2. Signaling Pathways
  3. Protein Tyrosine Kinase/RTK
  4. Src

Src

Src

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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).

Src Isoform Specific Products:

Src Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • HY-112291A
    SB 220025 (tri(hydrochloride))
    		Inhibitor
    SB 220025 trihydrochloride is a reversible, orally active, cell-permeable, ATP-competitive and selective human p38 MAPK inhibitor (IC50 = 60 nM). SB 220025 trihydrochloride also inhibits p56Lck and PKC with IC50 values of 3.5 and 2.89 μM, respectively. SB 220025 trihydrochloride inhibits the expression of IL-8 gene in response to globular adiponectin (gAd), reduces inflammatory cytokine production and inhibits angiogenesis. SB 220025 trihydrochloride effectively prevents the progression of arthritis in a chronic inflammatory disease model and can be used in the study of inflammation.
    SB 220025 (tri(hydrochloride))
  • HY-W994722
    ISO24
    		Ligand
    ISO24 (compound 4a) is a potent liagnd of Src SH2, with the IC50 of 4.4 mM in BIAcore assay.
    ISO24
  • HY-13314R
    Tesevatinib (Standard)
    		Inhibitor
    Tesevatinib (Standard) is the analytical standard of Tesevatinib. This product is intended for research and analytical applications. Tesevatinib (XL-647) is an orally available, blood-brain barrier-penetrant inhibitor of the epidermal growth factor receptor (EGFR). Tesevatinib significantly reduces cellular viability, with IC50 values of 11 nM and 102 nM in GBM12 and GBM6, respectively. Tesevatinib also inhibits HER2 (IC50=16.1 nM), VEGFR2 (IC50=1.5 nM), and Src (IC50=10.3 nM). Tesevatinib can inhibit tumor proliferation and exhibits antitumor activity.
    Tesevatinib (Standard)
  • HY-N14279
    Hibarimicin G
    		Inhibitor
    Hibarimicin G is a tyrosine kinase inhibitor found in Microbispora rosea subsp. Hibaria.
    Hibarimicin G
  • HY-160930
    TOP1288
    		Inhibitor
    TOP1288 is a narrow spectrum kinase inhibitor for P38α, Src and Syk kinase, with IC50 of 116nM, 24nM and 659nM, respectively. TOP1288 inhibits inflammatory cytokine release from inflamed biopsies and myofibroblasts.
    TOP1288
  • HY-10158S1
    Bosutinib-13C,d3
    		Inhibitor
    Bosutinib-13C,d3 (SKI-606-13C,d3) is 13C labeled Bosutinib. Bosutinib is an orally active Src/Abl tyrosine kinase inhibitor with IC50 of 1.2 nM and 1 nM, respectively.
    Bosutinib-<sup>13</sup>C<sub>,d<sub>3</sub>
  • HY-10181AR
    Dasatinib hydrochloride (Standard)
    		Inhibitor
    Dasatinib (hydrochloride) (Standard) is the analytical standard of Dasatinib (hydrochloride). This product is intended for research and analytical applications. Dasatinib (BMS-354825) hydrochloride is a highly potent, ATP competitive, orally active dual Src/Bcr-Abl inhibitor with potent antitumor activity. The Kis are 16 pM and 30 pM for Src and Bcr-Abl, respectively. Dasatinib hydrochloride inhibits Bcr-Abl and Src with IC50s of <1.0 nM and 0.5 nM, respectively. Dasatinib hydrochloride also induces apoptosis and autophagy.
    Dasatinib hydrochloride (Standard)
  • HY-50868R
    Bafetinib (Standard)
    		Inhibitor
    Bafetinib (Standard) is the analytical standard of Bafetinib. This product is intended for research and analytical applications. Bafetinib is an orally active Lyn/Bcr-Abl tyrosine kinase inhibitor. Bafetinib enhances the activity of several pro-apoptotic Bcl-2 homology (BH) 3-pure proteins (Bim, Bad, Bmf, and Bik) through intrinsic apoptotic pathways regulated by the Bcl-2 family, and induces apoptosis of Ph+ leukemia cells. Bafetinib has antitumor activity.
    Bafetinib (Standard)
  • HY-171218
    CGP062464
    		Inhibitor
    CGP062464 is an inhibitor of the tyrosine kinase c-Src (IC50: < 50 nM). CGP062464 can be used for research of osteoporosis and tumor-induced hypercalcemia.
    CGP062464
  • HY-10187
    TG 100801 Hydrochloride
    		Inhibitor
    TG 100801 Hydrochloride is a proagent that generates TG 100572 by de-esterification in development to treat age-related macular degeneration. TG 100572 is a multi-targeted kinase inhibitor which inhibits receptor tyrosine kinases and Src kinases; has IC50s of 2, 7, 2, 16, 13, 5, 0.5, 6, 0.1, 0.4, 1, 0.2 nM for VEGFR1, VEGFR2, FGFR1, FGFR2, PDGFRβ, Fgr, Fyn, Hck, Lck, Lyn, Src, Yes, respectively.
    TG 100801 Hydrochloride
