Src family kinase (SFK) is a family of non-receptor tyrosine kinases including nine members: Src, Yes, Fyn, and Fgr, forming the SrcA subfamily, Lck, Hck, Blk, and Lyn in the SrcB subfamily, and Frk in its own subfamily. In immune cells, Src-family kinases (SFKs) have been implicated as critical regulators of a large number of intracellular signaling pathways. Src-family kinases (SFKs) occupy a proximal position in numerous signaling transduction cascades including those emanating from the T and B cell antigen receptors, Fc receptors, growth factor receptors, cytokine receptors, and integrins. In addition to these positive regulatory roles, Src-family kinases (SFKs) can also function as negative regulators of cellular signaling by phosphorylating immunoreceptor tyrosine-based inhibitory motifs (ITIMs) on inhibitory receptors, resulting in recruitment and activation of inhibitory molecules such as the phosphatases SHP-1 and SH2 containing 5′ inositol phosphatase (SHIP-1).
Cat. No. | Product Name | CAS No. | Information |
---|---|---|---|
H9552 |
Elzovantinib |
2271119-26-5 | Elzovantinib is an oral-active inhibitor of SRC, MET and c-FMS, with IC50 values of 0.12 nM, 0.14 nM and 0.76 nM for SRC, MET and c-FMS respectively. |
H9375 |
DGY-06-116 |
2556836-50-9 | DGY-06-116 is an irreversible covalent, selective Src inhibitor with an IC50 of 3nM. DGY-06-116 inhibits FGFR1 with an IC50 of 8340 nM. |
H9234 |
SquarunkinA |
2101958-02-3 | Squarunkin A selectively inhibits the binding of a myristoylated peptide representing the N-terminus of Src kinase to UNC119A with an IC50 value of 10 nM;It binds to UNC119 proteins in cell lysate and interferes with the activation of Src kinase. |
H9233 |
NCGC00262650 |
344359-25-7 | NCGC00262650 is a dual inhibitor of AMA1-RON2 interaction and c-Src tyrosine kinase activity. |
H8003 |
UNC119-Src interaction inhibitor 3 |
1358350-63-6 | UNC119-Src interaction inhibitor 3 is a potent, specific small molecule inhibitor of UNC119-Src interaction with IC50 of 12 nM for displacement of the Src peptide from UNC119A; selectivity released all N-myristoylated peptides from UNC119, but not the farnesyl-protein binding proteins PDE6d, AIPL1 and calmodulin; binds to UNC119 in cells (Kd=71.8 nM), and induces redistribution of Src to endomembranes and reduction of activating Src autophosphorylation on Y419; UNC119 inhibition in Src-dependent colorectal cancer cells results in the specific reduction of cell growth and clonogenic potential. |
H8002 |
UM-164 |
903564-48-7 | UM-164 is a movel potent, dual c-Src/p38 with Kd of 2.7 nM (c-Src), potently inhibits both p38α and p38β; inhibits c-Src autophosphorylation in TNBC cell lines, and shows potent antiproliferative activity with mean GI50 of 160 nM, alters the cell localization of c-Src in TNBC cells; completely inhibits p38 MAPK phosphorylation in SUM 149 cells at 50 nM; demonstrates potent anti-TNBC activity in xenograft models with limited in vivo toxicity. |
H8001 |
UCS15A |
108303-00-0 | UCS15A is a small moelcule SH3 domain-mediated protein-protein interaction blocking agent that inhibits proline-rich ligand-mediated protein-protein interactions (PLPI); disrupts the interaction of Src-SH3 with Sam68 both in vivo and in vitro, also disrupts the in vivo interactions of Sam68 with other SH3 domain containing proteins such as Grb2 and PLCγ; unable to disrupt the non-SH3-mediated protein-protein interactions of beta-catenin, with E-cadherin and alpha-cateni, and has no effect on the SH2-mediated interaction between Grb2 and activated EGFR; effectively inhibits AMAP1/cortactin binding and breast cancer invasion and metastasis. |
H8000 |
TX-1123 |
157397-06-3 | A tyrphostin AG17 analog that exihibits potent Src-K inhibitory activity with IC50 of 2.2 uM; also inhibits eEF2K (IC50=3.2 uM) and PKA (IC50=9.6 uM); exhibits potent anti-tumor activity in HepG2 (EC50=3.66 uM) and HCT116 (EC50=39 uM) tumor cells. |
H7999 |
TL02-59 |
1315330-17-6 |
TL02-59 is a potent, selective, orally available inhibitor of Src-family kinase Fgr IC50 of 0.03 nM, also inhibits Lyn and Hck with IC50 of 0.1 and 160 nM, respectively; inhibits Syk, Fes, Flt3-WT and Flt3-ITD with IC50 of 470, 290, 633 and 440 nM, inhibits MV4-11 AML cell growth with IC50 of <1 nM; completely eliminates leukemic cells from the spleen and peripheral blood while significantly reducing bone marrow engraftment at 10 mg/kg in mouse xenograft model of AML. |
H7998 |
TG 100801 hydrochloride |
1018069-81-2 | The prodrug of TG 100572, a potent, dual receptor tyrosine kinase/Src kinase inhibitor with IC50 of 2-16 nM for VEGFR, FGFR and PDGFR, 0.1-5 nM for Src family; significantly suppresses laser-induced CNV in mice, and reduces fluorescein leakage from the vasculature and retinal thickening in a rat model of retinal vein occlusion (topical administration). |
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