Catalog No.
Product Name
Application
Product Information
Citations
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WEE1 Inhibitor
MK-1775 is a potent and selective Wee1 kinase inhibitor in vitro and in vivo.- Hayden L Bell, .et al. , Cancer Cell Int, 2023, Sep 15;23(1):202 PMID: 37715172
- Chiao-Ping Chen, .et al. , Biomed Pharmacother, 2023, Oct:166:115389 PMID: 37659202
- Ting-Yu Chang, .et al. , Biomed Pharmacother, 2021, Jun;138:111485 PMID: 33740521
- 2018, .et al. , FEBS Open Bio, 2018, Jun; 8(6): 1001-1012 PMID: 29928579
- Rulina AV, .et al. , Cell Death Dis, 2016, Dec 1;7(12):e2505 PMID: 27906189
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Wee1/Chk inhibitor
PD0166285 is a potent Wee1 and Chk1 inhibitor with activity at nanomolar concentrations.PD0166285 is a novel G2 checkpoint abrogator.- Trang H. Nguyen Vu, .et al. , Cancer Sci, 2023, Dec; 114(12): 4664-4676 PMID: 37724648
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PROTAC Wee1 degrader
Pomalidomide-C3-adavosertib is a rapid and selective PROTAC degrader of Wee1, with an IC₅₀ of 3.58 nM. It exhibits anti-proliferative activity against cancer cells and induces apoptosis. -
Wee1 Inhibitor
WEE1-IN-7 is a selective Wee1 inhibitor with an IC50 value of 2.1 nM. This compound induces apoptosis and facilitates cell cycle arrest during the S phase, making it valuable in the study of tumor biology. WEE1-IN-7 demonstrates significant antitumor activity, providing a useful tool for cancer research and therapeutic development. -
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. -
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). -
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. -
WEE1 HEMTAC Degrader
HEMTAC WEE1 degrader-1 is a HSP90-mediated degrader specifically targeting the WEE1 kinase, with an IC50 of 16.76 nM for HSP90 inhibition. This compound facilitates the ubiquitination and subsequent degradation of WEE1, effectively disrupting the G2/M cell cycle checkpoint. It demonstrates significant anticancer activity in acute myeloid leukemia (AML) patient-derived xenograft models, making it a valuable reagent for research applications in AML therapeutics. -
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. -
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. -
WEE1 Inhibitor
Zedoresertib, a potent WEE1 inhibitor, exhibits an IC50 value of 0.8 nM and effectively inhibits phospho-CDC2. By abrogating the G2 checkpoint, Zedoresertib enhances the sensitivity of cancer cells to DNA-damaging agents, making it a valuable tool for anticancer research. This compound is essential for studies investigating cell cycle regulation and therapeutic strategies in oncology. -
PKMYT1 Inhibitor
PKMYT1-IN-12 is a selective inhibitor of the serine/threonine kinase PKMYT1, demonstrating an IC₅₀ of 2.6 nM. This compound effectively inhibits the phosphorylation of CDK1, with an IC₅₀ of 44 nM, making it a valuable tool for studying cell cycle regulation. Additionally, PKMYT1-IN-12 serves as a target protein ligand for the synthesis of PROTAC D16-M1P2, facilitating advancements in targeted protein degradation research. -
PKMYT1 Inhibitor
PKMYT1-IN-7 is a potent inhibitor of PKMYT1, demonstrating IC50 values of 1.6 nM against PKMYT1 and 0.06 μM against pCDK1. This compound effectively inhibits the phosphorylation of CDK1 at threonine 14 and tyrosine 15, making it valuable for research into cell cycle regulation. PKMYT1-IN-7 has shown significant anticancer activity, supporting its application in cancer biology studies. -
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. -
Wee1 Inhibitor
PKMYT1-IN-4 is a potent PKMYT1 inhibitor with an IC50 of less than 50 nM. This compound selectively targets the Wee1 kinase, a critical regulator of the cell cycle. PKMYT1-IN-4 is utilized in research applications focused on cell cycle regulation and cancer biology, making it suitable for studies exploring therapeutic strategies against proliferative diseases. -
MYT1 Kinase Inhibitor
Myt1-IN-6 is a selective inhibitor of MYT1 kinase, which plays a crucial role in the regulation of cell cycle progression and neuronal differentiation. This compound is particularly relevant for studies involving RB1-deficient cancers, such as triple-negative breast cancer, where MYT1 activity may contribute to oncogenesis and tumor progression. Myt1-IN-6 serves as a valuable tool for exploring therapeutic strategies targeting MYT1 in various malignancies.