  • HY-N14267
    Hibarimicin A
    		Inhibitor
    Hibarimicin A is a tyrosine kinase inhibitor found in Microbispora rosea subsp. hibaria. Hibarimicin A selectively inhibits the activity of src tyrosine kinase without affecting protein kinase A and C. Hibarimicin A also has moderate anti-Gram-positive bacteria activity with a MIC of 0.8-12.56 μg/mL.
    Hibarimicin A
  • HY-N12166
    2,3,4,6,8-Pentahydroxy-1-methylxanthone
    		Inhibitor
    2,3,4,6,8-Pentahydroxy-1-methylxanthone is a xanthone derivative of Wardomyces anomalus. 2,3,4,6,8-Pentahydroxy-1-methylxanthone shows significant antioxidant activities. 2,3,4,6,8-Pentahydroxy-1-methylxanthone is inhibitors of p56lck tyrosine kinase. 2,3,4,6,8-Pentahydroxy-1-methylxanthone can be used to treat cardiovascular disease.
    2,3,4,6,8-Pentahydroxy-1-methylxanthone
  • HY-32718S
    Pelitinib-d6
    Pelitinib-d6 (EKB-569-d6) is the deuterium labeled Pelitinib. Pelitinib (EKB-569) is an irreversible inhibitor of EGFR with an IC50 of 38.5 nM; also slightly inhibits Src, MEK/ERK and ErbB2 with IC50s of 282, 800, and 1255 nM, respectively.
    Pelitinib-d6
  • HY-10340R
    Tirbanibulin (Standard)
    		Inhibitor
    Tirbanibulin (Standard) is the analytical standard of Tirbanibulin. This product is intended for research and analytical applications. Tirbanibulin (KX2-391) is an inhibitor of Src that targets the peptide substrate site of Src, with GI50 of 9-60 nM in cancer cell lines.
    Tirbanibulin (Standard)
  • HY-125064
    AP22408
    		Inhibitor
    AP22408 is a nonpeptide inhibitor against Src SH2 with an IC50 value of 0.3 μM. AP22408 inhibits rabbit osteoclast-mediated resorption of dentine, exhibits bone-targeting properties based on a hydroxyapatite adsorption assay and demonstrates in vivo antiresorptive activity in a parathyroid hormone-induced rat model. AP22408 is proming for rasearch of osteoporosis and other bone-related diseases such as Paget’s disease, osteolytic bone metastasis and hypercalcemia associated with malignancy.
    AP22408
  • HY-164530
    SKLB646
    		Inhibitor
    SKLB646 is an orally active multi-target kinase inhibitor. SKLB646 shows significant inhibitory effects on SRC and VEGFR2 with IC50 values ??of 0.002 μmol/L and 0.012 μmol/L, respectively. SKLB646 also shows significant inhibitory effects on B-Raf and C-Raf with IC50 values ??of 0.022 μmol/L and 0.019 μmol/L, respectively. SKLB646 inhibits the activation of the SRC signaling pathway and blocks the MAPK signaling pathway by inhibiting Raf kinase. In addition, SKLB646 can inhibit the proliferation, migration and invasion of human umbilical vein endothelial cells (HUVEC) to inhibit tumor-induced angiopoietic formation. SKLB646 shows significant anti-proliferative and anti-survival activities against triple-negative breast cancer (TNBC) cell lines.
    SKLB646
  • HY-164527
    Si306
    		Inhibitor
    Si306 is a Src inhibitor with antitumor activity. Si306 reduces the phosphorylation of focal adhesion kinase (FAK) and the expression of epidermal growth factor receptor (EGFR), and inhibits the invasion of human glioblastoma (GBM).
    Si306
  • HY-N14618
    Rhodomycin A
    		Inhibitor
    Rhodomycin A can suppress lung cancer cell progression via modulating Src-related pathways.?Rhodomycin A significantly suppressed cancer cell proliferation, migration, invasion, and clonogenicity in vitro and tumour growth in vivo.
    Rhodomycin A
  • HY-10234S
    Saracatinib-d3
    		Inhibitor
    Saracatinib-d3 (AZD0530-d3) (ZG5129) is the deuterium-labeled analog of Saracatinib (HY-10234). Saracatinib-d3 is an inhibitor of the Src kinase, which can inhibit severe sepsis caused by bacterial or various microbial infections.
    Saracatinib-d<sub>3</sub>
  • HY-10340AR
    Tirbanibulin dihydrochloride (Standard)
    		Inhibitor
    Tirbanibulin (dihydrochloride) (Standard) is the analytical standard of Tirbanibulin (dihydrochloride). This product is intended for research and analytical applications. Tirbanibulin (dihydrochloride) (KX2-391 (dihydrochloride)) is an inhibitor of Src that targets the peptide substrate site of Src, with GI50 of 9-60 nM in cancer cell lines.
    Tirbanibulin dihydrochloride (Standard)
Cat. No. Product Name / Synonyms Application Reactivity
Src Isoform Comparison

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