TrxR2-IN-1 is a thioredoxin reductase 2 (TrxR2) inhibitor with an IC50 value of 0.83 μM. TrxR2-IN-1 accumulates in mitochondria, impairs mitochondrial function and membrane potential, increases reactive oxygen species (ROS) levels, activates ASK1-mediated caspase-dependent apoptosis (apoptosis), induces G2/M cell cycle arrest, and inhibits cancer cell migration. TrxR2-IN-1 can be used in the research of hepatocellular carcinoma.

SSTR3 Agonist-1 (Compound EX 38) is an orally active SSTR3 agonist, with an EC50 of 0.14 nM. SSTR3 Agonist-1 reduces the kidney cystic index. SSTR3 Agonist-1 can be used in the research of autosomal dominant polycystic kidney disease.

GRK5-IN-5 (Compound 4a) is a selective G protein-coupled receptor (GPCR) kinase 5 (GRK5) inhibitor with an IC50 of 0.03 μM. GRK5-IN-5 shows IC50 values of 2.2 and 0.036 μM for GRK2 and GRK6. GRK5-IN-5 has potent anti-myocardial hypertrophy activity and also inhibits the proliferation of non-myocardial cells. GRK5-IN-5 can inhibit the abnormal upregulation of hypertrophy marker genes Nppa and Nppb, thus blocking pathological myocardial remodeling. GRK5-IN-5 can be used for the research of cardiac hypertrophy.

DCAF11 ligand-Linker Conjugate 1 is a conjugate of a DCAF11 ligand and a linker. DCAF11 ligand-Linker Conjugate 1 can be used for the synthesis of PROTAC LGF308.

5-CNAC disodium is an orally active enhancer of absorption, with no pharmacological activity on its own. 5-CNAC disodium can significantly enhance the absorption efficiency of the drug (such as Salmon calcitonin) when administered together with it in the gastrointestinal tract. 5-CNAC disodium binds reversibly and non-covalently to peptide drugs, protecting them from degradation by gastrointestinal enzymes, increasing their lipid solubility, promoting passive transcellular absorption, and not damaging the integrity of the intestinal epithelium. 5-CNAC disodium can be used in the research of adjuvants for orally administered peptide agents.

i-AZD1775 (TFA) is an immobilizable analogue of AZD1775. i-AZD1775 (TFA) retains the ability to inhibit WEE1 in vitro. i-AZD1775 (TFA) can be studied in anticancer research.

PD-166285 is a PKMYT1 inhibitor, with an IC50 value of 17 nM. PD166285 shows strong antiproliferative effects against CCNE1-amplified OVCAR3 cells (IC50 = 0.14 μM) and HCC1569 cells (IC50 = 0.21 μM). PD166285 induces apoptosis and arrests CCNE1-amplified HCC1569 cells at the G1/S phase of the cell cycle. PD166285 can be used for the research of PKMYT1-targeted therapies for CCNE1-amplified cancers.

ZN-c3 is an orally active, highly potent and selective Wee1 inhibitor (IC50=3.9 nM). ZN-c3 can be used for the research of cancer.

Debio 0123 (Debio0123) is a potent, orally available, and highly selective Wee1 kinase inhibitor with IC50 of 0.8 nM, Ki of 0.1 nM.Debio 0123 is highly selective to Wee1 on 465 selected kinases in a cellfree system, does not inhibit Plk1 and Plk2, as also reported in recent publications for AZD1775.Debio 0123 exhibits in vitro growth inhibition activity in a broad number of human cancer cell lines (IC50= 0.109 to 7.08 uM).Debio 0123 prevent CDC2 / Cdk1 phosphorylation, induces γH2AX and enhances phosphorylation of histone H3.Debio 0123 induces apoptosis through mitotic catastrophe following cell cycle progression despite accumulation of unrepaired DNA damage both in vitro and in vivo.

MK-1775 is a potent and selective Wee1 inhibitor with IC50 of 5.2 nM.

Pomalidomide-C3-adavosertib is a rapid and selective Wee1 degrader (IC50=3.58 nM). Pomalidomide-C3-adavosertib shows anti-cancer cell proliferation activity, and induces apoptosis.

LEB-03-146 is a WEE1 DUBTAC (deubiquitinase-targeting chimera) linking AZD1775 (Adavosertib) to the OTUB1 recruiter EN523 through a PEG2 linker. LEB-03-146 shows significant WEE1 stabilization in HEP3B hepatoma cancer cells.

Wee1 Inhibitor II is a potent, selective, ATP-binding site-targeting inhibitor of Wee1 with IC50 of 59 nM, 590-fold selectivity over the related checkpoint kinase Chk1 (IC50=35 uM).