Src Inhibitor

(R)-LW-Srci-8 is a selective covalent inhibitor of c-Src (IC₅₀= 35.83 nM) that disrupts the autophosphorylation of c-Src by targeting its autophosphorylation site (Y419).

BTK-IN-45 (Compound 6b) is a potent, reversible, and selective BTK inhibitor with an IC₅₀ of 1.14 μM. BTK-IN-45 also exhibits modest inhibition for LCK. BTK-IN-45 can be used in the research of cancers, including leukemia.

Squarunkin A hydrochloride is a potent and selective UNC119-cargo interaction inhibitor (IC₅₀ of 10 nM for inhibiting the UNC119A-myristoylated Src N-terminal peptide interaction). Squarunkin A hydrochloride interferes with the activation of Src kinase in cells.

Lyn peptide inhibitor TFA is a potent and cell-permeable inhibitor of Lyn-coupled IL-5 receptor signaling pathway, while keeping other signals intact. Lyn peptide inhibitor TFA blocks Lyn activation and inhibits the binding of Lyn tyrosine kinase to βc subunit of IL-3/GM-CSF/IL-5 receptors. Lyn peptide inhibitor TFA can be used for study of  asthma, allergic, and other eosinophilic disorders.

AP22161 is a potent and selective Src SH2 domain inhibitor with an IC₅₀ of 0.24 µM. AP22161 exhibits >120-fold selectivity over Yes SH2 (IC₅₀ = 29.38 µM) and ZAP SH2 (IC₅₀ = 421.86 µM). AP22161 inhibits Src-dependent cellular activity and diminishes osteoclast resorptive activity. AP22161 can be used for osteoporosis research.

PROTAC CYP1B1 degrader-2 is a CYP1B1 PROTAC degrader with a DC₅₀ of approximately 0.1 nM. PROTAC CYP1B1 degrader-2 induces ubiquitination and proteasomal degradation of CYP1B1, and forms a ternary complex with VHL ubiquitin ligase and CYP1B1. PROTAC CYP1B1 degrader-2 inhibits P-gp. PROTAC CYP1B1 degrader-2 inhibits FAK/SRC. PROTAC CYP1B1 degrader-2 exhibits anticancer activity against paclitaxel (HY-B0015)-resistant non-small cell lung cancer. PROTAC CYP1B1 degrader-2 can be used in studies related to non-small cell lung cancer.

Antifibrotic agent 1 is an orally active anti-idiopathic pulmonary fibrosis (IPF) agent. Antifibrotic agent 1 effectively attenuates IPF-related processes, including TGF-β induced EMT and FMT processes, as well as pro-fibrotic M2 polarization. Antifibrotic agent 1 selectively inhibits CSF-1R, PDGFR-α and Src family kinases (SFKs), while sparing VEGFRs, FGFRs and Abl to minimize off-target toxicity. Antifibrotic agent 1 has potent anti-fibrotic activity in Bleomycin (BLM) (HY-108345)-induced pulmonary fibrosis mice model.

BJ-2302 is a Src kinase inhibitor with an IC₅₀ of 3.23 μM, and inhibits cathepsin S (CTSS) activity.BJ-2302 binds to Src, suppresses PI3K/AKT and Ras/Raf/ERK pathways, and reduces CTSS and MMP-9 expression.BJ-2302 inhibits cancer cell invasion, metastasis, proliferation, and tumor growth.BJ-2302 does not induce cytotoxicity in normal breast epithelial cells.BJ-2302 can be used for the research of breast cancer and triple-negative breast cancer.

Src Inhibitor 4 (Compound 18) is a derivative of KX-01 and an Src inhibitor. Src Inhibitor 4 can inhibit tumor cells, disrupt microtubules, and induce cell cycle arrest, apoptosis, and immunogenic cell death. After the introduction of phenolic or aniline functionality, Src Inhibitor 4 can serve as a payload attachment site for antibody-drug conjugates and has anti-tumor activity.

PP2 Analog (compound 3) is a ATP-competitive Src family kinases inhibitor with the IC₅₀ values of 0.22, 0.15, 2.68, and 7 aganist of lck (64-509), src , kdr, and tie-2.

