Protein Tyrosine Kinases

Buflomedil is a vasoactive agent used to treat peripheral vascular disease.

Lapatinib is a dual tyrosine kinase inhibitor which interrupts the HER2 growth receptor pathway. Lapatinib is a potent EGFR and ErbB2 inhibitor with IC50 of 10.8 and 9.2 nM in cell-free assays, respectively. Lapatinib induces ferroptosis and autophagic cell death.

MK-2461, a novel multitargeted kinase inhibitor, preferentially inhibits the activated c-Met receptor.

Radicicol is a potent inhibitor of Hsp90, SRC, and Cox-2

CP-547632 is a novel, potent vascular endothelial growth factor receptor-2 tyrosine kinase inhibitor

ASP3026 is a novel and selective inhibitor for the ALK kinase. ASP3026 potently inhibited ALK kinase activity and was more selective than crizotinib in a Tyr-kinase panel.

ALK-IN-1, an analog of AP26113, is an orally-available, potent, and selective inhibitor of ALK with a potency of 0.62 nM against wild-type and activity against a wide range of mutants, including the crizotinib-resistant L1196M line.

AG-17 is an inhibitor of EGF receptor kinase with an IC50 value of 460 μM in the human epidermoid carcinoma cell line A431.

PQ 401 is a cell-permeable phenylquinolinyl-urea compound that inhibits IGF-1R autophosphorylation.

ZM 323881 is a potent and selective inhibitor of the kinase activity of the human vascular endothelial growth factor receptor 2 (VEGFR2/KDR).

ZM 306416 is a VEGF receptor tyrosine kinase inhibitor that inhibits KDR (IC50 = 100 nM) and Flt (IC50 = 2 uM) tyrosine kinases.

GW2580 is a small-molecule, ATP-competitive inhibitor of cFMS kinase.

TG-02 is a novel small molecule potent CDK/JAK2/FLT3 inhibitor.

(-)-Gallocatechin possesses free radical scavenging ability. It inhibits the growth and adherence of P. gingivalis onto the buccal epithelial cells.

Sorafenib N-Oxide is a metabolite of Sorafenib, a potent Raf kinase inhibitor.

AZ7550 is an active metabolite of AZD9291 and inhibits the activity of IGF1R with an IC50 of 1.6 μM.

(-)-Catechin gallate is an antioxidant constituent of green tea. At uM concentrations, inhibits VEGF-induced tyrosine phosphorylation.

Thalidomide fluoride (Cereblon ligand 4) is the Thalidomide-based Cereblon ligand used in the recruitment of CRBN protein. Thalidomide fluoride (Cereblon ligand 4) can be connected to the ligand for IRAK4 protein by a linker to form PROTAC IRAK4 degrader-1.

Picropodophyllin (AXL1717) is the first targeted oral small-molecule IGF-1 receptor inhibitor with no effect on the insulin receptor.

KX1-004 is a potent small molecule inhibitor of Src-PTK as a potential protective drug for NIHL.

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.

Src Inhibitor 1 is a potent and selective dual site Src tyrosine kinase inhibitor with IC50 values of 44 nM for Src and 88nM for Lck.

FIIN-2 is an irreversible inhibitor of FGFR1-4 with IC50 values of 3.1, 4.3, 27, and 45 nM, respectively.

A83-01 is a selective inhibitor of the transforming growth factor-beta type I receptor ALK5, the Nodal receptor ALK4, and the nodal receptor ALK7

MLR 1023 is a selective allosteric activator of Lyn kinase (EC50 = 63 nM)

Go6976 is a potent PKC inhibitor with IC50 of 7.9 nM, 2.3 nM, and 6.2 nM for PKC (Rat brain), PKCα, and PKCβ1, respectively. Also a potent inhibitor of JAK2 and Flt3.

CHMFL-ABL/KIT-155 (CHMFL-ABL-KIT-155; compound 34) is a highly potent and orally active type II ABL/c-KIT dual kinase inhibitor.

TCS 359 is a potent inhibitor of FLT3 receptor tyrosine kinase (IC50 = 42 nM) that displays selectivity over a range of other kinases.

SU 5416 is an inhibitor of vascular endothelial growth factor receptor (VEGFR) that also inhibits other tyrosine kinases KIT, MET, FLT3 and RET.

