Catalog No.
Product Name
Application
Product Information
Citations
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EGFR, PKA,PKC inhibitor
Daphnetin is a coumarin analog that acts as an inhibitor of several protein kinases. It inhibits EGFR kinase (IC50 = 7.67 μM), PKA (IC50 = 9.33 μM), and PKC (IC50 = 25 μM), in vitro. The inhibition of EGFR kinase by daphnetin was competitive to ATP and non-competitive to the peptide substrate. Also acts as a potent antioxidant and anti-malarial agent. -
IGF-1R inhibitor
GSK1904529A selectively inhibits IGF-IR and IR with IC(50)s of 27 and 25 nmol/L, respectively. -
c-Met inhibitor
c-Met inhibitor JNJ-38877605 selectively binds to c-Met, thereby inhibiting c-Met phosphorylation and disrupting c-Met signal transduction pathways. -
HER2 inhibitor
Lapatinib is a dual tyrosine kinase inhibitor which interrupts the HER2 growth receptor pathway. -
c-Met inhibitor
MGCD265 is a multitargeted tyrosine kinase inhibitor that binds to and inhibits the phosphorylation of several RTKs, including the c-Met receptor (HGFR); the Tek/Tie-2 receptor; VEGFR types 1, 2, and 3; and MST1R. -
VEGFR inhibitor
Motesanib, also known as AMG-706, is an orally administered multikinase inhibitor that selectively targets VEGF receptors, platelet-derived growth factor receptors, and Kit receptors. -
HER2/ErbB2 inhibitor
Mubritinib (TAK 165) is a potent EGFR and p34cdc2 inhibitor with IC50 of 6 nM and 0.2 μM, respectively. Mubritinib(TAK 165) also inhibits p33cdk2 and p33cdk5. -
EGFR inhibitor
PD153035 is an extremely potent and specific inhibitor of the tyrosine kinase activity of EGFR. -
c-Met Inhibitor
PF-04217903 is a novel c-Met/hepatocyte growth factor receptor tyrosine kinase inhibitors. -
c-Met Inhibitor
PHA665752 is a small-molecule inhibitor of c-Met/HGF/SF signaling. -
Syk Inhibitor
R406 is an orally available spleen tyrosine kinase inhibitor with an IC50 of 41 nM. -
RAF/VEGFR Inhibitor
RAF265 (CHIR-265) is an oral, highly selective RAF and VEGFR kinase inhibitor, which is to control or normalize VEGFR-2 along with the inhibition of B-raf and c-Raf mutation to prevent cancers. -
RAF/VEGFR Inhibitor
Raf265 derivative is a derivative of Raf265 that is an oral, highly selective RAF and VEGFR kinase inhibitor with IC50 of of 5 to 10 μM. -
FLT3 Inhibitor
Tandutinib (MLN518) inhibits the autophosphorylation of FLT3, c-KIT and PDGF receptor tyrosine kinases, thereby inhibiting cellular proliferation and inducing apoptosis. -
p38 MAPK inhibitor
Pexmetinib is a potent inhibitor of cytokine synthesis, via the dual inhibition of p38 mitogen-activated protein kinase (MAPK), and Tie2/Tek receptor tyrosine kinase. -
VEGFR-2 inhibitor
Telatinib (BAY 57-9352) is an orally available, small-molecule inhibitor of vascular endothelial growth factor receptors 2 and 3 (VEGFR-2/-3) and platelet-derived growth factor receptor β tyrosine kinases. -
Tie2 kinase inhibitor
Tie2 kinase inhibitor is a potent and selective Tie2 inhibitor with IC50 of 0.25 μM. -
HER2 Inhibitor
ARRY-380 is an ErbB-2 inhibitor that selectively binds to and inhibits the phosphorylation of ErbB-2, resulting in growth inhibition and death of ErbB-2-expressing tumor cells. -
CDK Inhibitor
PHA-848125 (Milciclib) is an orally bioavailable inhibitor of CDKs and TRKA with potential antineoplastic activity. -
EGFR, HER2 and VEGFR inhibitor
XL647 is an orally bioavailable small-molecule RTK inhibitor that binds to and inhibits several tyrosine receptor kinases that play major roles in tumor cell proliferation and tumor vascularization, including EGFR, HER2, ERBB2, VEGFR and EphB4. -
JAK2/FLT3 inhibitor
TG-101348 is an orally bioavailable, ATP-competitive and selective inhibitor of Janus-associated kinase 2 with potential antineoplastic activity. - GIP (1-39) (Gastric inhibitory peptide (1-39) (porcine)) is an insulinotropic peptide that stimulats insulin secretion from rat pancreatic islets. GIP (1-39) at 100 nM was able to significantly increase intracellular Ca2+ concentration ([Ca2+]i), and capable of enhancing exocytosis.
