Fmoc-Val-Ala-PAB-PNP is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs).

Novel mc (maleimidocaproyl) linker plus MMAD (Monomethylauristatin D) to be used for prepare antibodies conjugates via cysteine-capped mechanism

Val-cit-PAB-OH is a peptide prodrug linker.

SN34960 is a small molecule Perforin inhibitor, inhibits perforin-induced lysis of Jurkat T-lymphoma cells with IC50 of 6.65 uM, shows suboptimal physicochemical properties and toxicity toward the natural killer (NK) cells that secrete perforin in vivo.

Gingerenone A is a Nrf2-Gpx4 activator with anti-breast-cancer properties. Gingerenone A results a delayed G2/M in cancer cells, following oxidative stress and senescence responses. Gingerenone A also alleviates ferroptosis in secondary liver injury (SLI) in dextran sodium sulfate (DSS)-induced colitis mice. Gingerenone A can be isolated from Zingiber officinale.

5-HT3 antagonist 4 is a 5-HT3 receptor (5HT3R) antagonist. 5-HT3 antagonist 4 prevents diabetes-induced depressive phenotypes in mice.

BAPTA is a selective chelator for calcium. BAPTA, as calcium indicator, has high selectivity against magnesium and calcium. BAPTA is widely used as an intracellular buffer for investigating the effects of Ca2+ release from intracellular stores or influx via Ca2+-permeable channels in the plasma membrane. BAPTA can also inhibit phospholipase C activity independently of their role as Ca2+ chelators.

DVR-01 is a HBV inhibitor with EC50 values of 1.7 and 1.6 μM in AML12HBV10 and HepDES19 cells, respectively. DVR-01 shows antiviral activity against drug-resistant HBV mutants with EC50s of 2.403-3.273 μM. DVR-01 can be used for the research of HBV infection and related diseases.

JNJ10191584 (VUF6002) is an orally active and selective histamine H4 receptor antagonist with a Ki value of 26 nM. JNJ10191584 shows 540-fold selectivity to H4 receptor over H3 receptor with a Ki value of 14.1 μM. JNJ10191584 inhibits chemotaxis of eosinophils and mast cells with IC50 values of 530 nM and 138 nM, respectively.

SRI 6409-94 is an orally active Ro 13-6298 analogue that is teratogenic. SRI 6409-94 serves as a molecular tool to study the effect of the three-dimensional configuration of retinol on teratogenic activity.

UNC1021 is a selective L3MBTL3 inhibitor with an IC50 of 0.048 μM.

Oct4 inducer-1 (compound OAC-3) is a potent Oct4 activator. Oct4 inducer-1 activates Oct4 and Nanog promoters and enhances induced pluripotent stem cells (iPSC) formation. Oct4 inducer-1 facilitates the reprogramming of cells by enhancing efficiency and shortening the reprogramming time.

Tucidinostat (Chidamide, HBI-8000, CS055) is a novel histone deacetylase (HDAC) inhibitor with IC50 of 95/160/67/733/78/432 nM for HDAC1/2/3/8/10/11, respectively; shows no activity against Class IIa HDAC4/4/7/9 and HDAC6; demonstrates significant and broad spectrum in vitro and in vivo antitumor activity, induces G1 arrest, ROS-dependent apoptosis and differentiation in human leukaemia cells.

RGT1383 is a novel GLP-1R agonist, an analog of PF-06882961.

SW203668 is a potent, tumor-specific inhibitor of stearoyl CoA desaturase (SCD) with better bioavailability than SW208108.

Gilteritinib (ASP2215) hemifumarate is a potent and ATP-competitive FLT3/AXL inhibitor with IC50 of 0.29 nM/0.73 nM, respectively.

