S49076 is a novel, potent inhibitor of MET, AXL/MER, and FGFR1/2/3 with IC50 values below 20 nM.
KW-2449 is a multi-targeted kinase inhibitor of FLT3, ABL, ABLT315I and Aurora kinase with IC50s of 6.6, 14, 4 and 48 nM, respectively.
Metadoxine blocks adipocyte differentiation in association with inhibition of the protein kinase A-cAMP response element binding protein (PKA-CREB) pathway.
Aristolactam A IIIa (Sch 546909) is an aristolactam-type alkaloid that can be isolated from Glycosmis chlorosperma. Aristolactam A IIIa is a DYRK1A Inhibitor. Aristolactam A IIIa inhibits platelet aggregation induced by arachidonic acid (AA), collagen and platelet-activating factor (PAF). Aristolactam A IIIa has strong cytotoxic effect on HeLa cells[1].
Namilumab (AMG203) is a human IgG1 monoclonal antibody that binds with high affinity to the GM-CSF ligand, potently neutralizing GM-CSF. Namilumab can be used for the research of rheumatoid arthritis[1].
ALK-IN-6 (compound 11) is an orally bioavailable inhibitor of anaplastic lymphoma kinase (ALK), with IC50 values of 71 nM, 18.72 nM and 36.81 nM for ALK wild, ALK F1196M and ALK F1174L, respectively[1].
AG 538 is a potent, competitive inhibitor of IGF-1 receptor kinase, with an IC50 of 400 nM[1].
AZD8601 is an mRNA designed to produce vascular endothelial growth factor A (VEGF-A). AZD8601 accelerates diabetic wound healing[1][2].
Dyrk1A-IN-5 (compound 5j) is a potent and selective DYRK1A inhibitor, with an IC50 of 6 nM. Dyrk1A-IN-5 dose-dependently reduces the phosphorylation of Thr434 in SF3B1, with an IC50 of 0.5 μM. Dyrk1A-IN-5 inhibits phosphorylation of tau at Thr212, with an IC50 of 2.1 μM. Dyrk1A-IN-5 can be used for Down syndrome research[1].
Saracatinib (AZD0530) is a potent Src family inhibitor with IC50s of 2.7 to 11 nM for c-Src, Lck, c-YES, Lyn, Fyn, Fgr, and Blk and shows high selectivity over other tyrosine kinases.
HP1142 is a potent and selective inhibitor of FLT3 receptor tyrosine kinase (FLT3/ITD mutation). HP1142 is a benzoimidazole scaffold-based compound. HP1142 has the potential for the research of FLT3/ITD leukemia[1].
BCR-ABL-IN-1 is an inhibitor of BCR-ABL tyrosine kinase, with a pIC50 of 6.46, and may be used in the research of chronic myelogenous leukemia.
BI-1622 is an orally active, potent and highly selective HER2 (ERBB2) inhibitor, with an IC50 of 7 nM. BI-1622 shows greater than 25-fold selectivity over EGFR. BI-1622 shows high antitumor efficacy in vivo in xenograft mouse tumor models with engineered H2170 and PC9 cells and had a favorable drug metabolism and pharmacokinetics profile[1].
G-749 is a novel FLT3 inhibitor that showed potent and sustained inhibition of the FLT3 wild type and mutants with IC50s of 0.4/0.6/3.5/7.5 nM for Wt Flt3/D835Y/MV4-11/Molm-14 respectively.IC50 value: 0.4/0.6/3.5/7.5 nM(Wt Flt3/D835Y/MV4-11/Molm-14) [1]Target: Flt3 inhibitorG-749 showed potent and sustained inhibition of the FLT3 wild type and mutants including FLT3-ITD, FLT3-D835Y, FLT3-ITD/N676D, and FLT3-ITD/F691L in cellular assays. G-749 retained its inhibitory potency in various drug-resistance milieus such as patient plasma, FLT3 ligand surge, and stromal protection. Furthermore, it displayed potent antileukemic activity in bone marrow blasts from AML patients regardless of FLT3 mutation status, including those with little or only minor responses to AC220 or PKC412. Oral administration of G-749 yielded complete tumor regression and increased life span in animal models.
BTK-IN-11 is a potent inhibitor of BTK. BTK plays an important role in signaling mediated by B cell antigen receptor (BCR) and Fcγreceptor (FcγR) in B cells and myeloid cells, respectively. BTK-IN-11 has the potential for the research of related diseases, especially autoimmune diseases, inflammatory diseases or cancer (extracted from patent WO2022063101A1, compound Z2)[1].
