fgr

Ibrutinib (PCI-32765) is an irreversible inhibitor of BTK (IC50: 0.5 nM) that selectively blocks B cell activation.

TL02-59 is a selective inhibitor of Fgr in Src-family kinase (IC50 = 0.03 nM). TL02-59 inhibits Lyn and Hck with IC50s of 0.1 nM and 160 nM, respectively. TL02-59 potently suppresses acute myelogenous leukemia cell growth.

TL02-59 dihydrochloride is an orally active inhibitor of the Src-family kinase Fgr, with an IC50 of 0.03 nM.

Vemurafenib (RG7204) is a B-RAF inhibitor that inhibits RAFV600E and c-RAF-1 (IC50=31/48 nM) selectively and potently. Vemurafenib exhibits antitumor activity and is used for the treatment of BRAF V600E mutation-positive melanoma.

PRT062607 hydrochloride (P505-15 Hydrochloride) is a selective inhibitor of Syk (IC50: 1 nM). It displays at least 80-fold selectivity for Syk over other kinases.

TAK-901 has been used in trials studying the treatment of Lymphoma, Myelofibrosis, Multiple Myeloma, Myeloid Metaplasia, and Advanced Solid Tumors, among others.

Saracatinib (AZD0530) is a small molecule inhibitor belonging to the Src family kinase inhibitors (IC50=2.7–11 nM), featuring high selectivity, cell permeability, and oral bioavailability, with anti-fibrotic, anti-inflammatory, and potential anti-tumor activities.

Staurosporine (AM-2282) is a protein kinase inhibitor with ATP-competitive and non-selective inhibitory activity (IC50=6/15/2/3/3000 nM) against PKC, PKA, c-Fgr, phosphorylase kinase and TAOK2. Staurosporine also induces apoptosis.

A-770041 is an orally active and selective Lck inhibitor that inhibits concanavalin A-stimulated IL-2 production in whole blood and prevents cardiac allograft rejection. A-770041 reduces pulmonary fibrosis by inhibiting TGF-β production in regulatory T cells.

BMS-243117 is an effective selective LCK inhibitor with good cell activity (IC(50)=1.1 microM) and inhibition of T cell proliferation, which has great potential for therapeutic immunosuppression and the treatment of diseases such as rheumatoid arthritis a

Midostaurin (PKC412) is a multi-targeted tyrosine kinase inhibitor with antitumor activity, exhibiting IC50 values ranging from 22 to 500 nM against PKCα/β/γ, Syk, Flk-1, Akt, PKA, c-Kit, c-Fgr, c-Src, FLT3, PDFRβ, and VEGFR1/2. Midostaurin is indicated for the treatment of acute myeloid leukemia (AML) and systemic mastocytosis (SM).

Vofatamab (B-701) is a fully human monoclonal antibody targeting FGFR3. Vofatamab has potential anticancer and antitumor activity and is often used in combination with other compounds to treat cancer.

Human Follicular Gonadotropin Releasing Peptide (hF-GRP) is a hormonal peptide that, in vitro, can induce the secretion of pituitary luteinizing hormone (LH) and follicle-stimulating hormone (FSH) [1] [2].

BING, a antimicrobial peptide discovered in Japanese medaka fish (O. laptipes), originates from vacuolar protein sorting-associated protein 13D-like (Vps13D). It exhibits efficacy against a range of Gram-negative and Gram-positive bacteria, notably including methicillin-resistant S. aureus (MRSA; MICs = 4-64 µg/ml). Furthermore, BING enhances the effectiveness of antibiotics such as ampicillin, amoxicillin, and novobiocin against P. aeruginosa, and it prevents resistance development to kanamycin and ampicillin in E. coli. Notably, its administration in vivo significantly improves survival rates in O. laptipes challenged with E. tarda.

TG 100572 Hydrochloride is a inhibitor of multi-targeted kinase which inhibits receptor tyrosine kinases and Src kinases(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 100572 is a inhibitor of multi-targeted kinase which inhibits receptor tyrosine kinases and Src kinases(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 is a prodrug to treat age-related macular degeneration. TG 100572 is a inhibitor of multi-targeted kinase(IC50s of 2, 7, 2, 16, 13, 5, 0.5, 6, 0.1, 0.4, 1, 0.2 for VEGFR1, VEGFR2, FGFR1, FGFR2, PDGFRβ, Fgr, Fyn, Hck, Lck, Lyn, Src,

SIK1-IN-1 (Compound 27) is a selective inhibitor of salt-inducible kinase 1 (SIK1) with an IC50 of 0.7 nM, demonstrating greater potency for SIK1 compared to SIK2 and SIK3. It shows no cytotoxicity in HEK293 cells and PBMC at concentrations up to 30 μM. Additionally, SIK1-IN-1 effectively inhibits 392 kinases, particularly tyrosine kinases such as FGR, HCK, and LYN.

DCC-2036 (Rebastinib (DCC-2036)) is a conformational control Bcr-Abl inhibitor for Abl1(WT, IC50: 0.8 nM) and Abl1(T315I, IC50: 4 nM), also inhibits LYN, SRC, HCK, FGR, FLT3, KDR, and Tie-2, and low activity to c-Kit. Rebastinib aimed at the Angiopoietin2-Tie2 pathway.

BMS-986143, an orally active, reversible BTK inhibitor with an IC50 value of 0.26 nM, is designed for autoimmune disease research. Additionally, it targets TEC, BLK, BMX, TXK, FGR, YES1, and ITK, exhibiting IC50s of 3 nM, 5 nM, 7 nM, 10 nM, 15 nM, 19 nM, and 21 nM, respectively [1].