TG-100435 is a multitargeted, orally active protein tyrosine kinase inhibitor, with Ki of 13 to 64 nM for Src, Lyn, Abl, Yes, Lck, and EphB4. TG-100435 plays an important role in cancer research.

RK-20448 is an ATP-competitive inhibitor of Lck, Src, KDR/VEGF2R and Tie-2 with IC50 values of 0.24, 1.19, 10.74 and 5.85 µM, respectively. RK-20448 also inhibits BLK, Csk, Fyn and Lyn with IC50 values of 0.37, 4.27, 2.03 and 0.43 µM, respectively. RK-20448 is the cis isomer of A-419259 derivative with neuroprotective and PP2A activating activities. FTY720-Mitoxy has the property of targeting mitochondria. In addition, FTY720-Mitoxy protects neurons by reducing inflammatory responses and is used in the study of neurodegenerative diseases such as Parkinson's disease.

K882 (Compound 4e) is a Src inhibitor, with KD of 0.315 μM. K882 induces Apoptosis. K882 inhibits XIAP and Survivin. K882 inhibits the activation of PI3K/Akt/mTOR, Jak1/Stat3, Ras/MAPK signaling pathways. K882 shows anti-tumor activity against non-small cell lung cancer.

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.

Src kinase inhibitor I is a potent competitive inhibitor of both Src and Lck (IC50 = 44 and 88 nM, respectively), as well as Csk and Yes.

Saracatinib (AZD0530) is a potent Src inhibitor with IC50 of 2.7 nM, and potent to c-Yes, Fyn, Lyn, Blk, Fgr and Lck; less active for Abl and EGFR (L858R and L861Q).

KX2-391, the first clinical Src inhibitor (peptidomimetic class) that targets the peptide substrate site of Src, with GI50 of 9-60 nM in cancer cell lines.

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.

JP-153 (JP153) is a novel small molecule targets the Src-FAK-Paxillin signaling, inhibits Src-dependent phosphorylation of paxillin (Y118) and downstream activation of Akt (S473) in RECs; potently inhibits VEGF-induced proliferation and migration, inhibits retinal neovascularization in the murine oxygen-induced retinopathy model.

WH-4-023 is a potent and selective dual Lck/Src inhibitor with IC50 of 2 nM/6 nM for Lck and Src kinase respectively; little inhibition on p38α and KDR.

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

AMG-47a is a potent inhibitor of Lck and T cell proliferation; exhibits anti-inflammatory activity (ED50 = 11 mg/kg) in the anti-CD3 induced production of IL-2 in mice.

1-Naphthyl PP1(1-NA-PP 1) is a selective inhibitor of src family kinases v-Src and c-Fyn as well as the tyrosine kinase c-Abl (IC50 values are 1.0, 0.6, 0.6, 18 and 22 μM for v-Src, c-Fyn, c-Abl, CDK2 and CAMK II respectively).

RK-24466 (KIN 001-51) is a potent and selective Lck inhibitor; inhibits Lck (64-509) and LckCD isoforms with IC50s of less than 1 and 2 nM, respectively.

UM-164 is a Potent c-Src/p38 Kinase Inhibitor with In Vivo Activity against Triple-Negative Breast Cancer.

SRI-37264 (SRI 37264) is a small molecule inhibitor of HIV-1 Nef-mediated activation of the myeloid Src-family kinase Hck, blocks HIV-1 replication in macrophages and disrupts MHC-I downregulation.

PD-173955 is a src tyrosine kinase inhibitor. PD173955 inhibited Bcr-Abl-dependent cell growth.

Fenlean, a natural squamosamide derivative, is a Src tyrosine kinase inhibitor. Fenlean can inhibit over-activated microglia and protect dopaminergic neurons. Fenlean can attenuate neuroinflammation in Parkinson's disease models.

1-Naphthyl PP1(1-NA-PP1) is a selective inhibitor of src family kinases v-Src and c-Fyn as well as the tyrosine kinase c-Abl.

Antiallergic agent-1, a Src-family kinase inhibitor, may serve as a new valuable lead compound for future antiallergic drug discovery.

CGP77675 hydrate is an orally active and potent inhibitor of Src family kinases. CGP77675 hydrate inhibits phosphorylation of peptide substrates and autophosphorylation of purified Src (IC50s of 5-20 and 40 nM, respectively),and also inhibits Src, EGFR, KDR, v-Abl, and Lck with IC50s of 0.02, 0.15, 1.0, 0.31, and 0.29 μM, respectively. Anticancer activity.

iHCK-37 (ASN05260065) is a potent and specific Hck inhibitor with a Ki value of 0.22 μM. iHCK-37 blocks HIV-1 viral replication with an EC50 value of 12.9 μM. iHCK-37 is used for chronic myeloid leukemia (CML) research.

EPQpYEEIPIYL, a phosphopeptide, is a Src homology 2 (SH2) domain ligand. EPQpYEEIPIYL activates Src family members (e.g. Lck, Hck, Fyn) by binding to SH2 domains.

Squarunkin A hydrochloride is a potent and selective UNC119-cargo interaction inhibitor (IC50 of 10 nM for inhibiting the UNC119A-myristoylated Src N-terminal peptide interaction). Squarunkin A hydrochloride interferes with the activation of Src kinase in cells.

Lck-IN-1 is a potent lymphocyte protein tyrosine kinase (Lck) inhibitor extracted from patent WO2007013673A1, example 48.

Tyrosine Kinase Peptide 1 is a control substrate peptide for c-Src assay.

Caffeic acid-pYEEIE TFA, a non-phosphopeptide inhibitor, exhibits potent binding affinity for the GST-Lck-SH2 domain.

Caffeic acid-pYEEIE, a non-phosphopeptide inhibitor, exhibits potent binding affinity for the GST-Lck-SH2 domain.

Ac-Tyr(PO3H2)-Glu-Glu-Ile-Glu-OH TFA (compound 1) is a high-affinity pentapeptide to bind to the src SH2 domain (IC50≈1 μM). Ac-Tyr(PO3H2)-Glu-Glu-Ile-Glu-OH TFA is an inhibitor for src SH3-SH2:phosphoprotein interactions.

Ac-Tyr(PO3H2)-Glu-Glu-Ile-Glu-OH (compound 1) is a high-affinity pentapeptide to bind to the src SH2 domain (IC50≈1 μM). Ac-Tyr(PO3H2)-Glu-Glu-Ile-Glu-OH is an inhibitor for src SH3-SH2:phosphoprotein interactions.