Teprasiran (QPI-1002) is a small interfering RNA that temporarily inhibits p53-mediated cell death that underlies acute kidney injury (AKI)[1].
icFSP1 is a potent ferroptosis suppressor protein-1 (FSP1) inhibitor. icFSP1 does not competitively inhibit FSP1 enzyme activity, but instead triggers subcellular relocalization of FSP1 from the membrane and FSP1 condensation before ferroptosis induction, in synergism with GPX4 inhibition[1].
BMS-202 is an inhibitor of the PD-1/PD-L1 protein/protein interaction with an IC50 of 18 nM.
(rac)-Exatecan Intermediate 1 is an isomer of Exatecan Intermediate 1 (HY-42487). Exatecan Intermediate 1 (compound 6) is an intermediate of Exatecan (HY-13631), a camptothecin-based anticancer agent. Exatecan inhibits tumor growth by interfering with the proliferation and division of tumor cells by interacting with DNA. Exatecan is primarily used in research into a variety of cancers including ovarian, lung and breast cancer[1][2].
PBRM1-BD2-IN-7 is a selective and cell-active polybromo-1 (PBRM1) bromodomain inhibitor. PBRM1-BD2-IN-7 has inhibitory activity for PBRM1-BD2 with an IC50 value of 0.29 μM. PBRM1-BD2-IN-7 can be used for the research of cancer[1].
Feladilimab (Anti-ICOS/CD278 Reference Antibody (feladilimab); GSK3359609) is humanized IgG4 anti-ICOS agonist monoclonal antibody. Feladilimab binds to ICOS-expressing T cells. Feladilimab has the potential for the research of cancer[1].
BIX02189 is a potent and selective MEK5 inhibitor with an IC50 of 1.5 nM. BIX02189 also inhibits ERK5 catalytic activity with an IC50 of 59 nM.
β-Glucuronide-dPBD-PEG5-NH2 is the β-glucuronide-linked pyrrolobenzodiazepine dimer, which binds to the prenylated antibody for synthesis of antibody-drug conjugate (ADC) cIRCR201-dPBD. β-glucuronide-linkage as a cleavable linker. β-Glucuronide-dPBD-PEG5-NH2, as a prodrug of cIRCR201-dPBD, reduces side effects[1].
Seviteronel (VT-464) racemate is the racemate form of Seviteronel (VT-464), which is a potent CYP17 lyase inhibitor(h-Lyase IC50=nM)inhibition.
Menin-MLL inhibitor 20 is an irreversible menin-MLL interaction inhibitor with antitumor activities (WO2020142557A1, compound 6)[1].
Tamarixin is flavonoid that isolated from Astragalus tanae Sosn that has hepatoprotective, antioxidant, anticancer, and antimicrobial activities[1].
MSC-4106 is an orally active and potent inhibitor of YAP/TAZ-TEAD. MSC-4106 inhibits TEAD1 or TEAD3 auto-palmitoylation and shows inhibitory effect on NCI-H226 tumor xenograft model[1].
HM43239 is an orally active and selective FLT3 inhibitor with IC50s of 1.1 nM, 1.8 nM and 1.0 nM for FLT3 WT, FLT3 internal tandem duplication (ITD) and FLT3 D835Y kinases, respectively. HM43239 inhibits the kinase activity of FLT3 as a reversible type I inhibitor and modulates p-STAT5, p-ERK, SYK, JAK1/2, and TAK1. HM43239 inhibits the proliferation and induces the apoptosis of leukemic cells[1][2][3].
AIM-100 is a small molecule inhibitor of Ack1 with an IC50 of 24 nM.IC50 value: 24 nM [3]Target: Ack1Ack1 inhibitor AIM-100 not only inhibited Ack1 activation but also suppressed AKT tyrosine phosphorylation, leading to cell cycle arrest in the G1 phase [1].The Ack1 inhibitor AIM-100 not only inhibited Ack1 activity but also was able to suppress AR Tyr(267) phosphorylation and its recruitment to the ATM enhancer. Notably, AIM-100 suppressed Ack1 mediated ATM expression and mitigated the growth of radioresistant CRPC tumors [2]. AIM-100, not only inhibited Ack1 activation but also able to suppress pTyr267-AR phosphorylation, binding of AR to PSA, NKX3.1, and TMPRSS2 promoters, and inhibit AR transcription activity [3].
