wee1

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]

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.

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

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-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-9 (Compound 1) is a Wee1 inhibitor used for cancer research.

Wee1 Inhibitor I 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.

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

WEE1-IN-10 (compound 77) is an inhibitor of the Wee1 kinase. It exhibits inhibitory activity against the growth of LOVO cells, with an IC50 value of 0.524 μM. WEE1-IN-10 can be utilized in researching diseases caused by aberrant Wee1 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.

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.

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.

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.

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).

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].

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

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

PKMYT1-IN-3 (compound 8ma) is a potent, selective inhibitor of PKMYT1, demonstrating an IC50 of 16.5 nM and exhibiting antitumor activity.

GSK-1520489A is an active PKMYT1 inhibitor.

NSC-37445 has anti-tumor activity, such as inhibits growth of bladder tumor cells in a nude mice model , prevents the recurrence and progression of non-muscle-invasive urothelial cell carcinoma. NSC-37445 can significantly reduce the expression of CDK1-inhibitory kinases, Myt1 and Wee1, and cause cyclin B1 protein accumulation leading to CDK1 activation in T24 cells. 3. Flavokawain A (Flavokavain A) may exert anti-inflammatory responses by suppressing LPS-induced expression of pro-inflammatory mediators via blockage of NF-κB-AP-1-JNK p38 MAPK signaling pathways in the murine macrophages.

SR-1277 is a potent, highly selective and ATP-competitive CK1δ ε inhibitor with IC50 values of 49 nM and 260 nM, respectively.CK1δ plays a crucial role in regulating Wee1 activity at the G2 M cell-cycle interface, and exhibits significant antiproliferative activity against a variety of cancer cells.