wee1

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.

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

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

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.

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

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 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].

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

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

WEE1-IN-8 (Compound 55) is a selective WEE1 inhibitor with an IC50 value of 0.98 nM. It can be used in the study of various cancers, including pancreatic, ovarian, colorectal, and uterine serous carcinoma.

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.

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.

PKMYT1-IN-8 (Compound 137) is an inhibitor of PKMYT1, with an IC50 value of 9 nM. It also inhibits EPHB3, EPHA1, KIT, EPHB1, EPHA2, EPHA3, and EPHB2, exhibiting IC50 values of 1.79, 3.17, 4.29, 6.32, 6.83, 8.10, and 10.9 μM, respectively. Additionally, PKMYT1-IN-8 suppresses the proliferation of cancer cells OVCAR3 with a GI50 of 2.02 μM.

PD173952 is a tyrosine (Src) kinase and Myt1 inhibitor with antitumor activity, inhibits Lyn, Abl and Csk, and induces Bcr-Abl-dependent hematopoietic cell apoptosis.

GSK-1520489A is an active PKMYT1 inhibitor.

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).

p38α inhibitor9 (Compound 2015) is a p38α inhibitor that effectively blocks the enzyme activity of p38α, with an IC50 of less than 20 nM. It inhibits MK2T334 phosphorylation and activates Cdc25b and Cdc25c while inactivating Wee1, leading to mitotic catastrophe, aneuploidy or polyploidy, and DNA damage. Additionally, p38α inhibitor9 can suppress colorectal cancer (CRC) metastasis.

PD-166285 is an effective and broadly active inhibitor of protein tyrosine kinase.

LEB-03-146, a WEE1 DUBTAC (deubiquitinase-targeting chimera), effectively links AZD1775 (Adavosertib) with the OTUB1 recruiter EN523 via a PEG2 linker. This compound demonstrates considerable WEE1 stabilization in HEP3B hepatoma cancer cells [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].