Src Inhibitor

FITC-amide-C2 Lck inhibitor 2 is a FITC-labeled Lck inhibitor.

A-770041 (Standard) is the analytical standard of A-770041 (HY-11011). This product is intended for research and analytical applications. A-770041 is a selective and orally active Src-family Lck inhibitor. A-770041 inhibits Lck with an IC₅₀ value of 147 nM with the presence of 1 mM ATP. A-770041 shows 300-fold selective to Lck over Fyn, the other Src family K_inase involved in T-cell signaling. A-770041 can be used for the research of acute rejection.

Dasatinib (hydrochloride) (Standard) is the analytical standard of Dasatinib (hydrochloride). This product is intended for research and analytical applications. Dasatinib (BMS-354825) hydrochloride 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 hydrochloride inhibits Bcr-Abl and Src with IC50s of <1.0 nM and 0.5 nM, respectively. Dasatinib hydrochloride also induces apoptosis and autophagy.

Src Inhibitor 1 (Standard) is the analytical standard of Src Inhibitor 1 (HY-101053). This product is intended for research and analytical applications. Src Inhibitor 1 is a potent, ATP-competitive and selective dual site Src tyrosine kinase inhibitor with IC50 values of 44 nM for Src and 88nM for Lck.

Elzovantinib (Standard) is the analytical standard of Elzovantinib (HY-111787). This product is intended for research and analytical applications. Elzovantinib (TPX-0022) is an oral-active inhibitor of SRC, MET and c-FMS, with IC₅₀ values of 0.12 nM, 0.14 nM and 0.76 nM for SRC, MET and c-FMS respectively.

KB SRC 4 (Standard) is the analytical standard of KB SRC 4 (HY-108488). This product is intended for research and analytical applications. KB SRC 4 is a potent, and highly selective c-Src inhibitor, with a K_i of 44 nM and a K_d of 86 nM, and shows no inhibition on c-Abl up to 125 μM; KB SRC 4 has antitumor activity.

Bafetinib (Standard) is the analytical standard of Bafetinib. This product is intended for research and analytical applications. Bafetinib is an orally active Lyn/Bcr-Abl tyrosine kinase inhibitor. Bafetinib enhances the activity of several pro-apoptotic Bcl-2 homology (BH) 3-pure proteins (Bim, Bad, Bmf, and Bik) through intrinsic apoptotic pathways regulated by the Bcl-2 family, and induces apoptosis of Ph+ leukemia cells. Bafetinib has antitumor activity.

RK-24466 (Standard) is the analytical standard of RK-24466 (HY-108318). This product is intended for research and analytical applications. RK-24466 (K_iN 001-51) is a potent and selective Lck inhibitor; inhibits Lck (64-509) and LckCD isoforms with IC₅₀s of less than 1 and 2 nM, respectively.

CGP062464 is an inhibitor of the tyrosine kinase c-Src (IC₅₀: < 50 nM). CGP062464 can be used for research of osteoporosis and tumor-induced hypercalcemia.

PF 477736 (Standard) is the analytical standard of PF 477736 (HY-10032). This product is intended for research and analytical applications. PF 477736 (PF 00477736) is a potent, selective and ATP-competitive inhibitor of Chk1, with a Ki of 0.49 nM, it is also a Chk2 inhibitor, with a Ki of 47 nM. PF 477736 shows <100-fold selectivity for Chk1 over VEGFR2, Fms, Yes, Aurora-A, FGFR3, Flt3, and Ret (IC50=8 (Ki), 10, 14, 23, 23, 25, and 39 nM, respectively). PF 477736 can enhance Gemcitabine antitumor activity in vitro and in vivo.

5-O-Methylvisammioside (4'-O-β-D-Glucosyl-5-O-methylvisamminol) (Standard) is the analytical standard of 5-O-Methylvisammioside. This product is intended for research and analytical applications. 5-O-Methylvisammioside is an orally active natural chromone glycoside and multiple biological activities. 5-O-Methylvisammioside inhibits ferroptosis by activating the Nrf2/HO-1 signaling axis. 5-O-Methylvisammioside alleviates intestinal barrier damage by inhibiting the ROS/NF-κB/NLRP3 pathway. 5-O-Methylvisammioside exerts a protective effect against acute liver injury by reducing ALT/AST, decreasing inflammatory infiltration, and inhibiting IκB-α phosphorylation and NF-κB nuclear translocation. 5-O-Methylvisammioside blocks the HMGB1/RAGE/MEK/ERK signaling axis to exert anti-tumor and anti-angiogenic effects. 5-O-Methylvisammioside improves depression-like behaviors by inhibiting Src kinase and the NF-κB pathway.

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

2,3,4,6,8-Pentahydroxy-1-methylxanthone is a xanthone derivative of Wardomyces anomalus. 2,3,4,6,8-Pentahydroxy-1-methylxanthone shows significant antioxidant activities. 2,3,4,6,8-Pentahydroxy-1-methylxanthone is inhibitors of p56lck tyrosine kinase. 2,3,4,6,8-Pentahydroxy-1-methylxanthone can be used to research cardiovascular disease.

Multi-kinase-IN-11 (Compound 1a) is a DFG-out conformation-targeted multi-kinase inhibitor, including SRC, LCK, ABL, PYK2, CSK, HCK, P38 and C-KIT. Multi-kinase-IN-11 serves as a scaffold for the preparation of fluorescently labeled binding probes and affinity matrices.

PP121 (Standard) is the analytical standard of PP121 (HY-10372). This product is intended for research and analytical applications. PP121 is a multi-targeted kinase inhibitor with IC₅₀s of 10, 60, 12, 14, 2 nM for mTOR, DNK-PK, VEGFR2, Src, PDGFR, respectively.

Tirbanibulin (Standard) is the analytical standard of Tirbanibulin. This product is intended for research and analytical applications. Tirbanibulin (KX2-391) is an inhibitor of Src that targets the peptide substrate site of Src, with GI50 of 9-60 nM in cancer cell lines.

AP22408 is a nonpeptide inhibitor against Src SH2 with an IC₅₀ value of 0.3 μM. AP22408 inhibits rabbit osteoclast-mediated resorption of dentine, exhibits bone-targeting properties based on a hydroxyapatite adsorption assay and demonstrates in vivo antiresorptive activity in a parathyroid hormone-induced rat model. AP22408 is proming for rasearch of osteoporosis and other bone-related diseases such as Paget’s disease, osteolytic bone metastasis and hypercalcemia associated with malignancy.

TG 100572 hydrochloride (Standard) is the analytical standard of TG 100572 hydrochloride (HY-10185). This product is intended for research and analytical applications. TG 100572 Hydrochloride is a multi-targeted kinase inhibitor which inhibits receptor tyrosine kinases and Src kinases; has IC₅₀s of 2, 7, 2, 16, 13, 5, 0.5, 6, 0.1, 0.4, 1, 0.2 nM for VEGFR1, VEGFR2, FGFR1, FGFR2, PDGFRβ, Fgr, Fyn, Hck, Lck, Lyn, Src, Yes, respectively.

Si306 is a Src inhibitor with antitumor activity. Si306 reduces the phosphorylation of focal adhesion kinase (FAK) and the expression of epidermal growth factor receptor (EGFR), and inhibits the invasion of human glioblastoma (GBM).

Rhodomycin A can suppress lung cancer cell progression via modulating Src-related pathways.?Rhodomycin A significantly suppressed cancer cell proliferation, migration, invasion, and clonogenicity in vitro and tumour growth in vivo.