BTK-IN-18 is a potent, reversible BTK inhibitor with an IC50 of 0.002 µM. BTK-IN-18 inhibits both CD69 and CD86 in vivo[1].
AZM475271 is a potent and selective Src kinase inhibitor with IC50 of 5 nM; no inhibitory activity on Flt3, KDR, Tie-2.IC50 value: 5 nM [1]Target: Src inhibitorin vitro: AZM475271 demonstrated strong dose-dependent inhibition of Src tyrosine kinase activity in the L3.6pl human pancreatic carcinoma cell line. Maximum reduction of Src kinase activity was observed after incubation for 4 hours with ≥5 μmol/L. The IC50 concentration of AZM475271 to inhibit the phosphorylation of c-src, lck, and c-yes was 0.01, 0.03, and 0.08 μmol/L, respectively, in comparison with an IC50 of 0.7 μmol/L AZM475271 to inhibit KDR [2].in vivo: Tumors appeared to be palpable at day 14 after tumor cell injection in all animals except mice treated with both AZM475271 and gemcitabine, in which the earliest possible palpation of the tumors was at day 17 after tumor cell injection. Treatment with gemcitabine or AZM475271 alone did not significantly change animal weight [2].
Chloropyramine hydrochloride is a histamine receptor H1 antagonist which can also inhibit the biochemical function of VEGFR-3 and FAK.
Chimaphilin is an IGF-1R inhibitor (IC50: 0.086 μM). Chimaphilin has antifungal, antioxidant and anticancer activities. Chimaphilin inhibits the growth of both drug-sensitive and drug-resistant osteosarcoma cell lines. Chimaphilin can induce cancer cell apoptosis. Chimaphilin is a main component of pyrola[1][2].
YH-306 is a candidate drug in preventing growth and metastasis of colorectal cancer by modulating FAK signalling pathway.
Leucettine L41 is a potent inhibitor of dual-specificity tyrosine phosphorylation-regulated kinase 1A (DYRK1A), DYRK2, CDC-like kinase 1 (CLK1), and CLK3 (IC50s = 0.04, 0.035, 0.015, and 4.5 µM, respectively)[1]. Leucettine L41 prevents lipid peroxidation and the accumulation of reactive oxygen species (ROS) induced by Aβ25-35 in the hippocampus in a mouse model of Alzheimer’s disease-like toxicity. Leucettine L41 also prevents memory deficits induced by Aβ25-35 in the same model[2].
CZC-8004 is a pan-kinase inhibitor and binds a range of tyrosine kinases, including ABL kinase.
EGFR-IN-26 is a EGFR inhibitor extracted from patent WO2019162323A1 compound I-028. EGFR-IN-26 can be used for the research of cancer[1].
GW2580 is an orally bioavailable inhibitor of c-Fms kinase which completely inhibits human cFMS kinase in vitro at 0.06 μM.
Antitumor agent-57 (Compound 3o) is an NQO1-directed antitumor agent. Antitumor agent-57 inhibits tumor cell growth, triggers ROS generation and induces cell apoptosis[1].
D-(+)-Sorbose, an active enantiomer of D-Sorbose, which inhibits disaccharidase activity and demonstrates suppressive action on postprandial blood levels of glucose and insulin in the rat. D-sorbose acts as a sweetener may contribute to the prevention of lifestyle-related diseases, such as type 2 diabetes mellitus[1].
Trastuzumab deruxtecan (DS-8201a) is an anti-human epidermal growth factor receptor 2 (HER2) antibody-drug conjugate (ADC). Trastuzumab deruxtecan is composed of a humanized anti-HER2 antibody, an enzymatically cleavable peptide-linker, and a topoisomerase I inhibitor. Trastuzumab deruxtecan can be used for the research of HER2-positive breast cancer and gastric cancer[1][2].
HKI-357 is an irreversible dual inhibitor of EGFR and ERBB2 with IC50s of 34 nM and 33 nM, respectively. HKI-357 suppresses EGFR autophosphorylation (at Y1068), and AKT and MAPK phosphorylation[1].
Sp-8-CPT-cAMPS, a cAMP analog, is a potent and selective activator of the cAMP-dependent protein kinas A (PKA I and PKA II). Sp-8-CPT-cAMPS selects site A of RI compares to site A of RII by 153-fold and site B of RII compares to site B of RI by 59-fold[1][2].
Malvidin-3-galactoside chloride, an anthocyanin monomer, induces hepatocellular carcinoma (HCC) cells cycle arrest and apoptosis. Malvidin-3-galactoside chloride inhibits the production and accumulation of ROS. Malvidin-3-galactoside chloride has anti-tumor function[1].