Src Inhibitor

Lck-IN-3 (compound 7m) is an LCK inhibitor targeting acute lymphoblastic leukemia (ALL) that inhibits LCK phosphorylation. Lck-IN-3 can induce cell cycle arrest in the G2/M phase, leading to apoptosis in ALL cells.

ARN25699 is a kinase inhibitor with an IC₅₀ of 5.5 nM against GSK-3β, 2.2 nM against FYN-α, and 242.3 nM against DYRK1A, and it exhibits oral bioavailability. ARN25699 reduces hyperphosphorylation of tau protein and promotes microtubule bundle formation. ARN25699 has a broader kinome inhibitory profile and targets kinases associated with the pathogenic mechanisms linked to Alzheimer's disease. ARN25699 can be used in the research of Alzheimer's disease and related tauopathies.

Cisplatin/Dasatinib prodrug-1 (Compound 3) is a prodrug of Cisplatin (HY-17394) and Dasatinib (HY-10181). Cisplatin/Dasatinib prodrug-1 exhibits antiproliferative activity against A2780, MDA-MB-231, MCF7, HCT116, RD, Thp1 and HL60 cancer cells with IC₅₀s of 0.1, 0.1, 0.36, 2.0, 0.4, 0.3 and 0.25 μM, respectively.

Multi-kinase-IN-1 (Compound 11k) is a potent kinase inhibitor with antitumor activity. Multi-kinase-IN-1 induces cell apoptosis, and can be studied for colorectal cancer.

LDDN-0003499 is a Src family tyrosine kinase inhibitor and anti-inflammatory agent. LDDN-0003499 reduces basal and Aβ-stimulated levels of active, phosphorylated Lyn and Src kinases, and attenuates Aβ-stimulated secretion of pro-inflammatory cytokines TNFα and IL-6 in microglial cells. LDDN-0003499 can be used for the research of Alzheimer's disease.

HL403 is a potent and dual BRD4/Src inhibitor. HL403 has IC₅₀ values of 133 nM for BRD4 inhibition and 4.5 nM for Src inhibition. HL403 shows anti-cancer activity.

N-Acetyl-O-phosphono-Tyr-Glu dipentylamide (Ac-Tyr-Glu-N(n-C₅H₁₁)₂), a dipeptide, is a pp60^c-src SH2 domain inhibitor. N-Acetyl-O-phosphono-Tyr-Glu dipentylamide can be used for cancer research.

Ac-Tyr(PO3H2)-Glu-Glu-Ile-Glu-OH TFA (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 TFA is an inhibitor for src SH3-SH2:phosphoprotein interactions.

AP-24567 is a Ligands for Target Protein for PROTAC, which can be used for the synthesis of SB1-G-187 (HY-137342).

Birelentinib (DZD8586) is an orally effective, selective, non-covalent inhibitor targeting LYN tyrosine kinase and BTK tyrosine kinase, capable of penetrating the blood-brain barrier. Birelentinib exhibits concentration-dependent antiproliferative effects in RI-1 cells and diffuse large B-cell lymphoma (DLBCL) cell lines carrying BTK resistance mutations (such as C481X, V416L, etc.). Birelentinib blocks both BTK-dependent and independent signaling of the B-cell receptor (BCR), thereby inhibiting tumor cell proliferation and inducing cell death. Birelentinib can be used in research to overcome resistance to existing covalent and non-covalent BTK inhibitors in B-cell non-Hodgkin lymphoma (B-NHL).

P60v-src(137-157) is a synthetic peptide that inhibits the tyrosine kinase activity of p60^v-src (IC₅₀: 7.5 μM).

HPK1-IN-61 (Compound 1) is an inhibitor of hematopoietic progenitor kinase 1 (HPK1) (K_i = 0.4 nM) and an inhibitor of Abl (IC₅₀ < 0.51 nM). HPK1-IN-61 also shows inhibitory activity against LCK with an IC₅₀ of 24 nM.

Tesevatinib (XL-647) tosylate is an orally available, blood-brain barrier-penetrant inhibitor of the epidermal growth factor receptor (EGFR). Tesevatinib tosylate significantly reduces cellular viability, with IC₅₀ values of 11 nM and 102 nM in GBM12 and GBM6, respectively. Tesevatinib tosylate also inhibits HER2 (IC₅₀=16.1 nM), VEGFR2 (IC₅₀=1.5 nM), and Src (IC₅₀=10.3 nM). Tesevatinib tosylate can inhibit tumor proliferation and exhibits antitumor activity.

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

Hck-IN-3 (compound 2D) is an orally effective inhibitor targeting HCK (K_D = 3.92 μM). Hck-IN-3 can inhibit the release of NO. Hck-IN-3 has an IC₅₀ of 6.52 μM in RAW264.7 cells. Hck-IN-3 can inhibit the release of TNF-α, IL-6, and IL-1β in a concentration dependent manner. Hck-IN-3 downregulates the protein expression of NLRP3, ASC, pro-caspase-1, and pro-IL-1β in a concentration dependent manner. Hck-IN-3 can be used for research on acute non traumatic inflammatory conditions.

Antiallergic agent-1, a Src-family kinase inhibitor, may serve as a new valuable lead compound for future antiallergic agent discovery. Antiallergic agent-1 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

MLS-2384 free base is a dual JAK/Src kinase inhibitor. MLS-2384 free base downregulates STAT3 downstream proteins c-Myc and Mcl-1. MLS-2384 free base induces Apoptosis. MLS-2384 free base exhibits anticancer activity against prostate cancer, breast cancer, skin cancer, ovarian cancer, lung cancer, and liver cancer.

Hck-IN-2 (Compound 8e) is an HCK inhibitor. Hck-IN-2 is cytotoxic to tumor cells, with IC₅₀ values of 19.58 μM and 1.42 μM against MDA-MB231 and MCF-7, respectively. Hck-IN-2 has anti-tumor activity.

Multi-target kinase-IN-15 is a multi-target kinase inhibitor that simultaneously inhibits kinases such as the PI3K family, mTOR, DNA-PK, and Src. Multi-target kinase-IN-15 competitively binds to the ATP pockets of multiple kinases, simultaneously blocking PI3K, mTOR, DNA-PK, and Src kinase signaling to achieve synergistic inhibition. PI3K-IN-16 can be used for research related to PI3K-mediated diseases, such as cancer.

c-Met-IN-32 is an orally active c-Met inhibitor with an IC50 of 18 nM, blocking autophosphorylation and downstream PI3K/AKT and RAS/ERK signaling pathways. c-Met-IN-32 inhibits MER, FYN, and SRC kinases. c-Met-IN-32 induces apoptosis, inhibits migration and invasion, suppresses the proliferation of MET-amplified cancer cells, and exhibits selectivity against non-MET-dependent cancer cell lines. c-Met-IN-32 can be used for research on non-small cell lung cancer.