Src Inhibitor

AD57 is an orally active multikinase inhibitor, inhibits RET, BRAF, S6K and Src, with greatly reduces mTOR activity.

GSK2646264 (Compound 44) is a potent and selective spleen tyrosine kinase (SYK) inhibitor with a pIC₅₀ of 7.1. GSK2646264 also inhibits other kinases with pIC₅₀ values of 5.4, 5.4, 5.3, 5, 4.5, <4.6 and <4.3 against LCK, LRRK2, GSK3β, JAK2, VEGFR2, Aurora B and Aurora A, respectively. GSK2646264 is penetrable into the epidermis and dermis of the skin.

Notoginsenoside Fe (Notoginseng triterpenes; Ginsenoside Mb) is a saponin with anti-obesity and anti-neuroblastoma activities. Notoginsenoside Fe can be isolated from leaves of Panax notoginseng. Notoginsenoside Fe specifically activates paraventricular nucleus neurons in the hypothalamus, effectively reducing body weight, improving fasting blood glucose and protecting liver function by decreasing food intake, increasing resting metabolic rate and enhancing energy expenditure. Notoginsenoside Fe also inhibits the c-Src signaling pathway, blocks the proliferation and viability of human neuroblastoma cells, while improving mitochondrial dysfunction and alleviating apoptosis. Notoginsenoside Fe can be used in studies related to diet-induced obesity and neuroblastoma.

Lyn peptide inhibitor (YGYRLRRKWEEKIPNP-NH₂) is a potent, cell-permeable Lyn kinase inhibitor that inhibits Lyn-coupled signaling pathways associated with the IL-5 receptor while preserving the integrity of other signals. Lyn peptide inhibitor blocks the activation of Lyn and inhibits the binding of Lyn tyrosine kinase to the βc subunit of the IL-3/GM-CSF/IL-5 receptor. Lyn peptide inhibitor can be used in the research of eosinophilic diseases such as asthma and allergy.

Larixol is an fMLP inhibitor and also inhibits Src kinase, ERK1/2, p38 and AKT phosphorylation signals in immune regulation. Larixol can interfere with the interaction between the βγ subunit of the fMLP receptor Gi protein and its downstream molecules, thereby inhibiting fMLP-induced respiratory burst. Larixol inhibits fMLP (0.1 μM)-induced superoxide anion production (IC₅₀: 1.98 μM), cathepsin G release (IC₅₀: 2.76 μM), and chemotaxis. Larixol improves neutrophil hyperactivation and reduces inflammation or tissue damage. A series of Larixol derivatives were found to have inhibitory effects on FSGS-related TRPC6 functional mutants.

Hck-IN-1 (compound B9), a diphenylpyrazolo compound, is a selective Nef-dependent Hck inhibitor with IC₅₀s of 2.8 μM, >20 μM for Nef:Hck complex and Hck, respectively. Hck-IN-1 is a direct and wide HIV-1 Nef antagonists with an IC₅₀ of 100-300 nM for wild-type HIV-1 replication. Hck-IN-1 binds pocket residue Asn126 and has anti-retroviral activity.

KX2-361 (KX-02) is a Src-kinase and tubulin polymerization inhibitor. KX2-361 shows good oral bioavailability and readily crosses the BBB in mice. KX2-361 shows anti-tumor activity and induces apoptosis of Glioblastoma (GBM) cell.

SRC-3-IN-2 (SI-12 6c)is an orally active steroid receptor coactivator 3 (SRC-3) inhibitor. SRC-3-IN-2 has antitumor activity.

Papaveroline hydrochloride is an orally active Fyn tyrosine kinase inhibitor. Papaveroline hydrochloride stably binds to the active site of Fyn tyrosine kinase via hydrogen bonding and hydrophobic interactions, thereby inhibiting kinase activity associated with the pathogenesis of Alzheimer's disease. Papaveroline hydrochloride can be used for the research of Alzheimer's disease.

