Src Inhibitor

Ponatinib (hydrochloride) (Standard) is the analytical standard of Ponatinib (hydrochloride). This product is intended for research and analytical applications. Ponatinib hydrochloride (AP24534 hydrochloride) is a hydrochloride of ponatinib. Ponatinib is an orally active multi-targeted kinase inhibitor with IC50s of 0.37 nM, 1.1 nM, 1.5 nM, 2.2 nM, and 5.4 nM for Abl, PDGFRα, VEGFR2, FGFR1, and Src, respectively.

BMS-243117 is a potent, and selective benzothiazole based p56^Lck inhibitor with an IC₅₀ of 4 nM. BMS-243117 inhibits anti-CD3/anti-CD28 induced PBL (human peripheral blood T-cells) proliferation with an IC₅₀ of 1.1 μM. BMS-243117 binds in an extended conformation to the ATP-binding site of Lck.

Protein kinase inhibitor 13 (Compound I-90) is the inhibitor for protein kinase that exhibits inhibitory effects on kinases such as PIM-1, CDK-2, GSK-3 and SRC.

Pelitinib (Standard) is the analytical standard of Pelitinib. This product is intended for research and analytical applications. Pelitinib (EKB-569;WAY-EKB 569) is an irreversible inhibitor of EGFR with an IC50 of 38.5 nM; also slightly inhibits Src, MEK/ERK and ErbB2 with IC50s of 282, 800, and 1255 nM, respectively.

ENMD-2076 Tartrate (Standard) is the analytical standard of ENMD-2076 (Tartrate) (HY-10987). This product is intended for research and analytical applications. ENMD-2076 Tartrate is a multi-targeted K_inase inhibitor with IC₅₀s of 1.86, 14, 58.2, 15.9, 92.7, 70.8, 56.4 nM for Aurora A, Flt3, K_dR/VEGFR2, Flt4/VEGFR3, FGFR1, FGFR2, Src, PDGFRα, respectively.

Saracatinib (Standard) is the analytical standard of Saracatinib. This product is intended for research and analytical applications. Saracatinib (AZD0530) is a potent Src family inhibitor with IC50s of 2.7 to 11 nM for c-Src, Lck, c-YES, Lyn, Fyn, Fgr, and Blk. Saracatinib shows high selectivity over other tyrosine kinases.

SIK1-IN-1 (Compound 27) is a selective Salt-inducible kinase 1 (SIK1) inhibitor with an IC₅₀ of 0.7  nM for SIK1 over SIK2 and SIK3. SIK1-IN-1 has no cytotoxicity against HEK293 cells and PBMCs (maximum concentration of 30 μM). SIK1-IN-1 also has potent inhibitory activities for 392 kinases, in particular tyrosine kinases, such as FGR, HCK and LYN).

proMMP-9 inhibitor-3c (compound 3c) is a potent proMMP-9 inhibitor. proMMP-9 inhibitor-3c is specific for binding to the proMMP-9 hemopexin-like domain (K_d=320 nM). proMMP-9 inhibitor-3c disruption of MMP-9 homodimerization prevents association of proMMP-9 with both α4β1 integrin and CD44 and results in the dissociation of EGFR. This disruption results in decreased phosphorylation of Src and its downstream target proteins focal adhesion kinase (FAK) and paxillin (PAX).

PD173955 (Standard) is the analytical standard of PD173955 (HY-10395). This product is intended for research and analytical applications. PD173955 is an orally active inhibitor of Src (IC₅₀= 22 nM), Yes, Abl, ATP and MAP kinases. PD173955 can effectively prevent the mitotic process and has anticancer activity.

ON012380 is a kinase inhibitor with an IC₅₀ of 9 nM against BCR-ABL. As a substrate-competitive BCR-ABL inhibitor, ON012380 binds to a non-ATP site, and inhibits the kinase activities of PDGFR, Fyn and LynB at higher concentrations. ON012380 induces apoptosis, inhibits STAT-5 phosphorylation, reduces cell viability and suppresses cell growth in leukemia cells. ON012380 can be used in the research of chronic myeloid leukemia and Imatinib (HY-15463)-resistant chronic myeloid leukemia.

Hibarimicin C is a tyrosine kinase inhibitor. Hibarimicin C selectively inhibits the activity of src tyrosine kinase without affecting protein kinase A and C. Hibarimicin C also has moderate anti-Gram-positive bacteria activity with a MIC of 0.8-12.56 μg/mL.

Masitinib (Standard) is the analytical standard of Masitinib. This product is intended for research and analytical applications. Masitinib (AB1010) 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 (AB1010) has anti-proliferative, pro-apoptotic activity and low toxicity.

Hibarimicin B (Angelmicin B) is a tyrosine kinase inhibitor. It selectively inhibits the activity of src tyrosine kinase without affecting protein kinase A and C. It also has moderate anti-Gram-positive bacteria activity with a MIC of 0.8-12.56 μg/mL.

Herbimycin B is an ansamycin antibiotic that acts as a Src family kinase inhibitor. Herbimycin B has herbicidal effect on most monocotyledons and dicotyledons, inhibits the activity of tobacco Mosaic virus (TMV), HeLa cells and Ehrlich cells.

Hydroxymethyl dasatinib (M24), a benzylhydroxy metabolite of Dasatinib (HY-10181), exhibits an IC₅₀ of 46.7nM in K562 CML cells.

KX2-361 (Standard) is the analytical standard of KX2-361 (HY-111187). This product is intended for research and analytical applications. KX2-361 (KX-02) is a Src-K_inase and tubulin polymerization inhibitor. KX2-361 shows good oral bioavailability and readily crosses the BBB in mice. KX2-361 shows anti-tumor activity and induces apoptosis of Glioblastoma (GBM) cell.

Saracatinib (difumarate) (Standard) is the analytical standard of Saracatinib (difumarate). This product is intended for research and analytical applications. Saracatinib (AZD0530) difumarate is a potent Src inhibitor with IC50 values of 2.7-11 nM for c-Src, Lck, c-YES, Lyn, Fyn, Fgr and Blk, and is selective for other tyrosine kinases. .

Hibarimicin D is a tyrosine kinase inhibitor. Hibarimicin D selectively inhibits the activity of src tyrosine kinase without affecting protein kinase A and C. Hibarimicin D also has moderate anti-Gram-positive bacteria activity with a MIC of 0.8-12.56 μg/mL.