Cancer Targeted Therapy

CRBN ligand-353 is an E3 ubiquitin ligase cereblon (CRBN) ligand used to recruit the cereblon protein. CRBN ligand-353 can be linked to a target protein ligand via a linker to form a PROTAC.

Cenisertib (AS-703569) benzoate is an ATP-competitive multi-kinase inhibitor that blocks the activity of Aurora-kinase-A/B, ABL1, AKT, STAT5 and FLT3. Cenisertib benzoate induces major growth-inhibitory effects by blocking the activity of several different molecular targets in neoplastic mast cells (MC). Cenisertib benzoate inhibits tumor growth in xenograft models of pancreatic, breast, colon, ovarian, and lung tumors and leukemia.

DMU2139 (Standard) is the analytical standard of DMU2139 (HY-101285). This product is intended for research and analytical applications. DMU2139 is a potent and specific CYP1B1 inhibitor, with IC50s of 9 nM and 795 nM for CYP1B1 and CYP1A1, respectively.

tert-Butyl (3-aminopropoxy)carbamate is a PROTAC linker that can be used in the synthesis of PROTACs.

CRBN ligand-780 is an E3 ubiquitin ligase cereblon (CRBN) ligand used to recruit the cereblon protein. CRBN ligand-780 can be linked to a target protein ligand via a linker to form a PROTAC.

680C91 (Standard) is the analytical standard of 680C91 (HY-108681). This product is intended for research and analytical applications. 680C91 is an orally active, selective tryptophan 2,3-dioxygenase (TDO) inhibitor with a K_i of 51 nM. TDO is the key enzyme of tryptophan catabolism. 680C91 can be used for the research of cancer immunotherapy and Alzheimer’s Disease.

Epristeride (Standard) is the analytical standard of Epristeride. This product is intended for research and analytical applications. Epristeride (ONO-9302) is a selective, specific and orally active uncompetitive inhibitor of human steroid 5 alpha-reductase isoform 2. Epristeride has inhibitory effects for SR isoenzymes types 2 with K_i value of 0.7-2 nM. Epristeride can be used for the research of prostatic hyperplasia and acne.

SC79 (Standard) is the analytical standard of SC79 (HY-18749). This product is intended for research and analytical applications. SC79, a unique specific and BBB permeable Akt activator, activates Akt in the cytosol and inhibits Akt membrane translocation. SC79 specifically binds to the PH domain of Akt.

Trilostane (Standard) is the analytical standard of Trilostane. This product is intended for research and analytical applications. Trilostane (Win 24540) is a competitive and orally active 3-β-hydroxysteroiddehydrogenase (3β-HSD) inhibitor. Trilostane is a synthetic nonhormonal steroid. Trilostane can be used for the research of breast cancer and prostate cancer.

Sepantronium bromide (Standard) is the analytical standard of Sepantronium bromide (HY-10194). This product is intended for research and analytical applications. Sepantronium bromide (YM-155) is a survivin inhibitor with an IC₅₀ of 0.54 nM.

tert-Butyl (3-(chlorosulfonyl)propyl)carbamate is a PROTAC linker that can be used in the synthesis of PROTACs.

Sivelestat (Standard) is the analytical standard of Sivelestat. This product is intended for research and analytical applications. Sivelestat (EI546) is a competitive inhibitor of human neutrophil elastase, with an IC50 of 44 nM and a Ki of 200 nM. Sivelestat (EI546) has the potential for the study of acute lung injury/acute respiratory distress syndrome or disseminated intravascular coagulation in COVID-19.

tert-Butyl 4-(4-aminophenoxy)piperidine-1-carboxylate is a PROTAC linker that can be used in the synthesis of PROTACs.

PEG3-bis(carbonochloridic acid) is a PROTAC linker that can be used in the synthesis of PROTACs.

(R)-Boc-4-NH2-3,3-difluoropiperidin is a PROTAC linker that can be used in the synthesis of PROTACs.

ZYJ-34c is an orally active and potent histone deacetylase inhibitor (HDACi) with IC₅₀s of 0.056 μM and 0.146 μM for HDAC6 and HDAC8, respectively. ZYJ-34c causes G1 phase arrest in low concentration. ZYJ-34c has antiproliferative activities. ZYJ-34c exhibits antitumor potency in MDA-MB-231 and HCT116 xenograft models and possesses antimetastatic potential in a mouse hepatoma-22 (H22) pulmonary metastasis model.

FPTI is a SYT-SSX1 fusion protein modulator with selective cytotoxicity in SYT-SSX1-positive synovial sarcoma cells. FPTI down-regulates SYT-SSX1 expression and modulates its downstream target genes. FPTI induces apoptosis in synovial sarcoma cells. FPTI can be used for the research of synovial sarcoma.

Trifluridine (Standard) is the analytical standard of Trifluridine. This product is intended for research and analytical applications. Trifluridine (Trifluorothymidine) is an irreversible and orally active thymidylate synthase inhibitor, and thereby suppressing DNA synthesis. Trifluridine is an antiviral molecule used for research of HSV, rhabdovirus and orthopoxvirus infection. Trifluridine induces cell apoptosis and autophagy. Trifluridine is also an anticancer agent used in studies of metastatic colorectal cancer, gastrointestinal tumors.

Melanocin A is a Melanin biosynthesis inhibitor. Melanocin A inhibits the biosynthesis of melanin and tyrosinase (IC₅₀ is 9.0 nM, MIC is 0.9 μM). Melanocin A also has antioxidant effect.

AKT inhibitor VIII (Standard) is the analytical standard of AKT inhibitor VIII (HY-10355). This product is intended for research and analytical applications. AKT inhibitor VIII (AKTi-1/2) is a cell-permeable quinoxaline compound that has been shown to potently, selectively, allosterically, and reversibly inhibit Akt1, Akt2, and Akt3 activity with IC₅₀s of 58 nM, 210 nM, and 2119 nM, respectively.