Wee1

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.

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.

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].

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.

RSS0680 is a protein kinase degrader that degrades a variety of kinases and can be used to study diseases caused by kinase abnormalities.

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

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

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

PF-06651481-00 (Bosutinib Isomer I) is a Bosutinib analog and a Bcr-Abl 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).

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.

PKMYT1-IN-4 (compound 27) functions as a PKMYT1 inhibitor with an IC50 value under 50 nM.

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.

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].

BMS-986463 is a WEE1 kinase molecule gel degrader and a CRBN E3 ligase regulator (CELMoD). BMS-986463 significantly inhibits tumor regression and reduces the level of phosphorylated CDK2. BMS-986463 can be used in the research of advanced malignant solid tumors such as non-small cell lung cancer (NSCLC).

Myt1-IN-5 (compound 4) is an inhibitor of MYT1 with an IC50 of less than 200 nM.

PKMYT1-IN-3 (compound 8ma) is a potent, selective inhibitor of PKMYT1, demonstrating an IC50 of 16.5 nM and exhibiting antitumor 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 Inhibitor I is an ATP-binding site-targeting Wee1 inhibitor.

PKMYT1-IN-6 (compound 98) is an inhibitor of PKMYT1, exhibiting an IC50 of less than 50nM.

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