Src Inhibitor

TX-1918 is an inhibitor for eukaryotic elongation factor 2 kinase (eEF2-K) and Src kinase with IC₅₀ of 0.44 and 4.4 μM, respectively. TX-1918 exhibits cytotoxicity in cell HepG2 and HCT116, with IC₅₀ of 2.07 and 230 μM, respectively. TX-1918 inhibits the C-terminal domain of HIV-1 CA (CA CTD)(IC₅₀ =3.81 μM), and inhibits the viral replication (IC₅₀ =15.16 μM).

Excisanin A is a potent anticancer agent. Excisanin A inhibits cell proliferation, migration, adhesion and invasion. Excisanin A decreases the expression of MMP-2, MMP-9, p-FAK, p-Src, integrin β1 protein. Excisanin A has the potential for the research of breast cancer.

BMS-358233 (compound 3) is a Lck inhibitor (IC₅₀: 1 nM; Ki: 540 pM) and inhibits T cell proliferation (IC₅₀: 262 nM).

SKS-927 is a Src kinase inhibitor, with an IC₅₀ value of 3.9 nM. SKS-927 inhibits the proliferation of Src-transformed rat fibroblasta, with an IC₅₀ value of 73 nM. SKS-927 exhibits an IC₅₀ value of 720 nM against EGFR. SKS-927 can be used for the study of cancer and osteoporosis.

Scr-IN-1 (Compound 4e) is a Tyrosine kinase inhibitor. Scr-IN-1 inhibits HCT-116 cells and MIA-PaCa-2 cells with IC₅₀s of 0.16 μM and 1.16 μM, respectively. Scr-IN-1 displays selectivity profile on HCT-116 cells and MIA-PaCa-2 cells with SI > 625 and SI > 86, respectively. Scr-IN-1 induces Apoptosis in HCT-116 colon cancer cell and does not cause any change in the rate of necrotic cells. Scr-IN-1 is a novel SRC kinase inhibitor candidate for HCT-116 cells. Scr-IN-1 is potential for cancer research.

SRT6 is a CD44 inhibitor. SRT6 exerts antiproliferative activity in CD44⁺ breast cancer and lung cancer cells. SRT6 inhibits CD44-associated SRC kinase, as well as EGFR, ERBB2, ERBB4, MAP3K10 and MAPKAPK2. SRT6 can be used for the research of breast cancer and lung cancer.

Protein kinase inhibitor 11 (Compound I-96) is a protein kinase inhibitor that can inhibit the activity of PIM-1, CDK-2, GSK-3, and SRC. Protein kinase inhibitor 11 holds promise for research in cancer, immune disorders, and neurodegenerative diseases.

c-Src Kinase-IN-1 is a highly selective, cell-permeable inhibitor of c-Src kinase that suppresses cancer cell growth. c-Src Kinase-IN-1 has a K_i of 44 nM and a K_d value of 86 nM against chicken-derived c-Src. c-Src Kinase-IN-1 interacts with the phosphate-binding loop of c-Src and exhibits selectivity toward homologous Src family kinases and c-Abl. c-Src Kinase-IN-1 can be used in cancer-related research.

BCR-ABL-IN-13 is a dual c-Src and Abl inhibitor, with a K_i value of 0.55 μM against c-Src, 0.10 μM against wild-type Abl, and 0.40 μM against the Abl^T315I mutant. BCR-ABL-IN-13 exerts competitive/mixed-type inhibitory effects on wild-type Abl, and non-competitive inhibitory effects on the drug-resistant Abl^T315I mutant. BCR-ABL-IN-13 can be used for the research of chronic myeloid leukemia.

CpCDPK1/TgCDPK1-IN-1 (compound 7p) is a potent CpCDPK1/TgCDPK1 dual inhibitor (IC₅₀: 10 nM and 5.0 nM respectively). CpCDPK1/TgCDPK1-IN-1 also inhibits Abl and Src (IC₅₀: 75 nM and 65 nM respectively). CpCDPK1/TgCDPK1-IN-1 can be used for research of toxoplasmosis.

HPK1-IN-2 TFA is an orally active HPK1 inhibitor (IC₅₀ < 0.05 µM) with antitumor activity. HPK1-IN-2 TFA inhibits the activity of Lck (IC₅₀ <0.05 µM) and Flt3 (IC₅₀ < 0.05 µM) kinases.

BTK-IN-48 is a BTK inhibitor with an IC₅₀ of 1.14 μM. BTK-IN-48 inhibits recombinant BTK and c-Src, and exerts moderate inhibitory effects on LCK, BMX/ETK, FLT3 and PIM1. BTK-IN-48 can be used in the research of B-cell malignancies and autoimmune diseases.

Lysoganglioside-GM1 (LysoGM1) potassium is a derivative of Monosialoganglioside GM1, which lacks a fatty acid. Lysoganglioside-GM1 potassium is also an inhibitor of GM1 aggregation. Lysoganglioside-GM1 potassium can inhibit the activation of Lyn and laminin-1-mediated neurite outgrowth. Lysoganglioside-GM1 potassium can be used in the research of nervous system diseases.

Bosutinib (Standard) (SKI-606 (Standard)) hydrate is the analytical standard of Bosutinib hydrate (HY-10158A). This product is intended for research and analytical applications. Bosutinib hydrate is an oraly activel Src/Abl tyrosine kinase inhibito with IC₅₀s of 1.2 nM and 1 nM, respectively.

DC-Srci-6649 is a c-Src kinase inhibitor that inhibits the phosphorylation and locks c-Src in the inactive state.

SRC-3-IN-1 (compound SI-10) is a steroid receptor coactivator 3 (SRC-3) inhibitor (IC₅₀=3.3 μM). SRC-3-IN-1 has good water solubility, oral bioavailability, and improved selectivity profile. SRC-3-IN-1 can be used in prostate cancer research.

LCB 03-0110 dihydrochloride is a dihydrochloride of LCB 03-0110. LCB 03-0110 is a potent inhibitor of Src family tyrosine kinase.

Ac-Tyr(PO3H2)-Glu-Glu-Ile-Glu-OH (compound 1) is a high-affinity pentapeptide to bind to the src SH2 domain (IC₅₀≈1 µM). Ac-Tyr(PO3H2)-Glu-Glu-Ile-Glu-OH is an inhibitor for src SH3-SH2:phosphoprotein interactions.

Lck-IN-4 (Compound A-1) is a protein tyrosine kinase Lck inhibitor with an IC₅₀ of 2  nM. Lck-IN-4 significantly inhibits YAP tyrosine phosphorylation and activity and induces apoptosis in cholangiocarcinoma CCA cells. Lck-IN-4 is cytotoxic in CCA tumor-derived organoids with elevated YAP activity Lck-IN-4 can be used for cancers like cholangiocarcinoma (CCA) research.

AD57 hydrochloride is an orally active multikinase inhibitor, inhibits RET, BRAF, S6K and Src.