Dasatinib (Standard) is the analytical standard of Dasatinib. This product is intended for research and analytical applications. Dasatinib (BMS-354825) is a highly potent, ATP competitive, orally active dual Src/Bcr-Abl inhibitor with potent antitumor activity. The K_is are 16 pM and 30 pM for Src and Bcr-Abl, respectively. Dasatinib inhibits Bcr-Abl and Src with IC₅₀s of <1.0 nM and 0.5 nM, respectively. Dasatinib also induces apoptosis and autophagy.

Momordicine I is a cucurbitane-type triterpenoids. Momordicine I suppresses glioma growth by promoting apoptosis and impairing mitochondrial oxidative phosphorylation. Momordicine I inhibits glycolysis, lipid metabolism, induces autophagy in HNC cells to suppress head and neck cancer growth. Momordicine I alleviates isoproterenol-induced cardiomyocyte hypertrophy through suppression of PLA2G6 and DGK-ζ. Momordicine I exerts its cardiovascular benefits by upregulating nitric oxide, inhibiting the activity of angiotensin-converting enzyme (ACE), activating the PI3K/Akt pathway, reducing oxidative stress and inflammation. Momordicine I inhibits AKT1, IL-6, and SRC, suggesting its potential application in type 2 diabetes.

TL13-68 is a biotin-tagged version of SM1-71, and it can be used to research the mechanism of SM1-71.

TG53 is a potent inhibitor of tissue transglutaminase (TG2) and fibronectin (FN) protein-protein interaction. TG53 inhibits formation of a complex with integrin β1 and activation of FAK and c-Src during SKOV3 cell attachment onto FN. TG53 can be used for ovarian cancer research.

Chrysotoxine is a dual inhibitor of Src/Akt. Chrysotoxine suppresses cancer stem cells (CSCs) phenotypes by down-regulating Src/Akt signaling. Chrysotoxine reduces cell viability and increases apoptosis level in H460 and H23 cells instead of non-tumor cell lines. Chrysotoxine shows rapid excretion and low bioavailability in rats. Chrysotoxine is used in cancer research.

PD-089828 is an ATP competitive inhibitor of FGFR-1, PDGFR-β and EGFR (IC₅₀s=0.15, 1.76, and 5.47 µM, respectively) and a noncompetitive inhibitor of c-Src tyrosine kinase (IC₅₀=0.18 µM). PD-089828 also inhibits MAPK with an IC₅₀ of 7.1 µM. PD-089828 inhibits PDGF-, EGF- and bFGF-mediated tyrosine kinase receptor autophosphorylation in vitro. PD-089828 has a long-lasting cellular activity.

pYEEI is a phosphotyrosine-containing tetrapeptide binds to Src SH2 domain with the K_d of 100 nM and with the IC₅₀ of 6.5 μM. pYEEI plays an important role in cancer research.

Pro-Dasatinib (compound 2j), an amino acid analog of Dasatinib (HY-10181), is a potent Src/Abl kinase inhibitor. Pro-Dasatinib has antiproliferative activity against K652 leukemia cancer cells with an IC₅₀ of 0.21 nM.

IGF-1R/SRC-IN-1 (Compound 3b) is an inhibitor for IGF-1R (IC₅₀ is 63 μM) and SRC.

CCT241161 is an orally active pan-RAF inhibitor with IC₅₀s of 3, 6, 10, 15 and 30 nM for LCK, CRAF, SRC, V600E-BRAF and BRAF, respectively. CCT241161 shows good activity to in BRAF and NRAS mutant melanomas. CCT241161 also exhibits anticancer cell proliferative activity.

A 419259 GMP is the GMP grade A 419259 (HY-15764), inducing cell apoptosis. GMP-grade small molecules can be used as auxiliary reagents in cell therapy. A 419259 (RK-20449) is a broad-spectrum pyrrole-pyrimidine inhibitor targeting Src, Lck, and Lyn with IC₅₀s of 9 nM, <3 nM, and <3 nM, respectively.