wee1

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

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.

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].

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

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.

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.

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

DB0614 (Example 21) is a bifunctional compound designed for the targeted degradation of kinases, effectively breaking down a wide array of kinases including AAK1, AURKA, BMP2K, CAMKK1, CDK16, CML, CDK6, EIF2AK2, FER, GAK, LCK, LIMK2, MAP3KH, MAPK8, MAPK9, NEK9, PLK4, PTK2B, SIK2, STK17A, STK17B, ULK1, ULK3, and WEE1. This compound has potential applications in the research of diseases or disorders caused by aberrant kinase activity [1].

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].

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

FMF-06-098-1 is a multitargeted depressant capable of promoting the degradation of a wide array of kinases, including AAK1, ABL2, AURKA, AURKB, BUB1B, CDC7, CDK1, CDK12, CDK13, CDK2, CDK4, CDK6, CDK7, CDK9, CHEK1, CSNK1D, EPHA1, PAK, FGFR1, GAK, IRAK4, ITK, LIMK2, MAP4K2, MAP4K3, MAPK6, MAPK7, MARK4, MELK, PKN3, PLK4, PRKAA1, PTK2, PTK6, RPS6KA4, SGK2, STK35, TNK2, UHMK1, ULK1, and WEE1 [1].

LEB-03-144 is a WEE1 DUBTAC (deubiquitinase-targeting chimera) linking AZD1775 (Adavosertib) to the OTUB1 recruiter EN523 through a C3 alkyl linker. LEB-03-144 shows significant WEE1 stabilization in HEP3B hepatoma cancer cells [1] .

GUN94110 is a WEE1 kinase inhibitors useful in treatment of cancer and other proliferative diseases. GUN94110 was reported in WO 2019028008. This product has no formal name at the moment. For the convenience of communication, a temporary code name was therefore proposed according to MedKoo Chemical Nomenclature (see web page: https://www.medkoo.com/page/naming).

LEB-03-153 is a WEE1 DUBTAC (deubiquitinase-targeting chimera) linking AZD1775 (Adavosertib) to the OTUB1 recruiter EN523 through no linker [1] .

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).

CJM-061 is a Wee1 inhibitor.

LEB-03-145 is a WEE1 DUBTAC (deubiquitinase-targeting chimera) linking AZD1775 (Adavosertib) to the OTUB1 recruiter EN523 through a C5 alkyl linker [1] .

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

MK-1775 hemihydrate is a WEE1 inhibitor with potential antineoplastic sensitizing activity.

(E)-Flavokawain A, a novel chalcone from kava extract, induces apoptosis in bladder cancer cells by involvement of Bax protein-dependent and mitochondria-dependent apoptotic pathway and suppresses tumor growth in mice.