Deruxtecan analog 2 (example 9 P3) is a Deruxtecan (HY-13631E) analog. Deruxtecan analog 2 is a drug-linker conjugate composed of Camptothecin (HY-16560) and a linker. Camptothecin (CPT) is a Topo I inhibitor with antineoplastic activity against colorectal, breast, lung and ovarian cancers. Deruxtecan analog 2 can be used for the preparation anti-FGFR2 ADC[1].
A66 is a highly specific and selective p110α inhibitor with an IC50 of 32 nM.
Neoisoliquiritigenin, isolated from Spatholobus suberectus, inhibits cell proliferation and induced cell apoptosis in breast cancer by directly binding to GRP78 to regulate the β-catenin pathway[1][2].
Cereblon inhibitor 1, an isoindoline derivative, is a cereblon E3 ubiquitin ligase modulating drug. Cereblon inhibitor 1 has the potential for cancer research[1].
CMK is a RSK2 kinase inhibitor which exhibits similar potency but less chemical stability compared with FMK.
SAFit2 is a novel, selective FK506-binding protein 51 (FKBP51) antagonist with a Ki of 6 nM and also enhances AKT2-AS160 binding.
WDR5 inhibitor 41 is a potent, selective and orally bioavailable WDR5 WIN-site inhibitor with TR-FRET Ki value of <0.02 nM, inhibits cell proliferation of MV4:11 and MOLM-13 with IC50 of 13 and 27 nM, respectively.WDR5 inhibitor 41 is well tolerated in mice by both iv and po dosing and showed no clinical sign of abnormalities suggesting an enhanced safetyprofile for the series.
Propargyl-O-C1-amido-PEG4-C2-NHS ester is a nonclaevable 4-unit PEG linker for antibody-drug-conjugation (ADC).
Tusamitamab ravtansine (SAR-408701) is a DM4 (HY-12454) anti-CEACAM5 antibody-drug conjugate (ADC). Tusamitamab ravtansine is composed of a humanized monoclonal antibody that binds carcinoembryonic antigen-related cell adhesion molecule-5 (CEACAM5) and a cytotoxic maytansinoid that selectively targets CEACAM5-expressing tumor cells[1].
Erythromycin gluceptate is a macrolide antibiotic produced by actinomycete Streptomyces erythreus with a broad spectrum of antimicrobial activity. Erythromycin gluceptate binds to bacterial 50S ribosomal subunits and inhibits RNA-dependent protein synthesis by blockage of transpeptidation and/or translocation reactions, without affecting synthesis of nucleic acid[1][2]. Erythromycin gluceptate also exhibits antitumor and neuroprotective effect in different fields of research[3][4].
Cancer-Targeting Compound 1 is used in the research of hormone-related cancer, extracted from patent WO 2008021331 A2.
L-NAME hydrochloride inhibits NOS with an IC50 of 70 μM. L-NAME is a precursor to NOS inhibitor L-NOARG which has an IC50 value of 1.4 μM.
mDPR-Val-Cit-PAB-MMAE consists the ADCs linker (mDPR-Val-Cit-PAB) and potent tubulin inhibitor (MMAE), mDPR-Val-Cit-PAB-MMAE is an antibody drug conjugate.
Azido-PEG6-alcohol is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1]. Azido-PEG6-alcohol is also a non-cleavable 6 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[2].
Cinchonine is a natural compound present in Cinchona bark. Cinchonine activates endoplasmic reticulum stress-induced apoptosis in human liver cancer cells[1].
A2AAR/HDAC-IN-1 (compound 14c) is an orally active, potent and balanced A2AAR/HDAC dual inhibitor, with a Ki of 163.5 nM for A2AAR and an IC50 of 145.3 nM for HDAC1. A2AAR/HDAC-IN-1 shows anticancer activity[1].