Capmatinib, also known as INCB28060 and INC280, is an orally bioavailable inhibitor of the proto-oncogene c-Met with potential antineoplastic activity. c-Met inhibitor INC280 selectively binds to c-Met, thereby inhibiting c-Met phosphorylation and disrupting c-Met signal transduction pathways. This may induce cell death in tumor cells overexpressing c-Met protein or expressing constitutively activated c-Met protein. Capmatinib was approved in 2020.

Tepotinib (EMD1214063, MSC2156119) is a potent, specific and ATP-competitive inhibitor of MET (HGFR) with IC50 of 23 nM for MET WT autophosphorylation and 2.2-42.6 nM for M1268T, Y1248H, H1112Y, L1213V, H1112L, V1110I, V1206L, and V1238I MET-mutated varia

DSF-102 (DSF102) is a small molecule EGFR inhibitor that interacts with the extracellular domain (ECD) of EGFR, inhibits the interaction with the EGF instead of blocking the intracellular kinase activity, shows inhibition of EGFR dimerization with IC50 of

Sotorasib racemate (Compound A) is an orally active racemate of Sotorasib, a covalent inhibitor of KRAS G12C mutant which induces adaptive feedback activation of MAPK pathway. Sotorasib racemate also exerts inhibitor activity against KRAS G12C induced cancer and can be applied to cancer research.

AMG-510 is a specific covalent inhibitor of K-RAS(G12C) with potential antineoplastic activity.

HRO761 is a potent, selective, allosteric WRN inhibitor with IC50 of 100 nM (ATPase assay) and GI50 of 40 nM (SW48 cells), respectively. HRO761 binds at the interface of the D1 and D2 helicase domains, locking WRN in an inactive conformation.

ARV-471 is a best-in-class, orally active estrogen receptor (ER) PROTAC degrader. ARV-471 is developed for the research of breast cancer.

NBCoV2 is a highly potent small molecule viral fusion inhibitor with potential pan-Coronavirus activity (SARS-CoV IC50=13.8 nM, SARS-CoV-2 IC50=22.8 nM, MERS-CoV IC50=77 nM, cell-based single-cycle assays). NBCoV2 also has potent antiviral activity against all mutant pseudoviruses carrying single-, double-, or triple-mutations featured in the B.1.1.7 UK, B.1.351 RSA, and B.1.617.2 Delta variants (IC50=30-80 nM). NBCoV2 completely preventing the induction of any virus-induced CPE (IC100=1.25 uM, SARS-CoV-2 (US_WA-1/2020)). NBCoV2 bind to the S2 subdomain of the SARS-CoV-2 trimer, thus, inhibits the fusion of CoVs with the cell membran, and is specific for the SARS-CoV-2 S protein.

Auranofin, also known as Ridaura and SKF-39162, is an oral chrysotherapeutic agent for the treatment of rheumatoid arthritis. Auranofin's exact mechanism of action is unknown, but it is believed to act via immunological mechanisms and alteration of lysosomal enzyme activity. Auranofin's efficacy is slightly less than that of injected gold salts, but it is better tolerated, and side effects which occur are potentially less serious.

GLPG3970 (compound 88) is a first-in-class SIK2/SIK3 inhibitor. GLPG3970 can be used for the research of inflammation and autoimmune disease.

TYA-018 (TYA018) is a potent, isoform-selective inhibitor of HDAC6 with IC50 of 10 nM, inhibits tubulin acetylation (Ac-Tubulin) with EC50 of 120 nM in cell-based assay in induced pluripotent stem cell-derived cardiomyocytes (iPSC-CMs).

ACT-1016-0707 is a potent, selective, and orally active lysophosphatidic acid receptor subtype 1 receptor (LPA1 receptor, LPAR1) antagonist with IC50 of 3.1 nM, highly selective over LPAR2 or LPAR3.

Nivasorexant is a potent orexin receptor antagonist.

IL-17A inhibitor 1 (example 24) is a IL-17A inhibitor, with IC50 values of <9.45 nM and 9.3 nM in alphalisa assay and HT-29 cells.