Butein is a plant polyphenol that acts as a specific protein tyrosine kinase inhibitor.

SU1498 is a selective inhibitor of the VEGFR2; inhibits Flk-1 with an IC50 of value of 700 nM.

GENZ-882706 is a potent colony stimulating factor-1 receptor (CSF-1R) Inhibitor extracted from patent WO 2017015267A1.

Tyrosine kinase-IN-1 is a multi-targeted tyrosine kinase inhibitor with IC50s of 4, 20, 4, 2 nM for KDR, Flt-1, FGFR1 and PDGFRα, respectively.

c-met-IN-1 (compound 16) is a potent and selective c-Met inhibitor, with IC50 of 1.1 nM, with antitumor activity.

ALW-II-41-27 is a novel Eph receptor tyrosine kinase inhibitor.

CHMFL-EGFR-202 is a potent, irreversible inhibitor of epidermal growth factor receptor (EGFR) mutant kinase, with IC50s of 5.3 nM and 8.3 nM for drug-resistant mutant EGFR T790M and WT EGFR kinases, respectively.

LY2801653 is a potent, orally bioavailable, small-molecule inhibitor of c-MET kinase(Ki= 2 nM).

EGFR-IN-2 is a a noncovalent, irreversible, mutant-selective second generation EGFR inhibitor.

PKC 412 is a broad spectrum protein kinase inhibitor. Inhibits conventional PKC isoforms α/β/γ, PDFRβ, VEGFR2, Syk, Flk-1, Flt3, Cdk1/B, PKA, c-Kit, c-Fgr, c-Src, VEGFR1 and EGFR. Displays potent antitumor activity.

AZ 23 is a potent and selective tyrosine kinase Trk inhibitor with IC50 to 2 and 8 nM for TrkA and TrkB respectively

JNJ-28312141 is an orally active CSF1R inhibitor (Colony-stimulating factor-1 receptor, CRF1R) and also a FLT3 inhibitor. CSF1R is expressed by many tumors and is a growth factor for macrophages and mediates osteoclast differentiation. JNJ-28312141 represents a new agent with potential therapeutic activity in acute myeloid leukemia and in settings where CSF-1-dependent macrophages and osteoclasts contribute to tumor growth and skeletal events.

NVP-BAW2881 is a potent and selective VEGFR inhibitor (vascular endothelial growth factor receptor tyrosine kinase inhibitor) with activity to inhibit chronic and acute skin inflammation.

Pacritinib, also known as SB1518, is an orally bioavailable inhibitor of Janus kinase 2 (JAK2) and the JAK2 mutant JAK2V617F with potential antineoplastic activity. Pacritinib competes with JAK2 for ATP binding, which may result in inhibition of JAK2 activation, inhibition of the JAK-STAT signaling pathway, and so caspase-dependent apoptosis.

PP2 is a selective inhibitor of Src-family tyrosine kinases. Inhibits p56lck and p59fynT (IC50 values are 4 and 5 nM respectively). Displays > 10000-fold selectivity over ZAP-70 and JAK2. Moderately inhibits CSK (IC50 = 0.73 μM).

PP1 is a potent inhibitor of Src-family tyrosine kinases. Inhibits p56lck and p59fynT (IC50 values are 5 and 6 nM respectively). Displays > 8000-fold selectivity over ZAP-70 and JAK2. Also moderately inhibits p38, CSK, PDGF receptors, RET-derived oncoproteins, c-Kit and Bcr-Abl

PD168393 is a potent, cell-permeable, irreversible inhibitor of EGFR with IC50 value of 700 pM.

DMH-1 is a selective inhibitor of the bone morphogenic protein (BMP) ALK2 receptor (IC50 = 108 nM).

CGP-52411 is a slective inhibitor of the epidermal growth factor receptor (EGFR) (IC50 = 0.3 μM in vitro). Also inhibits and reverses the formation of Aβ42 fibers associated with Alzheimer's disease.

ARRY-543 is a novel, oral ErbB family inhibitor that, unlike approved ErbB inhibitors, targets all members of the ErbB family, including ErbB3, either directly or indirectly, and has potential advantages in treating tumors that signal through multiple ErbB family members.

DDR-TRK-1 is a selective Discoidin Domain Receptor 1 (DDR1) inhibitor, with an IC50 value of 9.4 nM. DDR-TRK-1 also inhibits TRK family.