Src Inhibitor

Larixyl acetate is a potent and selective TRPC6 inhibitor with IC₅₀ values of 0.58 μM and 6.83 μM against hTRPC6-YFP and hTRPC3-YFP, respectively. Larixyl acetate prevents HPV and is effective in protecting against traumatic brain injury-induced systemic endothelial dysfunction.

Notoginsenoside R2 (20(S)-Notoginsenoside R2; Ginsenoside Ng-R2) is an orally active notoginsenoside. Notoginsenoside R2 activates P90RSK and Nrf2 via the MEK1/2-ERK1/2 pathway to inhibit 6-OHDA-induced apoptotic damage in nerve cells. Notoginsenoside R2 upregulates SOX8/β-catenin by reducing miR-27a, thereby suppressing Aβ_25-35-induced neuronal apoptosis and inflammatory responses. Notoginsenoside R2 alleviates lipid accumulation and mitochondrial dysfunction in diabetic nephropathy by inhibiting c-Src. Notoginsenoside R2 alleviates hepatic fibrosis by inducing hepatic stellate cell senescence and inhibiting the inflammatory microenvironment via JAK/STAT3 suppression. Notoginsenoside R2 can be used in research related to Parkinson's disease, Alzheimer's disease, diabetic nephropathy and hepatic fibrosis.

Dasatinib metabolite M6 (Dasatinib carboxylic acid) is a circulating metabolite of Dasatinib (HY-10181). Dasatinib exhibits potent anti-tumor activity.

KIN-8194 is an orally active dual inhibitor of HCK and BTK, with IC₅₀ values of 0.915 and <0.495 nM, respectively. KIN-8194 impairs growth and integrin-mediated adhesion of BTKi-resistant mantle cell lymphoma (MCL). KIN-8194 overcomes ibrutinib (HY-10997) resistance with a survival benefit in TMD-8 ABC DLBCL xenografted mice.

(R)-9b is an ATP-competitive kinase inhibitor. (R)-9b binds to the ATP-binding site of ACK1/TNK2, inhibiting their kinase activity and autophosphorylation, with a human IC₅₀ of 56 nM. (R)-9b also inhibits JAK2, Tyk2, ALK, c-Src, ABL1, CHK1, FGFR1, LCK, and ROS/ROS1. (R)-9b can be used for research on prostate cancer.

PP58 is a pyrido[2,3-d]pyrimidine-based compound that inhibits PDGFR, FGFR and Src family activities with nanomolar IC₅₀ values.

Dasatinib-d₈ (BMS-354825-d₈) is a deuterium labeled Dasatinib. Dasatinib is a dual Bcr-Abl and Src family tyrosine kinase inhibitor.

Avenanthramide C is an orally active polyphenolic compound that penetrates the blood-brain barrier. Avenanthramide C is derived from oats. Avenanthramide C inhibits NF-κB nuclear translocation and inhibits the phosphorylation of PI3K, PLCγ1, Lyn, Syk, and Akt. Avenanthramide C inhibits the expression and activity of MMP-9 and inhibits MAPK phosphorylation. Avenanthramide C scavenges DPPH radicals, reduces intracellular ROS, and inhibits pro-inflammatory cytokine release and adhesion molecule expression. Avenanthramide C inhibits cell degranulation. Avenanthramide C attenuates active systemic anaphylaxis and inhibits passive cutaneous anaphylaxis. Avenanthramide C ameliorates PHZ-induced blood stasis. Avenanthramide C inhibits neuroinflammation, restores long-term potentiation, and improves recognition and spatial memory in Alzheimer's disease models. Avenanthramide C can be used for research on allergic inflammation, thrombosis, atherosclerosis, and Alzheimer's disease.

UM-164 (DAS-DFGO-II) is a highly potent inhibitor of c-Src with a K_d of 2.7 nM. UM-164 also potently inhibits p38α and p38β.

Bosutinib hydrate is an oraly activel Src/Abl tyrosine kinase inhibito with IC₅₀ of 1.2 nM and 1 nM, respectively.

Grb2 SH2 domain inhibitor 1 TFA is a conformationally restricted cyclic cell penetrating peptide (CPP) containing d-pro-l-pro motif ring (AF Φ Rpprrfq) (where Φ It is L-naphthylalanine, R is D-arginine, P is D-proline), which is mainly used as a cyclic peptide inhibitor.

AZM475271 (M475271) is an orally active and selective Src kinase inhibitor. AZM475271 inhibits phosphorylation of c-Src kinase, Lck, c-yes (IC₅₀s = 0.01, 0.03, 0.08 μM, respectively). AZM475271 induces apoptosis. AZM475271 reduces tumor cell proliferation and migration in vitro and in vivo, and reduces microvessel density (MVD). AZM475271 inhibits tumor growth and metastasis. AZM475271 sensitizes tumor cells to the cytotoxic effects of Gemcitabine (HY-17026).

Peruvoside is a potent inhibitor of Src, PI3K, JNK, STAT, and EGFR. Peruvoside induces apoptosis and autophagy and possesses a broad spectrum of anticancer activity in breast, lung, liver cancers and leukemia. Peruvoside is a broad-spectrum and potent antiviral activity against positive-sense RNA viruses. Peruvoside sensitizes Gefitinib (HY-50895)-resistant tumour cells (A549, PC9/gef and H1975) to Gefitinib.

TG 100572 Hydrochloride 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.

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.

PD180970 is a highly potent and ATP-competitive p210^Bcr-Abl kinase inhibitor, with an IC₅₀ of 5 nM for inhibiting the autophosphorylation of p210^Bcr-Abl. PD180970 also inhibits Src and KIT kinase with IC₅₀s of 0.8 nM and 50 nM, respectively. PD180970 indcues apoptosis of K562 leukemic cells, and can be used for chronic myelogenous leukemia research.

Pyridostatin (RR82) trihydrochloride is a G-quadruplex (G4) inducer/stabilizer with a K_d of 490 nM. Pyridostatin trihydrochloride also acts as an inhibitor of Zika virus (ZIKV) NS2B-NS3 protease, with an IC₅₀ of 11.0 μM. Pyridostatin trihydrochloride interacts with G-quadruplex structures, regulates the expression of SRC and SUB1, and induces replication- and transcription-dependent DNA damage, growth arrest, and genomic instability. Pyridostatin trihydrochloride exhibits antiproliferative and antiviral activities. Pyridostatin trihydrochloride can be used in studies related to breast cancer, cervical cancer, and Zika virus infection.

Osteogenic Growth Peptide (10-14) (OGP(10-14)), the C-terminal truncated pentapeptide of osteogenic growth peptide (OGP), retains the full OGP-like activity. Osteogenic Growth Peptide (10-14) is responsible for the binding to the OGP receptor and activates an intracellular Gi-protein-MAP kinase signaling pathway. Osteogenic Growth Peptide (10-14) is a potent mitogen and stimulator of osteogenesis and hematopoiesis. Osteogenic Growth Peptide (10-14) acts as a Src inhibitor.

Tirbanibulin Mesylate (KX2-391 Mesylate) is an inhibitor of Src that targets the peptide substrate site of Src, with GI₅₀ of 9-60 nM in cancer cell lines.

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.