autophosphorylation kinase

CEP-37440 is an effective and specific Dual FAK/ALK inhibitor with IC50s of 120 nM(ALK cellular in 75% human plasma) and 2.3 nM (FAK).

Quizartinib (AC220) is an inhibitor of FLT3 (Kd: 1.6 nM) and demonstrates high selectivity for FLT3 when tested against a panel of 227 additional kinases.

Prexasertib (LY2606368) is a selective checkpoint kinase 1 (CHK1) inhibitor (Ki 0.9 nM, IC50<1 nM). Prexasertib causes double-stranded DNA breaks and replication mutations, leading to apoptosis. Prexasertib has antitumor activity.

HNMPA is a membrane impermeable inhibitor of insulin receptor tyrosine kinase. HNMPA inhibits tyrosine and serine autophosphorylation by the human insulin receptor. HNMPA exhibits no effect on cyclic AMP-dependent protein kinase or protein kinase C activities.

CGP77675 (ZINC1488120) is a potent and selective inhibitor of Src family kinase with IC50s of 5-20 and 40 nM for the phosphorylation of peptide substrates and autophosphorylation of purified Src. CGP77675 exhibits anticancer activity.

AKN-028 is an orally active and potent FLT3 tyrosine kinase inhibitor ( IC 50 = 6 nM). AKN-028 causes dose-dependent inhibition of FLT3 autophosphorylation.

LY2457546 is a highly potent, orally bioavailable multi-target anti-angiogenic tyrosine kinase inhibitor. It shows strong inhibitory activity against multiple targets including VEGFR2, PDGFRβ, FLT-3, Tie-2, and Eph family receptors, and is applied in cancer research such as leukemia.

RG13022 (Tyrphostin RG13022) is a tyrosine kinase inhibitor; inhibits the autophosphorylation reaction of the EGF receptor (IC50: 4 μM).

(Rac)-SAR131675 is an effective and specific VEGFR-3 inhibitor. It inhibited VEGFR-3 tyrosine kinase activity (IC50: 20 nmol/L) and VEGFR-3 autophosphorylation (IC50: 45 nmol/L) in HEK cells, respectively. SAR131675 is highly specific for VEGFR-3 versus 107 receptors, enzymes, ion channels, and 65 kinases. SAR131675 is a highly specific VEGFR-3-TK inhibitor with significant antitumoral and antimetastatic activities in vivo through inhibition of lymphangiogenesis and TAM invasion.

3-Hydroxy Midostaurin (CGP 52421), a PKC412 metabolite, inhibits FMS-like tyrosine kinase-3 (FLT3) autophosphorylation with IC50 values of approximately 132 nM in culture medium and 9.8 μM in plasma. Although less selective, it shows greater cytotoxicity compared to PKC412[1].

AG 1295, a selective inhibitor of platelet-derived growth factor receptor (PDGFR) tyrosine-kinase, effectively halts PDGFR autophosphorylation without impacting the autophosphorylation of the EGF receptor[1][2][3][4].

Lestaurtinib (CEP 701) is an orally available and selective inhibitor of FMS-like tyrosine kinase-3 (FLT3, IC50: 0.9 nM), which inhibits FLT3 autophosphorylation in vitro.Lestaurtinib promotes the expression of c-MYC, inhibits the phosphorylation of RPTKs, and has high affinity for TrkA and JAK2. Lestaurtinib promotes c-MYC expression, inhibits phosphorylation of RPTKs, has a high affinity for TrkA and JAK2, induces apoptosis and cell growth arrest, and can be used to study leukemia.

PKR-IN-C16 is a specific protein kinase (PKR) inhibitor. PKR-IN-C16 is able to inhibit the autophosphorylation of PKR and unlock the translation blockade induced by PKR in primary neuronal cultures.PKR-IN-C16 binds the ATP-binding site of PKR and blocks autophosphorylation with an IC50 value of 186-210 nM. PKR-IN-C16 protects human neuroblastoma cells against cell damage triggered by tunicamycin-mediated endoplasmic reticulum stress.

Tandutinib (CT53518) (MLN518, CT53518), an effective FLT3 antagonist (IC50: 0.22 μM), can also inhibit c-Kit and PDGFR, 15-20 fold higher potency for FLT3 versus CSF-1R and >100-fold selectivity for the same target versus FGFR, EGFR, and KDR.

GNE-9605 is a highly effective, specifical, and brain-penetrant LRRK2 inhibitor (IC50: 19 nM).

3-Hydroxy Midostaurin-D5 is a deuterium-labeled 3-Hydroxy Midostaurin (T12610L) which is a metabolite of PKC412. PKC412 effectively inhibits FMS-like tyrosine kinase-3 (FLT3) autophosphorylation (IC50s: 132 nM and 9.8 μM in culture medium and plasma).

(R)-LW-Srci-8 is a selective covalent inhibitor of c-Src, with an IC50 of 35.83 nM, that disrupts c-Src autophosphorylation by targeting the autophosphorylation site (Y419) of the c-Src kinase.

Ifebemtinib (tosylate) (BI-853520 (tosylate); IN-10018 (tosylate)) is a highly selective PTK2 kinase inhibitor with anti-tumor properties. It inhibits FAK autophosphorylation in prostate cancer cells and suppresses spheroid formation and in situ tumor growth in vivo. Ifebemtinib (tosylate) is applicable in cancer research, including studies on solid tumors, breast cancer, and malignant pleural mesothelioma.

AURKA-IN-3 (Compound AL8) is an irreversible covalent inhibitor of Aurora kinase A (AURKA) with an IC50 of 23.0 nM. It inhibits the activation of AURKA-mediated cAMP and phospholipase C (PLC) signaling pathways, as well as reduces the autophosphorylation of AURKA. AURKA-IN-3 is a potential candidate for research into malignancies associated with high AURKA expression, such as leukemia and lymphoma.

Sunitinib (SU 11248) glucuronate is a multi-target receptor tyrosine kinase inhibitor with IC50 values of 80 nM for VEGFR2 and 2 nM for PDGFRβ. As an ATP-competitive inhibitor, it effectively suppresses Ire1α phosphorylation by inhibiting autophosphorylation and subsequent RNase activation.

LY3295668 (AK-01) erbumine is a highly selective, orally active inhibitor of Aurora-A kinase, with Ki values of 0.8 nM for AurA and 1038 nM for AurB. It effectively suppresses AurA autophosphorylation, inducing mitotic arrest and apoptosis (apoptosis), while preventing polyploidy associated with AurB inhibition. LY3295668 erbumine is applicable for studying small cell lung cancer.

c-Kit-IN-13 (Compound I) is an inhibitor of the c-kit kinase. It suppresses the autophosphorylation of the wild-type c-kit, with an IC50 of 0.3 nM for pKIT. Additionally, c-Kit-IN-13 inhibits Exon 11 KIT with an IC50 of 0.9 nM. This compound can be utilized in research on mast cell-mediated diseases such as urticaria.

Cot-IN-5 (compound 1) is a potent ATP-competitive inhibitor of cancer Osaka thyroid (COT). It effectively blocks the autophosphorylation of the COT kinase.

PF-6274484, a high affinity, irreversible covalent inhibitor of EGFR kinase with Ki of 0.14 nM, inhibits the autophosphorylation of wild-type EGFR in A549 cells and EGFRL858R/T790M in H1975 cells with IC50 of 5.8 nM and 6.6 nM, respectively.