PRN694 is a highly selective and potent covalent inhibitor of T cell kinase (ITK) and resting lymphocyte kinase (RLK) with IC50s of 0.3 and 1.4 nM, respectively.
Ceritinib (LDK378) is a potent and specific ALK inhibitor with an IC50 of 0.2 nM.
Insulin levels modulator could be used to treat diabetes.
(R)-Larotrectinib is a potent TRK inhibitor with an IC50 value of 28.5 nM for TrkA. (R)-Larotrectinib can be used for researching cancer, inflammatory and certain infectious diseases[1]
iHCK-37 (ASN05260065) is a potent and specific Hck inhibitor with a Ki value of 0.22 μM. iHCK-37 blocks HIV-1 viral replication with an EC50 value of 12.9 μM. iHCK-37 is used for chronic myeloid leukemia (CML) research[1].
FGFR2-IN-2 (Compound 38) is a selective FGFR2 inhibitor with IC50s of 389, 29, and 758 nM for FGFR1, FGFR2, and FGFR3, respectively[1].
R112 is an ATP-competitive inhibitor of Syk kinase with a Ki of 96 nM. R112 inhibits Syk kinase activity with an IC50 of 226 nM. IC50 value: 226 nM [1]Target: Sykin vitro: R112 blocks leukotriene C4 production and all proinflammatory cytokines tested. Its onset of action was immediate, and the inhibition was reversible. R112 is able to completely inhibit all three IgE-induced mast cell functions: degranulation, lipid mediator production, and cytokine production. R112 potently, completely, and rapidly abrogated all mast cell activation cascades triggered by IgE receptor cross-linking.[1]
Osimertinib mesylate (AZD-9291 mesylate) is an irreversible and mutant selective EGFR inhibitor with IC50s of 12 and 1 nM against EGFRL858R and EGFRL858R/T790M, respectively.
AMG-458 is a potent, selective and orally bioavailable c-Met inhibitor, with Ki values of 1.2 nM and 2.0 nM for human and mouse c-Met, respectively[1].
Timtraxanib (AVI-3207) is a selective VEGF-2 inhibitor. Timtraxanib can be used for the research of senile macular degeneration[1].
Bezuclastinib (CGT9486; PLX 9486) is a potent inhibitor of c-kit and c-kit D816V (0.0001
Lorlatinib is a potent, dual ALK/ROS1 inhibitor, with Kis of 0.02 nM, 0.07 nM, and 0.7 nM for ROS1, wild type ALK, and ALK-L1196M, respectively.
TL4830031 (compound 8i), a quinolone antibiotic derivatives, is a potent Axl inhibitor with an IC50 value of 26 nM. TL4830031 inhibits the phosphorylation of Axl. TL4830031 inhibits cell invasion and migration. TL4830031 can be used for cancer research[1].
Btk inhibitor 1 R enantiomer is a pyrazolo[3,4-d]pyrimidine derivative as a Btk kinase inhibitor.IC50 value:Target: BtkFrom PCT Int. Appl. (2012), WO 2012158843 A2 20121122.
Surfen dihydrochloride is a potent HS (heparan sulfate) antagonist. Surfen binds to glycosaminoglycans. Surfen neutralizes the anticoagulant activity of both unfractionated and low molecular weight heparins. Surfen affects sulfation of heparin and inhibits degradation by heparin lyases. Surfen inhibits FGF2 binding and signaling. Surfen inhibits cell attachment, and virus infection[1].
CEP-11981(ESK981; BOL 303213X) is an orally active tyrosine kinase inhibitor (TKI), which can target TIE2, VEGFR1-3 and FGFR1, and has potential anti-tumor and anti-angiogenic effects[1].
ULK1-IN-2 (compound 3s) is a potent ULK1 inhibitor. ULK1-IN-2 shows highest cytotoxic effect against cancer cell lines, with IC50 of 1.94 μM in A549. ULK1-IN-2 can induce apoptosis and simultaneously block autophagy, and can be used to study NSCLC (Non-small cell lung cancer)[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].
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.
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].
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].
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].
ALK5-IN-7 is a potent inhibitor of ALK5. Transforming growth factor beta (TGF-β) is a multifunctional cytokine that is involved in regulating cell proliferation, differentiation and apoptosis through complex receptor signaling pathways on the cell surface in an autocrine, paracrine and endocrine manner. ALK5-IN-7 has the potential for the research of TGF-β-related diseases and conditions, including but not limited to tumors, fibrotic diseases, inflammatory diseases, autoimmune diseases, etc (extracted from patent WO2021129621A1, compound 4)[1].
Lavendustin A (RG-14355), isolated from Streptomyces Griseolavendus, is a potent, specific and ATP-competitive inhibitor of tyrosine kinase, with an IC50 of 11 ng/mL for EGFR-associated tyrosine kinase[1]. It suppresses VEGF-induced angiogenesis and blocks the induction of LTPGABA-A[2][3].
Rp-cAMPS, a cAMP analog, is a potent, competitive cAMP-induced activation of cAMP-dependent PKA I and II (Kis of 12.5 µM and 4.5 µM, respectively) antagonist. Rp-cAMPS is resistant to hydrolysis by phosphodiesterases[1][2][3][4][5][6].
Jaspamycin (7-CN-7-C-Ino) is a potent activator of PKA, binding to the R site (PKAR), with an EC50 of 6.5 nM and Kd of 8 nM in Trypanosoma brucei. Jaspamycin (7-CN-7-C-Ino) does not bind with purified human PKARIα. Anti-parasite activity[1].
Dovitinib (dilactic acid) is an orally active inhibitor of VEGF kinase. Dovitinib (dilactic acid) inhibits receptor tyrosine kinases (RTKs) involved in solid and hematologic cancers and tumor angiogenesis[1].
Resencatinib is a potent tyrosine kinase inhibitor with antineoplastic activity[1].