H-Arg-Gly-Tyr-Ala-Leu-Gly-OH is a competitive and CAMP dependent protein kinase inhibitor[1].
RU-301 is a pan-TAM receptor inhibitor, exerts pan-TAM inhibitory activity by binding at the interface between Gas6 and the Ig1 domain of the respective TAMs with Kd and IC50 values of 12 μM and 10 μM, respectively[1].
HER2-IN-7 is a potent inhibitor of HER2. Deregulation of ErbB family signalling modulates proliferation, invasion, metastasis, angiogenesis, and tumour cell survival. HER2-IN-7 has the potential for the research of diseases associated ErbBs (especially HER2), including cancer (extracted from patent WO2019214634A1, compound 23)[1].
Mavrilimumab (CAM 3001) is a monoclonal antibody that binds to the α subunit of the granulocyte-macrophage colony stimulating factor (GM-CSF) receptor and blocks intracellular signalling downstream of GM-CSF. GM-CSF might be a mediator of the hyperactive inflammatory response associated with respiratory failure and death[1].
Evobrutinib is an inhibitor of Bruton's tyrosin kinase (Btk) inhibitor extracted from patent US20140162983 example 0174.
ALK-IN-13 is an ALK inhibitor, extracted from patent US20130225528A1, example 19[1].
ALK-IN-27 (compound 1) is a potent ALK inhibitor. ALK-IN-27 shows antitumor activity. ALK-IN-27 has an IC50 of 2.7 nM for Ba/F3 CLIP1-LTK cell[1].
GDC-0834 (S-enantiomer) is the S-enantiomer of GDC-0834. GDC-0834 is a potent and selective BTK inhibitor.
PQ401, a selective insulin-like growth factor-1 receptor blocker, is a novel diarylurea compound that inhibits IGF1R autophosphorylation with IC50 < 1 uM.IC50 Value: 12 uM (inhibited autophosphorylation of the IGF-IR in cultured human MCF-7 cells) [1]Target: IGF1Rin vitro: PQ401 inhibited autophosphorylation of the IGF-IR in cultured human MCF-7 cells with an IC50 of 12 micromol/L and autophosphorylation of the isolated kinase domain of the IGF-IR with an IC50 <1 micromol/L. In addition,PQ401 inhibited the growth of cultured breast cancer cells in serum at 10 micromol/L. PQ401 was even more effective at inhibiting IGF-I-stimulated growth of MCF-7 cells (IC50, 6 micromol/L) [1]. Twenty-four hours of treatment with 15 micromol/L PQ401 induced caspase-mediated apoptosis. Pretreatment with PQ401 before IGF-1 (10 ng in 0.5 μl), both administered to the POA 30 min apart, showed significant attenuation of the IGF-1-induced increase in core body temperature (p < 0.05). A similar attenuated hyperthermic response to IGF-1 by PQ401 pretreatment is observed when the temperature of the BAT is measured [3].in vivo: IGF1R inhibition by PQ401 exerted no significant effects on diabetic kidney disease parameters, arguing against a role for IGF-I in the pathogenesis of diabetic kidney disease. However, PQ401 affects normal kidneys, inducing renal hypertrophy as well as collagen and fat accumulation, with increased renal IGF-I mRNA, suggestive of a damage-regeneration process [2].Clinical trial: No Development Reported
Meleagrin is a roquefortine C-derived alkaloid produced by fungi of the genus Penicillium and has antimicrobial and anti-proliferative activities. Meleagrin is a class of FabI inhibitor. Meleagrin is a lead c-Met inhibitory entity useful for the control of c-Met-dependent metastatic and invasive breast malignancies[1][2][3].
Foretinib is a multi-target tyrosine kinase inhibitor with IC50s of 0.4 nM and 0.9 nM for Met and KDR.
PF-573228 is a potent and selective FAK inhibitor with IC50 of 4 nM for purified recombinant catalytic fragment of FAK.
BAY 61-3606 (dihydrochloride) is a potent, ATP-competitive, reversible, and highly selective inhibitor of Syk tyrosine kinase (IC50=10 nM) with no inhibitory effect on Btk, Fyn, Itk, Lyn, and Src.
Mutated EGFR-IN-3 (compound 3) is a potent, ATP-competitive and highly selective allosteric dibenzodiazepinone inhibitor of the EGFR(L858R/T790M) and EGFR(L858R/T790M/C797S) mutants with IC50 values of 12 nM and 13 nM, respectively[1].
