Tolimidone, formerly known as MLR-1023, is a novel and potent insulin receptor potentiator, and also a selective allosteric activator of Lyn kinase (EC50 of 63 nM).
Bosutinib hydrate (SKI606; KIN001160; SKI-606; KIN-001160; Bosulif), the mono-hydrated form of bosutinib, is a synthetic quinolone derivative and dual kinase inhibitor targeting both Abl and Src kinases with potential antineoplastic activity.
KIN001-051 (Lck inhibitor; C-8863; KIN-001-051) is a novel, potent, cell-permeable and ATP-competitive inhibitor of Lymphocyte-specific protein tyrosine kinase (LCK, IC50s < 1 and 2 nM for C/D isoforms).
Tirbanibulin Mesylate (also known as KXO-1 Mesylate and KX2-391 Mesylate) is a tubulin/Src inhibitor that has gained FDA approval in 2020 for the treatment of actinic keratosis on the face or scalp.
Lck inhibitor 2, a bis-anilinopyrimidine derivative, is a novel and potent multi-kinase inhibitor of tyrosine kinases including LCK, BTK, LYN, SYK, and TXK with IC50 values of 13nM, 9nM, 3nM, 26nM and 2nM for Lck, Btk, Lyn, Btk and Txk respectively.
AMG-47a is a novel, potent inhibitor of Lck and T cell proliferation which exhibits anti-inflammatory activity with ED50 of 11 mg/kg in the anti-CD3 induced production of IL-2 in mice.
TG 100572 HCl (TG-100572; TG100572), the hydrochloride salt of TG100572, is a novel, potent and selective multi-targeted kinase (receptor tyrosine kinases and Src kinases) inhibitor with anti-proliferative activity and is being developed for the treatment of AMD (age-related macular degeneration).
1-Naphthyl PP1 HCl (also known as 1-NA-PP1 hydrochloride) 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.
Scutellarein is a novel and potent natural product.
KX1-004 is a novel and potent small molecule inhibitor of Src-protein tyrosine kinase that can be used to reduce cisplatin ototoxicity while preserving its antitumor effect.