuable tool for cancer research. Myt1-IN-2 can be utilized in studies aimed at elucidating the role of Myt1 in cell cycle regulation and its implications in oncogenesis. -
WEE1 DUBTAC
LEB-03-144 is a WEE1 DUBTAC (deubiquitinase-targeting chimera) designed to link AZD1775 (Adavosertib) with the OTUB1 recruiter EN523 via a C3 alkyl linker. This compound demonstrates notable stabilization of WEE1 in HEP3B hepatoma cancer cells, indicating its potential role in enhancing the therapeutic efficacy of WEE1 inhibition. LEB-03-144 is suitable for studies focused on cancer biology and drug discovery applications targeting WEE1-mediated signaling pathways. -
PKMYT1 Inhibitor
PKMYT1-IN-9 is a selective inhibitor of PKMYT1, demonstrating an IC50 of 4.4 nM. This compound shows significantly higher selectivity for PKMYT1 compared to WEE1, which has an IC50 of 32.4 μM. PKMYT1-IN-9 has been characterized by its antitumor activity, making it a valuable tool in cancer research and therapeutic studies targeting checkpoint pathways. -
Wee1 Inhibitor
WEE1-IN-12 is a potent Wee1 kinase inhibitor with an IC50 of 2.0 nM. It demonstrates significant antiproliferative effects in HT29 colorectal cancer cells, exhibiting an IC50 of 1.07 μM. The compound enhances the efficacy of Gemcitabine, showing improved activity with an IC50 of 0.34 μM in combination studies. WEE1-IN-12 is valuable for research into targeted therapies for tumors, particularly colon cancer. -
PKMYT1 Inhibitor
PKMYT1-IN-2 is a potent inhibitor of PKMYT1, exhibiting an IC50 value of 5.7 nM. This compound effectively suppresses the growth of HCC1569 cancer cells with an IC50 of 22 nM. PKMYT1-IN-2 serves as a valuable tool for research in cancer biology, particularly in studies focused on targeting the PKMYT1 pathway for therapeutic interventions. -
WEE1/PKMYT1 Inhibitor
WEE1/PKMYT1-IN-2 is a potent inhibitor of WEE1 and PKMYT1 kinases, exhibiting an axial chiral P configuration. This compound demonstrates significant antiproliferative activity, making it a valuable tool for cancer research. It is particularly relevant for studies investigating cell cycle regulation and the therapeutic potential of targeting WEE1 and PKMYT1 in various malignancies. -
Anticancer Agent
i-AZD1775 TFA is an immobilizable analogue of AZD1775, functioning as a selective inhibitor of the WEE1 kinase. This compound exhibits significant potential in inhibiting cell cycle regulation, enabling the investigation of its efficacy in cancer cell lines. i-AZD1775 TFA is valuable for studies focused on anticancer therapies, particularly in exploring combination treatments and resistance mechanisms in various tumor types. -
Wee1 Inhibitor
WEE1-IN-9 is a selective inhibitor of the Wee1 kinase, which plays a critical role in regulating the cell cycle by inhibiting the progression from G2 to mitosis. This compound exhibits potent anti-tumor activity and is valuable for studying the effects of Wee1 inhibition in cancer research. WEE1-IN-9 can be utilized in investigations of cancer cell proliferation and therapy resistance mechanisms, contributing to the development of novel cancer treatments. -
WEE1 Inhibitor
WEE1-IN-6 is a potent WEE1 inhibitor with a DC50 value of ≤ 100 nM. This compound effectively inhibits cell proliferation, making it a valuable tool for studies related to cell cycle regulation and cancer research. Its oral bioactivity enables convenient administration in various in vivo studies targeting WEE1 pathways. -
WEE1/PKMYT1 Inhibitor
WEE1/PKMYT1-IN-3 is a potent inhibitor of WEE1 and PKMYT1, specifically designed with an axial chiral M configuration. This compound exhibits significant antiproliferative activity, making it a valuable tool for cancer research. It can be utilized to explore the mechanisms of cell cycle regulation and to investigate therapeutic strategies targeting these critical kinases in various malignancies. -
WEE1 DUBTAC
LEB-03-145 is a WEE1 deubiquitinase-targeting chimera (DUBTAC) that effectively links AZD1775 (Adavosertib) to the OTUB1 recruiter EN523 via a C5 alkyl linker. This compound enhances the stability and activity of AZD1775 by modulating ubiquitination processes. LEB-03-145 is valuable for studying WEE1 regulation and offers potential in cancer research, particularly in the context of targeting tumor cell proliferation and survival pathways. -
WEE1 Inhibitor
WEE1-IN-8 is a highly selective WEE1 inhibitor, exhibiting an IC50 of 0.98 nM. This compound is effective in research applications targeting various malignancies, including pancreatic cancer, ovarian cancer, colorectal cancer, and uterine serous carcinoma. By facilitating the abrogation of G2/M checkpoint control, WEE1-IN-8 demonstrates potential as a therapeutic agent in cancer treatment strategies. -
Target Protein Ligand-Linker Conjugate
Adavosertib-C3-NH-Boc is a target protein ligand-linker conjugate designed to incorporate a Wee1 ligand and a PROTAC linker, facilitating the recruitment of E3 ligases. This compound enables the synthesis of PROTAC Pomalidomide-C3-adavosertib, allowing for targeted protein degradation studies. It serves as a useful tool in the exploration of therapeutic mechanisms involving protein regulation and degradation in cancer research and other biological applications. -
PKMYT1 Inhibtor
PKMYT1-IN-11 is a potent inhibitor of PKMYT1, exhibiting an IC50 of 4.49 nM. This compound effectively suppresses the proliferation of HCC1569 cancer cells and demonstrates a significant anti-tumor effect in combination with Gemcitabine in the OVCAR3 xenograft mouse model. PKMYT1-IN-11 is valuable for researching various cancers, including breast and ovarian cancer, providing insights into therapeutic strategies targeting PKMYT1. -
Wee1 Inhibitor
WEE1-IN-11 is a potent inhibitor of the Wee1 kinase, demonstrating an impressive IC50 of 2.0 nM against CDK2. This compound effectively inhibits various cancer cell lines, including NCI-H446, A427, OVCAR3, C33A, and WiDr, with IC50 values of 93.9 nM, 34.5 nM, 86.7 nM, 23.1 nM, and 85 nM, respectively. It serves as a valuable tool for investigating cell cycle regulation and the therapeutic potential of targeting Wee1 in cancer research. -
WEE1 DUBTAC
LEB-03-153 is a WEE1 deubiquitinase-targeting chimera (DUBTAC) designed to effectively recruit OTUB1 to the WEE1 protein via a novel mechanism. This compound facilitates the modulation of WEE1 activity, potentially influencing cell cycle progression and enhancing the therapeutic effects of AZD1775 (Adavosertib). LEB-03-153 is ideal for research applications involving cancer biology, particularly in studies focused on checkpoint regulation and therapeutic resistance.
