Fidasimtamab (IBI-315; BH2950) is a recombinant human IgG1 bispecific antibody that targets, binds and inhibits both HER2 and PD-1 and their downstream signalling pathways, and links PD-1 expressing T cells to HER2 expressing tumour cells. Fidasimtamab has potential immunosuppressive and antitumor activity[1].
E-7050 is a potent dual inhibitor of both c-Met and VEGFR2 kinases with IC50s of 14 and 16 nM, respectively.
Gastric Inhibitory Peptide, porcine is a glucose-dependent insulinotropic polypeptide, is a 42 amino acid intestinal hormone with effects on fat and glucose metabolism[1].
Osimertinib (AZD-9291) is an irreversible and mutant selective EGFR inhibitor with IC50s of 12 and 1 nM against EGFRL858R and EGFRL858R/T790M, respectively.
Axatilimab (SNDX-6352) is a humanized IgG4 antibody with high affinity to CSF-1R. Axatilimab can be used for the research of chronic graft versus host disease (cGVHD) and neoplastic diseases[1][2].
Scutellarin, a main active ingredient extracted from Erigeron breviscapus (Vant.) Hand-Mazz., has been wildly used to treat acute cerebral infarction and paralysis induced by cerebrovascular diseases.
Cenisertib (AS-703569) is a multi-kinase inhibitor that blocks the activity of Aurora-kinase-A/B, ABL1, AKT, STAT5 and FLT3. Cenisertib induces major growth-inhibitory effects by blocking the activity of several different molecular targets in neoplastic mast cells (MC)[1]. Cenisertib inhibits tumor growth in xenograft models of pancreatic, breast, colon, ovarian, and lung tumors and leukemia[2].
Ginsenoside Rg5 is the main component of Red ginseng. Ginsenoside blocks binding of IGF-1 to its receptor with an IC50 of ~90 nM. Ginsenoside Rg5 also inhibits the mRNA expression of COX-2 via suppression of the DNA binding activities of NF-κB p65.
ARQ 531 is a reversible non-covalent inhibitor of Bruton’s Tyrosine Kinase (BTK), with IC50s of 0.85 nM and 0.39 nM for WT-BTK and C481S-BTK, respectively.
Orniplabin (SMTP-7) is a low-molecular-weight compound that enhances plasminogen–fibrin binding, urokinase-catalyzed activation of plasminogen, and urokinase and plasminogen-mediated fibrin degradation. Orniplabin shows potential thrombolytic and anti-inflammatory effects. Orniplabin inhibits ROS[1][2].
TG101209 is a selective JAK2 inhibitor with IC50 of 6 nM, less potent to Flt3 and RET with IC50 of 25 nM and 17 nM, appr 30-fold selective for JAK2 than JAK3, and sensitive to JAK2V617F and MPLW515L/K mutations.
FAK-IN-7 (compound 5r) is a FAK inhibitor (IC50=11.72 µM). FAK-IN-7 has good anti-proliferative activity and can be used in cancer research[1].
TAK-659 is a highly potent, selective, reversible and orally available inhibitor of spleen tyrosine kinase (SYK) and fms related tyrosine kinase 3 (FLT3), with an IC50 of 3.2 nM for SYK. TAK-659 induces cell death in tumor cells but not in nontumor cells, and with potential for the treatment of chronic lymphocytic leukemia (CLL)[1][2][3][4].
Tyrphostin AG 112 is an EGFR phosphorylation inhibitor[1].
CNX-500 is a probe consisting of a covalent Btk inhibitor (CC-292) chemically linked to biotin. CNX-500 retains inhibitory activity against Btk (IC50 of 0.5 nM) and the ability to form a covalent bond with Btk. CNX-500 has low inhibitory effects on kinase epidermal growth factor receptor, and upstream Src-family kinases including Syk and Lyn[1].
TPX-0131 is a potent, selective, CNS-penetrant and orally active inhibitor of wild-type ALK (IC50 of 1.4 nM) and ALK-resistant mutation, e.g. G1202R (IC50 of 0.3 nM), L1196M (IC50 of 0.3 nM). TPX-0131 has strong antitumor activities[1].
Warangalone is an anti-malarial compound which can inhibit the growth of both strains of parasite 3D7 (chloroquine sensitive) and K1 (chloroquine resistant) with IC50s of 4.8 μg/mL and 3.7 μg/mL, respectively. Warangalone can also inhibit cyclic AMP-dependent protein kinase catalytic subunit (cAK) with an IC50 of 3.5 μM.