NEO212 is an orally active, blood-brain barrier permeable conjugate of Temozolomide (TMZ) (HY-17364) and Perillyl Alcohol (POH) (HY-N7000), with potent anticancer activity. NEO212 overcomes classical TMZ resistance and DNA alkylation by depleting MGMT. By inhibiting the FAK/Src signaling pathway, NEO212 reduces the production of MMP2 and MMP9, induces mesenchymal-epithelial transition, and inhibits the migration, invasion and tumor progression of glioma stem cells. NEO212 disrupts autophagy flux to enhance mitochondrial apoptosis; it induces differentiation of acute myeloid leukemia (AML) cells into macrophages and proliferation arrest.

Multi-kinase-IN-12 is a non-selective multi-target inhibitor, with IC₅₀ values against human targets as follows: Flt3 < 0.001 μM, c-Src 0.002 μM, KDR 0.004 μM, Eph-A2, MNK-1 and Flt1 0.011 μM, Lck 0.016 μM, Rsk1 0.21 μM, and α2 subunit of AMPK 0.041 μM. Multi-kinase-IN-12 can be used in research related to solid tumors.

Dasatinib (monohydrate) (Standard) is the analytical standard of Dasatinib (monohydrate). This product is intended for research and analytical applications. Dasatinib (BMS-354825) monohydrate is a highly potent, ATP competitive, orally active dual Src/Bcr-Abl inhibitor with potent antitumor activity. The Kis are 16 pM and 30 pM for Src and Bcr-Abl, respectively. Dasatinib monohydrate inhibits Bcr-Abl and Src with IC50s of <1.0 nM and 0.5 nM, respectively. Dasatinib monohydrate also induces apoptosis and autophagy.

Src Inhibitor 3 (Compound 7d) is a Src inhibitor with an IC₅₀ of 285 nM. Src Inhibitor 3 inhibits HepG2 cells proliferative with an IC₅₀ of 1.55 μM.

Multi kinase ligand 4 is a target protein ligand used in the synthesis of PROTAC DB-0646 (HY-137343).

N-Deshydroxyethyl Dasatinib-C3-NH2 is an Target Protein Ligand-Linker Conjugate that incorporates a ligand for LCK (HY-107447) and a PROTAC linker (HY-76667), which recruits E3 ligases. N-Deshydroxyethyl Dasatinib-C3-NH2 can be used for synthesis of PROTAC SJ11646 (HY-175281).

Scutellarein (Standard) is the analytical standard of Scutellarein. This product is intended for research and analytical applications. Scutellarein is a natural flavonoid compound with anti-inflammatory effects.

STAT-3/c-Src-IN-1 (Compound 12d) is a dual STAT-3 (IC₅₀=0.844 μM) and c-Src (IC₅₀=0.268 μM) inhibitor. STAT-3/c-Src-IN-1 blocks tumor cell proliferation, migration, and angiogenesis signaling pathways. STAT-3/c-Src-IN-1 exhibits potent anti-proliferative activity against melanoma (SK-MEL-2) and CNS cancer (SNB-75) cell lines (GI₅₀=-5.75 μM and -5.63 μM), inducing tumor cell apoptosis via G0/G1 and G2/M phase cell cycle arrest. STAT-3/c-Src-IN-1 is promising for research of melanoma and glioblastoma.

WH-4-023 GMP is WH-4-023 (HY-12299) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. WH-4-023 (Dual LCK/SRC inhibitor) is a Lck/Src dual target inhibitor with functions in stem cell maintenance and differentiation regulation. WH-4-023 blocks epithelial-mesenchymal transition, supports the self-renewal of porcine embryonic stem cells, and inhibits their differentiation into mesoderm and endoderm. WH-4-023 is a key component of 3i/LAF medium, and enables the stable establishment and long-term maintenance of porcine pre-gastrulation epiblast stem cell lines. Removal of WH-4-023 reduces the expression of pluripotency factors in porcine and human extended pluripotent stem cells. WH-4-023 can be applied to relevant studies such as non-small cell lung cancer resistant to EGFR-TKIs.

Aminogenistein is a p56^lck inhibitor with a 1.2 μM IC₅₀. Aminogenistein inhibits production of Aβ1-40 and Aβ1-42 peptides. Aminogenistein induces accumulation of APP-CTFα and APP-CTFβ, indicating γ-secretase cleavage inhibition. Aminogenistein can be used for the research of alzheimer's disease.