AZM475271 is a potent, selective and oral inhibitor of Src kinase with IC50 of 5 nM and with potential anticancer activities; it has no inhibitory activity on Flt3, KDR, Tie-2.

Tirbanibulin dihydrochloride (also known as KXO1 dihydrochloride and KX2-391 dihydrochloride) is a dual Src/tubulin inhibitor approved in 2020 for the treatment of actinic keratosis on the face or scalp.

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

1-NM-PP1, a C3-modified analog of PP1, is a novel, potent and cell permeable protein kinase D (PKD) inhibitor with an IC50 of 0.398 μM.

WH-4-023 (also called KIN112; WH-4023; KIN-001-112) is a novel, potent, selective and orally bioactive inhibitor of Src family kinase (dual Lck/Src inhibitor) with potential anti-inflammatory and anticancer activity. It inhibits dual Lck/Src kinases with IC50s of 2 nM and 6 nM in cell-free assays, respectively. WH-4-023 increased LPS-stimulated IL-10 production and greatly suppressed proinflammatory cytokine […]

Bosutinib (formerly also known as SKI-606; trade name Bosulif) is a novel, quinolone-based, and potent dual Src/Abl kinase inhibitor with potential antitumor activity. It inhibits Src and Abl with IC50 of 1.2 nM and 1 nM in cell-free assays, respectively. Bosutinib was approved by the US FDA and EU European Medicines Agency on September 4, […]

PP1 (known also as EI275; EI-275; PP-1; PP 1; AG1872; AG-1872) is a novel, potent and selective Src kinase inhibitor with potential antitumor activity. It inhibits Lck/Fyn kinases with IC50 of 5 nM/6 nM. It exhibits excellent anti-proliferative activity in vitro and high in vivo antitumor efficacy.

SU 6656 (SU-6656) is a novel, potent and selective Src family kinase (Src, Yes, Lyn, and Fyn) inhibitor with potential antineoplastic activity. It inhibits Src, Yes, Lyn, and Fyn with IC50 of 280 nM, 20 nM, 130 nM, and 170 nM respectively. SU6656 modulates CTGF (connective tissue growth factor) expression in an ERK-dependent manner. SU6656 […]

PP2 (also known as AG 1879; AG-1879) a novel, potent, reversible, and ATP-competitive and selective Src family kinase inhibitor with potential anticancer activity. It inhibits Lck/Fyn kinases with IC50s of 4 nM/5 nM in cell-free assays, and is less potent to or inactive for EGFR, ZAP-70, JAK2 and PKA. PP2 is a chemical substance frequently […]

Tirbanibulin (also known as KXO1; KX2-391; Klisyri) is novel, potent and the first clinical peptidomimetic Src kinase inhibitor as well as a mitotic/tubulin inhibitor with potential anticancer activity. It has been approved by FDA in 2020 as a medication for the treatment of actinic keratosis on the face or scalp. Tirbanibulin inhibits the peptide substrate […]