Src Inhibitor

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.

Tyrosine kinase-IN-12 is a selective kinase inhibitor with inhibitory activity against human tyrosine kinases KDR, Abl, Lyn and Fyn.

Fyn-IN-1 (Compound 43) is a selective, blood-brain barrier permeable Fyn and GSK-3β inhibitor with IC₅₀ values of 0.044 μM and 0.61 μM, respectively. Fyn-IN-1 significantly downregulates the pro-inflammatory enzyme iNOS. Fyn-IN-1 can be used in the research of neurodegenerative 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.

Multi-kinase-IN-2 (compound 7h) is an orally active and potent angiokinase inhibitor. Multi-kinase-IN-2 exhibits excellent inhibitory activity against angiokinases including VEGFR-1/2/3, PDGFRα/β, and FGFR-1, as well as LYN and c-KIT kinases. Multi-kinase-IN-2 significantly attenuates phosphorylation of AKT and ERK proteins. Multi-kinase-IN-2 induces cell apoptosis. Multi-kinase-IN-2 shows anticancer activity.

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.

PP162 is a selective DNA-dependent protein kinase (DNA-PK) inhibitor with an IC₅₀ of 53 nM. PP162 selectively inhibits DNA-PK by binding to a conserved hydrophobic pocket. PP162 exhibits weak inhibitory activity against various tyrosine kinases and PI3K family members. PP162 can be used for research on selective kinase targeting.

Lck-IN-2 (compound 12a) is an inhibitor of Lymphocyte-specific protein tyrosine kinase (Lck) with IC₅₀ of 10.6 nM. Lck-IN-2 reveals efficacy in colon cancer cells with GI₅₀s of 0.24-1.26 μM. Lck-IN-2 exhibits an apoptotic effect in Colo201 cells.

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.

Antiproliferative agent-54 (Compound 6z) is the inhibitor for multiple kinases, such as ABL WT, B-RAF, EGFR, HCK, LYN A and SRC with IC₅₀ of 6-50 nM. Antiproliferative agent-54 inhibits proliferation of several cancer cell, inhibits HUVEC and HepG2, with EC₅₀ of 34 and 38 nM. Antiproliferative agent-54 exhibits good pharmacokinetic characteristics in rats.

Scr-IN-2 is an effective c-Scr inhibitor with an IC₅₀ of 302 nM. Scr-IN-2 exhibits nanomolar-level anti-breast cancer activity. Scr-IN-2 increases the level of ROS in cells, induces mitochondrial damage, G1 phase arrest, and apoptosis. Scr-IN-2 can be used in the research of breast cancer.

FAK inhibitor 7 is a type of FAK inhibitor with an IC₅₀ value of 3.58 nM. FAK inhibitor 7 can inhibit the downstream signaling cascades of FAK (like Src and AKT), causing ovarian cancer cells to stall in the G0/G1 phase and induce cytotoxic autophagy. FAK inhibitor 7 can also suppress tumor metastasis and growth in ovarian cancer mice.