CH6953755 is a potent, orally active and selective YES1 kinase (a member of the SRC family) inhibitor with an IC50 of 1.8 nM. CH6953755 inhibits YES1 kinase, leading to antitumor activity against YES1 Gene -amplified cancers in vitro and in vivo[1].
A-3 hydrochloride is a potent, cell-permeable, reversible, ATP-competitive non-selective antagonist of various kinases. It against PKA (Ki=4.3 µM), casein kinase II (Ki=5.1 µM) and myosin light chain kinase (MLCK) (Ki=7.4 µM). A-3 hydrochloride also inhibits PKC and casein kinase I with Ki values of 47 µM and 80 µM, respectively[1].
Dalmelitinib is an orally active selective c-Met kinase inhibitor (IC50: 2.9 nM) that binds to the ATP-binding region of c-Met. Dalmelitinib induces the phosphorylation of MET, partially or completely inhibits the phosphorylation of AKT and ERK. Dalmelitinib potently inhibits cancer cell (c-Met oncogene amplification) proliferation, and is used for the research of cancers like human non-small cell lung cancer (NSCLC)[1].
(E/Z)-AG490 ((E/Z)-Tyrphostin AG490) is a racemic compound of (E)-AG490 and (Z)-AG490 isomers. (E)-AG490 (HY-12000) is a tyrosine kinase inhibitor that inhibits EGFR, Stat-3 and JAK2/3.
Fascaplysin is an antimicrobial and cytotoxic red pigment, that can come from the marine sponge (Fascaplysinopsis sp.). Fascaplysin has been synthesized in seven steps from indole (65% yield). Fascaplysin can induces apoptosis and autophagy in human leukemia HL-60 cells. Fascaplysin shows anti-tumor activity[1][2].
Dacomitinib (PF-00299804) hydrate is an orally active, irreversible pan-ErbB inhibitor. Dacomitinib hydrate can be used in the research of cancers such as metastatic non-small cell lung cancer (NSCLC)[1].
Hu7691 free base is an orally active, selective Akt inhibitor with IC50s of 4.0 nM, 97.5 nM, 28 nM for Akt1, Akt2 and Akt3, respectively. Hu7691 free base inhibits tumor growth and enables decrease of cutaneous toxicity in mice[1].
ALK-IN-1 is a potent and selective active inhibitor of anaplastic lymphoma kinase(ALK), Patent US20140066406 A1.
Harmine Hydrochloride (Telepathine Hydrochloride) is a natural dual-specificity tyrosine phosphorylation-regulated kinase (DYRK) inhibitor with anticancer and anti-inflammatory activities. Harmine has a high affinity of 5-HT2A serotonin receptor, with an Ki of 397 nM[1].
FLT3-IN-10 (compound 7c) is a potent inhibitor of FMS-like tyrosine kinase 3 (FLT3). FLT3-IN-10 has the potential for the treatment of FLT3-mutated acute myeloid leukemia (AML)[1].
Luxeptinib (CG-806) is an orally active, reversible, first-in-class, non-covalent and potent pan-FLT3/pan-BTK inhibitor. Luxeptinib induces cell cycle arrest, apoptosis or autophagy in acute myeloid leukemia cells[1][2][3][4].
ALK inhibitor 1 is a novel and selective inhibitor for the ALK kinase.
Mifanertinib dimaleate is a potent tyrosine kinase inhibitor with antineoplastic activity[1].
TRK-IN-18 is a potent inhibitor of TRK. Tropomyosin-related kinases (Trks) are a family of receptor tyrosine kinases activated by neurotrophins, a group of soluble growth factors including Nerve Growth Factor (NGF), Brain-Derived Neurotrophic Factor (BDNF) and Neurotrophin-3 (NT-3) and Neurotrophin-4/5 (NT-4/5). TRK-IN-18 has the potential for the research of cancer diseases (extracted from patent WO2021148805A1, compound 7)[1].
BTK-IN-25 (compound 71) is a potent inhibitor of BTK, and inhibits BTK(C481S) with an IC50 value of 0.77 nM. BTK-IN-25 inhibits BTK in DOHH2 cells with an IC50 value of 1 nM[1].
pan-HER-IN-1 (Compound C5) is an irreversible, orally active pan-HER inhibitor with IC50 values of 0.38, 1.6, 2.2 and 3.5 nM against EGFR, HER4, EGFRT790M/L858R and HER2, respectively. pan-HER-IN-1 induces apoptosis and shows antitumor activities[1].