Src Inhibitor

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.

Masitinib (mesylate) (Standard) is the analytical standard of Masitinib (mesylate). This product is intended for research and analytical applications. Masitinib mesylate (AB-1010 mesylate) is a potent, orally bioavailable, and selective inhibitor of c-Kit (IC50=200 nM for human recombinant c-Kit). It also inhibits PDGFRα/β (IC50s=540/800 nM), Lyn (IC50= 510 nM for LynB), Lck, and, to a lesser extent, FGFR3 and FAK. Masitinib mesylate (AB-1010 mesylate) has anti-proliferative, pro-apoptotic activity and low toxicity.

SB 220025 trihydrochloride is a reversible, orally active, cell-permeable, ATP-competitive and selective human p38 MAPK inhibitor (IC₅₀ = 60 nM). SB 220025 trihydrochloride also inhibits p56^Lck and PKC with IC₅₀ values of 3.5 and 2.89 μM, respectively. SB 220025 trihydrochloride inhibits the expression of IL-8 gene in response to globular adiponectin (gAd), reduces inflammatory cytokine production and inhibits angiogenesis. SB 220025 trihydrochloride effectively prevents the progression of arthritis in a chronic inflammatory disease model and can be used in the study of inflammation.

AD80 (Standard) is the analytical standard of AD80 (HY-101963). This product is intended for research and analytical applications. AD80, a multikinase inhibitor, inhibits RET, RAF,SRCand S6K, with greatly reduced mTOR activity.

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