- Insulin (human) is a polypeptide hormone that regulates the level of glucose.
- GIP (3-42), human acts as a glucose-dependent insulinotropic polypeptide (GIP) receptor antagonist, moderating the insulin secreting and metabolic actions of GIP in vivo.
- Gastric Inhibitory Peptide, porcine is a glucose-dependent insulinotropic polypeptide, is a 42 amino acid intestinal hormone with effects on fat and glucose metabolism.
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FGFR3 inhibitor
VSPPLTLGQLLS is a small peptide FGFR3 inhibitor, peptide P3, inhibits FGFR3 phosphorylation. VSPPLTLGQLLS inhibits 9-cisRA-induced tracheal lymphangiogenesis and blocks lymphatic endothelial cell (LEC) proliferation, migration, and tubule formation. - [D-Ala2]-GIP (human) is a GIP receptor agonist. [D-Ala2]-GIP (human) improves glucose tolerance. [D-Ala2]-GIP (human) shows neuroprotective activity in MPTP-induced Parkinson's disease model. [D-Ala2]-GIP (human) also improves cognitive function and hippocampal synaptic plasticity in obese diabetic rats. [D-Ala2]-GIP (human) can be used for research of type 2 diabetes, Parkinson's disease, etc
- Insulin receptor (1142-1153), pTyr1150 is a biological active peptide. (Peptide used as insulin receptor tyrosine kinase substrate.)
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multi-kinase inhibitor
Multi-kinase inhibitor 1 is a potent multi-kinase inhibitor. Multi-kinase inhibitor 1 has the potential for diseases or disorders associated with abnormal or deregulated tyrosine kinase activity, particularly diseases associated with the activity of PDGF-R, c-Kit and Bcr-abl. -
SU-4313 is a small-molecule modulator of protein tyrosine kinases (PTKs). It inhibits multiple receptor tyrosine kinases with reported IC₅₀ values of 14.5 μM (PDGFR), 18.8 μM (FLK-1/VEGFR2), 11 μM (EGFR), 16.9 μM (HER2 kinase), and 8.0 μM (IGF-1R).
Through its multi-kinase inhibitory profile, SU-4313 modulates tyrosine kinase–mediated signal transduction pathways involved in the regulation of cell proliferation and growth. It is therefore commonly used as a research tool for investigating aberrant receptor tyrosine kinase signaling and proliferation-associated pathways.
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FLT3 inhibitor
5'-Fluoroindirubinoxime (5'-FIO, compound 13), an Indirubin derivative, is a potent FLT3 inhibitor, with an IC50 of 15 nM.
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IRAK1 Degrader
JNJ-1013 is a selective degrader of IRAK1, demonstrating potent efficacy with IC50 values of 72 nM for IRAK1, 443 nM for IRAK4, and 1071 nM for VHL. This compound induces apoptosis and promotes the cleavage of PARP, signaling significant pro-apoptotic activity. Additionally, JNJ-1013 effectively reduces the expression of IRAK1, phosphorylated IKBα, and phosphorylated STAT3 (Tyr705), making it a valuable tool for research in inflammatory pathways and therapeutic interventions targeting IRAK1. -
PROTAC ALK Degrader
TL13-12 is a selective PROTAC degrader targeting anaplastic lymphoma kinase (ALK), exhibiting an IC50 of 0.69 nM for ALK inhibition. In addition to its primary action, TL13-12 induces degradation of several other kinases, including Aurora A (IC50 = 13.5 nM), FER (IC50 = 5.74 nM), PTK2 (IC50 = 18.4 nM), and RPS6KA1 (IC50 = 65 nM). This compound is designed through the conjugation of TAE684 and the Cereblon ligand derived from Pomalidomide, making it a valuable tool for studying kinase biology and developing targeted therapies. -
PROTAC IRAK Degrader
Zomiradomide is an orally bioavailable PROTAC degrader targeting IRAK4, with a DC50 of 6 nM, which effectively inhibits the NF-κB signaling pathway. In addition to its suppression of IRAK4, Zomiradomide functions as a molecular glue, facilitating the degradation of Ikaros with a DC50 of 1 nM and consequently activating the type I IFN signaling pathway. This dual action positions Zomiradomide as a valuable tool in research focused on immune modulation and inflammatory responses.
