Src Inhibitor

TG53 is a potent inhibitor of tissue transglutaminase (TG2) and fibronectin (FN) protein-protein interaction. TG53 inhibits formation of a complex with integrin β1 and activation of FAK and c-Src during SKOV3 cell attachment onto FN. TG53 can be used for ovarian cancer research.

Chrysotoxine is a dual inhibitor of Src/Akt. Chrysotoxine suppresses cancer stem cells (CSCs) phenotypes by down-regulating Src/Akt signaling. Chrysotoxine reduces cell viability and increases apoptosis level in H460 and H23 cells instead of non-tumor cell lines. Chrysotoxine shows rapid excretion and low bioavailability in rats. Chrysotoxine is used in cancer research.

pYEEI is a phosphotyrosine-containing tetrapeptide binds to Src SH2 domain with the K_d of 100 nM and with the IC₅₀ of 6.5 μM. pYEEI plays an important role in cancer research.

Pro-Dasatinib (compound 2j), an amino acid analog of Dasatinib (HY-10181), is a potent Src/Abl kinase inhibitor. Pro-Dasatinib has antiproliferative activity against K652 leukemia cancer cells with an IC₅₀ of 0.21 nM.

IGF-1R/SRC-IN-1 (Compound 3b) is an inhibitor for IGF-1R (IC₅₀ is 63 μM) and SRC.

A 419259 GMP is the GMP grade A 419259 (HY-15764), inducing cell apoptosis. GMP-grade small molecules can be used as auxiliary reagents in cell therapy. A 419259 (RK-20449) is a broad-spectrum pyrrole-pyrimidine inhibitor targeting Src, Lck, and Lyn with IC₅₀s of 9 nM, <3 nM, and <3 nM, respectively.

Dasatinib (BMS-354825) (GMP) is a GMP-grade Dasatinib (HY-10181). GMP-grade small molecules can be used as adjuvant agents in cell therapy. Dasatinib (BMS-354825) is an orally active, ATP-competitive, dual Src/Bcr-Abl inhibitor with potent antitumor activity. The K_i values ​​for Src and Bcr-Abl are 16 pM and 30 pM, respectively. Dasatinib inhibits Bcr-Abl and Src with IC₅₀ values ​​of less than 1.0 nM and 0.5 nM, respectively. Dasatinib also induces apoptosis and autophagy.

T338C Src-IN-2 is a mutant c-Src kinase inhibitor, with an IC₅₀ of 317 nM against T338C c-Src, 57 nM against T338C/V323A c-Src, and 19 nM against T338C/V323S c-Src. T338C Src-IN-2 inhibits the kinase activity of endogenous cysteine gatekeeper MOK. T338C Src-IN-2 reduces global phosphotyrosine levels in v-Src-ES1-transformed NIH-3T3 cells.

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

Papaveroline is a Fyn tyrosine kinase inhibitor, Na⁺,K⁺-ATPase inhibitor with an IC₅₀ of 0.20 mM, Mg²⁺-ATPase inhibitor, K⁺-activated pNPPase inhibitor with an IC₅₀ of 1.51 mM, and apoptosis inducer. Papaveroline binds to the active site of Fyn tyrosine kinase and forms stable interactions with pocket amino acid residues. Papaveroline induces cell apoptosis, produces pycnotic and fragmented cell nuclei, and does not reduce intracellular ATP levels. Papaveroline is a dopamine-derived neurotoxin candidate associated with the pathogenesis of Parkinson's disease. Papaveroline can be used in the research of Alzheimer's disease and Parkinson's disease.

Bosutinib-d₈ is a deuterium labeled Bosutinib. Bosutinib is a dual Src/Abl inhibitor with IC₅₀s of 1.2 nM and 1 nM, respectively.

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.

Herbimycin A is an antibiotic and protein tyrosine kinase inhibitor. Herbimycin A directly inhibits the autophosphorylation of p210 BCR-ABL with an IC₅₀ of approximately 5 μM, and reduces Src kinase activity. Herbimycin A also induces the degradation of receptor tyrosine kinases such as insulin-like growth factor 1 receptor (IGF-1R), insulin receptor (IR) and epidermal growth factor receptor (EGFR) via the ubiquitin-20S proteasome pathway. Herbimycin A directly modifies NF-κB p50, with the main target site involving Cys62, thereby blocking the DNA binding of p50 and NF-κB-driven gene expression. Herbimycin A can be used in studies related to tyrosine kinase signaling, chronic myeloid leukemia, NF-κB signaling, osteoclast function, apoptosis and cellular stress.

T338C Src-IN-1 is a potent mutant-Src T338C inhibitor; exhibited the most potent inhibition of T338C(IC50=111 nM) relative to WT c-Src (10-fold increase).

KX1-004 is a potent and non-ATP competitive Src-PTK inhibitor with an IC₅₀ of 40 μM. KX1-004 protects the cochlea from hazardous noise and prevents noise-induced hearing loss (NIHL).

PP2 (Standard) is the analytical standard of PP2. This product is intended for research and analytical applications. PP2 is a reversible and ATP-competitive Src family kinases inhibitor with IC50s of 4 and 5 nM for Lck and Fyn, respectively.

Dasatinib-d₄ (BMS-354825-d₄) is deuterium labeled Dasatinib. Dasatinib (BMS-354825) is a highly potent, ATP competitive, orally active dual Src/Bcr-Abl inhibitor with potent antitumor activity. The K_is are 16 pM and 30 pM for Src and Bcr-Abl, respectively. Dasatinib inhibits Bcr-Abl and Src with IC₅₀s of <1.0 nM and 0.5 nM, respectively. Dasatinib also induces apoptosis and autophagy.

Bosutinib-¹³C,d₃ (SKI-606-¹³C,d₃) is ¹³C labeled Bosutinib. Bosutinib is an orally active Src/Abl tyrosine kinase inhibitor with IC₅₀ of 1.2 nM and 1 nM, respectively.

AZD0424 is an orally active, and dual selective Src/Abl kinase inhibitor with potential antineoplastic activity. AZD0424 induces apoptosis and cell cycle arrest in lymphoma cells.

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