GSK1904529A is a selective inhibitor of IGF-1R and IR with IC50 of 27 nM and 25 nM, >100-fold more selective for IGF-1R/InsR than Akt1/2, Aurora A/B,B-Raf, CDK2, EGFR etc. IC50 value: 27/25 nM (IGF1R/IR) [1]Target: IGF1R/IRin vitro: GSK1904529A is a reversible, ATP-competitive inhibitor and has enzyme-inhibitor binding values against IGF-1R and IR with Ki of 1.6 nM and 1.3 nM, respectively. GSK1904529A potently inhibits the ligand-induced phosphorylation of IGF-1R and IR at concentrations above 0.01 μM, followed by blocking downstream signaling (AKT, IRS-1, and ERK). GSK1904529A potently inhibits NIH-3T3/LISN, TC-71, SK-N-MC, SK-ES RD-ES cells with IC50 of 60 nM, 35 nM, 43 nM, 61 nM and 62 nM, respectively. GSK1904529A also inhibits other multiple myeloma and Ewing's sarcoma cell lines including NCI-H929, MOLP-8, LP-1 and KMS-12-BM etc. GSK1904529A induces cell cycle arrest at the G1 phase in cell lines COLO 205, MCF-7, and NCI-H929, which are sensitive to GK1904529A [1].in vivo: GSK1904529A indicates 98% tumor growth inhibition in NIH-3T3/LISN tumor-bearing mice at a dose of 30 mg/kg (orally, twice-daily) and 75% in COLO 205 xenografts mice (once daily). Among HT29 and BxPC3 xenografts, GSK1904529A produces moderate tumor growth inhibition with no side effects at a dose of 30 mg/kg. Meanwhile, GSK1904529A shows minimal effects on blood glucose levels. GSK1904529A (~3.5 μM in blood) completely inhibits IGF-1R phosphorylation. GSK1904529A has been implicated in treatment of various IGF-1R-dependent tumors including prostate, colon, breast, pancreatic, ovarian, and sarcomas [1].
β-Nor-lapachone is a Candida glabrata antibiofilm agent. β-Nor-lapachone can stimulate ROS production, inhibits efflux activity, adhesion, biofilm formation and the metabolism of mature biofilms of Candida glabrata. β-Nor-lapachone has antifungal activity[1].
Axl-IN-11 (Example 1) is a potent AXL inhibitor. Axl-IN-11 can be used for the research of proliferative diseases, autoimmune diseases, allergic diseases, inflammatory diseases, transplant rejection, cancers, viral infectious diseases or other diseases of mammals[1].
Lapatinib (GW572016) is a potent EGFR and ErbB2 inhibitor with IC50s of 10.2 and 9.8 nM, respectively.
hVEGF-IN-2 (compound 19) is a selective VEGF (Flk-1) receptor tyrosine kinases (RTK) inhibitor with an IC50 value of 2.5 μM. hVEGF-IN-2 inhibits PDGF RTK activity with an IC50 value of 33.1 μM. hVEGF-IN-2 can be used for the development of RTK-specific drugs[1].
EGFR/HER2/CDK9-IN-3 (Compound 10) is a potent inhibitor of EGFR/HER2/CDK9 with IC50s of 191.08, 132.65, and 113.98 nM, respectively. EGFR/HER2/CDK9-IN-3 exhibits remarkable antitumor activity[1].
BPIQ-I (PD 159121) is a potent and ATP-competitive EGFR tyrosine kinase inhibitor.. BPIQ-I shows anti-proliferative actively[1][2].
Trk-IN-20 is a kind of 3-vinylindazole derivatives. Trk-IN-20 suppresses Trk kinases functions by phosphorylation inhibition of TrkA/B/C with IC50 values of 1.6 nM, 2.9 nM and 2.0 nM, respectively[1].
Mobocertinib is a potent epidermal growth factor receptor (EGFR) inhibitor and an antineoplastic agent, extracted from patent WO2019222093A1, compound A[1][2].
Zabedosertib (BAY 1834845) is a IRAK4 inhibitor with immunomodulatory potential. IRAK4 is a protein kinase involved in signaling innate immune responses from Toll-like receptors[1].
H-8 (dihydrochloride) is a cell-permeable, reversible and ATP-competitive PKA inhibitor[1].
VEGFR-2-IN-23 (compound 11b) is a potent and selective VEGFR-2 inhibitor with an IC50 value of 0.34 nM. VEGFR-2-IN-23 shows antitumor activity. VEGFR-2-IN-23 induces apoptosis and cell cycle arrest at G1 phase[1].
Lyn peptide inhibitor is a potent and cell-permeable inhibitor of Lyn-coupled IL-5 receptor signaling pathway, while keeping other signals intact. Lyn peptide inhibitor blocks Lyn activation and inhibits the binding of Lyn tyrosine kinase to βc subunit of IL-3/GM-CSF/IL-5 receptors. Lyn peptide inhibitor can be used for study of asthma, allergic, and other eosinophilic disorders[1].