Cancer Targeted Therapy

E3 Ligase Ligand-linker Conjugate 135 is a conjugate of E3 ligase ligand and linker that serve as a key intermediate for the synthesis of complete PROTAC molecule pan-KRAS degrader 5 (HY-168678).

HBX 41108 (Standard) is the analytical standard of HBX 41108 (HY-101666). This product is intended for research and analytical applications. HBX 41108 is an inhibitor of ubiquitin-specific protease 7 (USP7) with an IC50 of 424 nM. HBX 41108 inhibits USP7-mediated p53 deubiquitination to stabilize p53 and inhibits cancer cell growth. BX 41108 can be used in cancer and diabetes research.

Mitoxantrone (dihydrochloride) (Standard) is the analytical standard of Mitoxantrone (dihydrochloride). This product is intended for research and analytical applications. Mitoxantrone dihydrochloride is a potent topoisomerase II inhibitor. Mitoxantrone dihydrochloride also inhibits protein kinase C (PKC) activity with an IC50 of 8.5 μM. Mitoxantrone dihydrochloride induces apoptosis of B-CLL (B-chronic lymphocytic leukaemia) cells. Mitoxantrone dihydrochloride shows antitumor activity. Mitoxantrone dihydrochloride also has anti-orthopoxvirus activity with EC50s of 0.25 μM and and 0.8 μM for cowpox and monkeypox, respectively.

DCZ3112 is a Hsp90/Cdc37 protein-protein interaction inhibitor, with a K_d value of 4.98 µM against human Hsp90. DCZ3112 binds to the N-terminal domain of Hsp90, disrupts the Hsp90-Cdc37 interaction, and does not inhibit the ATPase activity of Hsp90. DCZ3112 induces G1 phase cell cycle arrest, apoptosis, reduces the phosphorylation levels of AKT and ERK, and inhibits the proliferation of HER2-positive breast cancer cells. DCZ3112 can be used in breast cancer-related research.

BAY-1436032 (Standard) is the analytical standard of BAY-1436032 (HY-100020). This product is intended for research and analytical applications. BAY-1436032 is a novel pan-mutant isocitrate dehydrogenase 1 (IDH1) inhibitor.

L-Canavanine (sulfate) (Standard) is the analytical standard of L-Canavanine (sulfate). This product is intended for research and analytical applications. L-Canavanine sulfate is a selective inhibitor of inducible NO synthase.

20-Hydroxylucidenic acid E2 is a triterpenoid compound found in Ganoderma lucidum. It exhibits significant inhibitory effects on inflammation induced by TPA (HY-18739). Additionally, 20-Hydroxylucidenic acid E2 can suppress the expression of EBV early antigen induced by TPA (HY-18739), with a IC₅₀ of 290 mol ratio/32 pmol TPA (meaning that when the molar concentration of this compound is 290 times that of 32 pmol of TPA, it can inhibit 50% of EBV early antigen expression). Therefore, 20-Hydroxylucidenic acid E2 has potential applications in anti-inflammatory and anticancer research.

Di-tert-butyl decanedioate is a PROTAC linker that can be used in the synthesis of PROTACs.

CRBN ligand-313 is an E3 ubiquitin ligase cereblon (CRBN) ligand used to recruit the cereblon protein. CRBN ligand-313 can be linked to a target protein ligand via a linker to form a PROTAC.

4(3H) -quinazolinone is a fused nitrogen heterocyclic compound whose derivatives have a wide range of antimicrobial and antitumor activities.

VH 101 phenol-alkylC6-amine dihydrochloride is a functionalized von-Hippel-Lindau (VHL) protein-ligand that can be used for PROTAC synthesis.

PI(3,4)P2 (18:1) ammonium salt is a phosphatidylinositol 3 kinase (PI3K) activator. PI(3,4)P2 (18:1) ammonium salt is a polyphosphorylated phosphatidylinositol that promotes the activation of AKT (protein kinase B) by activating PI3K, which affects cell metabolism, growth and survival. PI(3,4)P2 (18:1) ammonium salt is also involved in regulating dynamic changes in the cytoskeleton, affecting cell morphology and movement. PI(3,4)P2 (18:1) ammonium salt can be used in research on the development of cancer, diabetes and cardiovascular disease.

ZSQ836 is an orally active dual covalent inhibitor of CDK12/CDK13, with an EC₅₀ value of 32 nM against CDK12. ZSQ836 can induce apoptosis and exhibit anticancer activity in vivo. ZSQ836 can be used in the study of ovarian cancer.

Thalidomide-NH-C2-alkyne contains an E3 ligase ligand with an alkyl linker, and a terminal alkyne. Thalidomide-NH-C2-alkyne is ready for conjugation to target proteins for PROTAC R&D.

4-(4-((tert-Butoxycarbonyl)amino)phenyl)butanoic acid is a PROTAC linker that can be used in the synthesis of PROTACs.

CRBN ligand-679 is an E3 ubiquitin ligase cereblon (CRBN) ligand used to recruit the cereblon protein. CRBN ligand-679 can be linked to a target protein ligand via a linker to form a PROTAC.

ARN5187 trihydrochloride (Standard) is the analytical standard of ARN5187 trihydrochloride (HY-103691A). This product is intended for research and analytical applications. ARN5187 trihydrochloride is a lysosomotropic REV-ERBβ ligand with a dual inhibitory activity toward REV-ERB-mediated transcriptional regulation and autophagy. ARN5187 trihydrochloride shows lysosomotropic potency and cytotoxicity. ARN5187 trihydrochloride induces apoptosis.

AT008 is an anti-GPCR monoclonal antibody that blocks the binding of chemokine ligands to its cell surface receptor CCR4. AT008 can be studied in research for certain haematological and solid cancers.

Importazole (Standard) is the analytical standard of Importazole (HY-101091). This product is intended for research and analytical applications. Importazole is a small molecule inhibitor of the nuclear transport receptor importin-β.

Rabeprazole-¹³C,d₃ (sodium) (LY307640-¹³C,d₃ (sodium)) is ¹³C labeled Rabeprazole (sodium). Rabeprazole sodium (LY307640 sodium) is a second-generation proton pump inhibitor (PPI) that irreversibly inactivates gastric H⁺/K⁺-ATPase. Rabeprazole sodium induces apoptosis. Rabeprazole sodium acts as an uridine nucleoside ribohydrolase (UNH) inhibitor with an IC₅₀ of 0.3 μM. Rabeprazole sodium can be used for the research of gastric ulcerations and gastroesophageal reflux.