wee1

WEE1-IN-3 (JUN76288) is a potent Wee1 kinase inhibitor with an IC50 of <10 nM. It treatment of cancer and other proliferative diseases.

ZNL 02-096 (Pomalidomide-C3-adavosertib) is a rapid and selective degrader of Wee1 (IC50=3.58 nM).ZNL 02-096 selectively degrades Wee1 at submolar concentrations without damaging PLK1, a secondary target of AZD 1775.ZNL 02-096 induces degradation of Wee1 and accumulation of DNA damage in MOLT-4 cells in vitro, In vitro in MOLT-4 cells, ZNL 02-096 induced Wee1 degradation, accumulation of DNA damage, cell cycle arrest in G2/M phase and apoptosis.ZNL 02-096 showed anti-proliferative effects in 300 cancer cell lines.

Adavosertib (MK-1775) is a small molecule inhibitor of the checkpoint kinase WEE1 (IC50: 5.2 nM). It hinders the G2 DNA damage checkpoint.

PD 407824 is a chemical BMP sensitiser that promotes increased cellular sensitivity to subthreshold amounts of BMP4.PD 407824 is a potent inhibitor of the checkpoint kinases Chk1 and WEE1 (IC50s: 47 and 97 nM, respectively).

PD0166285 is a potent Wee1 and Chk1 inhibitor with activity at nanomolar concentrations.PD0166285 is a novel G2 checkpoint abrogator.

Azenosertib (ZN-c3) is a potent and selective Wee1 inhibitor with balanced potency, ADME, and pharmacokinetic properties.[1]

Debio-0123 (WEE1-IN-5) is a potent, orally available and highly specific WEE1 inhibitor with an IC 50 in the low nanomolar range. Debio-0123 inhibits phospho-CDC2 which translated into an increase in DNA damage and premature entry into mitosis. Debio-0123 increases the antitumoral activity of Carboplatin in vivo whereas neither agent was active alone [1].

WEE1/PKMYT1-IN-1 (compound 75) is an effective and orally bioavailable inhibitor of WEE1 and PKMYT1. It demonstrates antiproliferative activity.

HEMTACWEE1degrader-1 is a WEE1-targeting heterobifunctional chimeric degrader (HEMTAC) facilitated by HSP90, exhibiting an HSP90 enzyme inhibitory activity with an IC50 of 16.76 nM. It enhances the ubiquitination and subsequent degradation of WEE1, effectively blocking the G2/M cell cycle transition. This compound shows anticancer properties in patient-derived xenograft (PDX) models of acute myeloid leukemia (AML). HEMTACWEE1degrader-1 is utilized in AML research.

WEE1/PKMYT1-IN-2 is the axial chiral P configuration of WEE1/PKMYT1-IN-1. WEE1/PKMYT1-IN-1 is an effective and orally bioavailable inhibitor of WEE1 and PKMYT1, exhibiting antiproliferative activity.

Wee1/HDAC-IN-1 is a dual inhibitor targeting Wee1 and HDACs, exhibiting IC50 values of 1.2 nM for Wee1, 196 nM for HDAC1, 156 nM for HDAC3, and 55 nM for HDAC6. It shows potent antiproliferative activity against MV4-11 cells, with an IC50 of 0.076 μM. This compound selectively binds to the catalytic sites of Wee1 and HDACs, disrupting DNA damage repair pathways and inducing apoptosis in MV4-11 cells (apoptosis). Wee1/HDAC-IN-1 is applicable for studying acute myeloid leukemia.

WEE1-IN-10 (compound 77) is a Wee1 kinase inhibitor that inhibits the growth of LOVO cells (IC50=0.524 μM) and can be used to study diseases caused by abnormal Wee1 activity, such as pancreatic cancer, malignant melanoma, and malignant glioma.

WEE1-IN-11 (Compound 13) serves as a potent CDK2 inhibitor with an IC50 of 2.0 nM. It exhibits inhibitory effects on several cell lines, including NCI-H446, A427, OVCAR3, C33A, and WiDr, with respective IC50 values of 93.9, 34.5, 86.7, 23.1, and 85 nM.

WEE1-IN-12 (Compound 87) is a Wee1 kinase inhibitor with an IC50 of 2.0 nM. It inhibits the proliferation of HT29 cells (IC50: 1.07 μM) and shows enhanced efficacy when combined with Gemcitabine (IC50: 0.34 μM). WEE1-IN-12 is applicable in the study of tumors such as colon cancer.

WEE1-IN-14 (Compound 14) is a selective WEE1 inhibitor, with an IC50 of 0.5 nM determined by L-RB-FEP calculations and 1.0 nM in ADP-Glo​​ kinase assays. Inhibition of Wee1 in cancer cells disrupts the G2-M checkpoint, removing cell cycle regulation, leading to premature mitotic failure and subsequent tumor cell apoptosis. Thus, WEE1-IN-14 serves as a valuable tool for studying cancer biology.

WEE1-IN-13 (Compound 10) is a highly selective inhibitor of the WEE1 kinase (IC50=0.7 nM). It can disrupt the G2/M checkpoint and induce apoptosis in tumor cells. WEE1-IN-13 shows potential for research in solid tumors, including non-small cell lung cancer and ovarian cancer.

Wee1 Inhibitor I is an ATP-binding site-targeting Wee1 inhibitor.

WEE1-IN-6 (compound 110) is an orally active inhibitor of WEE1, displaying a DC50 value of ≤ 100 nM. This compound effectively inhibits cell proliferation [1].

WEE1degrader 1 (Compound 10) functions as a Wee1 degrader, exhibiting a DC50 value of 1.5 nM against Wee1. This compound also possesses anticancer properties that inhibit cell proliferation.

WEE1-IN-7 (compound 12h) is a potent, orally active WEE1 inhibitor with an IC50 value of 2.1 nM. This compound induces apoptosis and causes cell cycle arrest in the S phase, demonstrating antitumor activity.

Lunresertib (RP-6306) is a potent, selective, and orally active PKMYT1 inhibitor with an IC50 of 14 nM. Lunresertib (RP-6306) inhibits the growth of CCNE1-amplified tumor cells in several preclinical xenograft models.

AZD 1775 Linker Conjugate 1 TFA is a compound involved in ubiquitinase-targeted chimeric assays

Griseofulvin (Fulvicin) is an antifungal agent used in the treatment of TINEA infections.

PKMYT1-IN-9 is a highly selective, orally active inhibitor of PKMYT1 with an IC50 of 4.4 nM. It exhibits greater selectivity for PKMYT1 compared to WEE1, for which the IC50 is 32.4 μM. Additionally, PKMYT1-IN-9 demonstrates antitumor activity.