Src Inhibitor

PDD-87 is an orally active, blood-brain barrier permeable kinase inhibitor, with IC₅₀ values ranging from 0.07 nM to 0.72 nM against ABL, SRC family, BTK kinases and their key mutants. PDD-87 induces antiproliferative effects in leukemia and lymphoma cells, and inhibits tumor growth in mouse xenograft models. PDD-87 can be used for the research of leukemia and lymphoma.

Ac-PPPHPHARIK-NH2 (compound S1) is a compound that inhibits the interaction between androgen receptor and Src. It can inhibit the binding of androgen or estrogen-induced receptor and Src in cancer cells, as well as the activation of related signaling pathways, and can also inhibit cell cycle progression and tumor growth.

LCB 03-0110, a thienopyridine derivative, is a potent pan-discoidin domain receptor/c-Src family tyrosine kinase inhibitor. LCB 03-0110 suppresses scar formation by inhibiting fibroblast and macrophage activation.

PP487 is a selective dual inhibitor of Tyrosine kinase/PI3-K, with IC₅₀ values of 0.017 μM, 0.072 μM, 0.004 μM, 0.01 μM, 0.55 μM, 0.22 μM, and < 0.01 μM against DNA-PK, mTOR, Hck, Src, EGFR, EphB4, and PDGFR, respectively. PP487 can be used in cancer research.

Antiangiogenic agent 3 (compound 3) is a potent antiangiogenic agent. Antiangiogenic agent 3 is an inhibitor of human umbilical vein endothelial cells (HUVEC). Antiangiogenic agent 3 inhibits HUVEC migration and chemotactic motilities. Antiangiogenic agent 3 also decreases the gene expression of Src, cdc42, and MAPK.

SI-2 (EPH 116) is an inhibitor for steroid receptor coactivator-3 (SRC-3), which reduces the transcriptional activity and protein concentration of SRC-3 in cells, exhibits cytotoxicity in cancer cell, inhibits migration of MDA-MB-468, induces apoptosis of MDA-MB-468. SI-2 inhibits the tumor growth in mouse models, without significant toxicity for heart and other major organs (20 mg/kg).

eCF506-d₅ (NXP900-d₅) is deuterated labeled eCF506 (HY-112096). eCF506 is a highly potent and orally active YES1/SRC kinase inhibitor with an IC₅₀ of 0.47 nM. eCF506 locks its target into its native “closed” conformation, thereby inhibiting both kinase activity and complex formation with protein partners. eCF506 can be used for the study of esophageal squamous cancer and breast cancer.

Tyrosine kinase-IN-11 (Compound 4b) is a tyrosine kinase inhibitor. Tyrosine kinase-IN-11 decreases general tyrosine kinase activity, selectively inhibits PDGFR-β, SRC, and c-MET kinases. Tyrosine kinase-IN-11 induces apoptosis, accompanied by reduced ERK signalings. Tyrosine kinase-IN-11 exhibits selective anticancer activity against pancreatic cancer and renal cancer.

TX-1918 is an inhibitor for eukaryotic elongation factor 2 kinase (eEF2-K) and Src kinase with IC₅₀ of 0.44 and 4.4 μM, respectively. TX-1918 exhibits cytotoxicity in cell HepG2 and HCT116, with IC₅₀ of 2.07 and 230 μM, respectively. TX-1918 inhibits the C-terminal domain of HIV-1 CA (CA CTD)(IC₅₀ =3.81 μM), and inhibits the viral replication (IC₅₀ =15.16 μM).

CHMFL-ABL-053 (Compound 18a) is a potent, selective, and orally available BCR-ABL, SRC and p38 kinase inhibitor with IC₅₀ values of 70, 90 and 62 nM against ABL1, SRC and p38, respectively.

Excisanin A is a potent anticancer agent. Excisanin A inhibits cell proliferation, migration, adhesion and invasion. Excisanin A decreases the expression of MMP-2, MMP-9, p-FAK, p-Src, integrin β1 protein. Excisanin A has the potential for the research of breast cancer.

BMS-358233 (compound 3) is a Lck inhibitor (IC₅₀: 1 nM; Ki: 540 pM) and inhibits T cell proliferation (IC₅₀: 262 nM).

SKS-927 is a Src kinase inhibitor, with an IC₅₀ value of 3.9 nM. SKS-927 inhibits the proliferation of Src-transformed rat fibroblasta, with an IC₅₀ value of 73 nM. SKS-927 exhibits an IC₅₀ value of 720 nM against EGFR. SKS-927 can be used for the study of cancer and osteoporosis.

Scr-IN-1 (Compound 4e) is a Tyrosine kinase inhibitor. Scr-IN-1 inhibits HCT-116 cells and MIA-PaCa-2 cells with IC₅₀s of 0.16 μM and 1.16 μM, respectively. Scr-IN-1 displays selectivity profile on HCT-116 cells and MIA-PaCa-2 cells with SI > 625 and SI > 86, respectively. Scr-IN-1 induces Apoptosis in HCT-116 colon cancer cell and does not cause any change in the rate of necrotic cells. Scr-IN-1 is a novel SRC kinase inhibitor candidate for HCT-116 cells. Scr-IN-1 is potential for cancer research.

SRT6 is a CD44 inhibitor. SRT6 exerts antiproliferative activity in CD44⁺ breast cancer and lung cancer cells. SRT6 inhibits CD44-associated SRC kinase, as well as EGFR, ERBB2, ERBB4, MAP3K10 and MAPKAPK2. SRT6 can be used for the research of breast cancer and lung cancer.

Atractylenolide II (Standard) is the analytical standard of Atractylenolide II. This product is intended for research and analytical applications. Atractylenolide II (Asterolide) is a sesquiterpenoid compound. Atractylenolide II can induce G1 phase cell cycle arrest and apoptosis in B16 melanoma cells. Atractylenolide II is an orally effective anticancer agent that can exert anti-melanoma effects by inhibiting the STAT3 signaling pathway. In addition, Atractylenolide II has been shown to ameliorate myocardial fibrosis, oxidative stress, and neuroprotective activity.

TOP1362 is a narrow spectrum kinase inhibitor. TOP1362 is a potent inhibitor of P38-α and Syk kinases with K_d values of 26 and 18 nM, respectively and an IC₅₀ of 14 nM in the Src kinase activity assay. TOP1362 potently inhibits P38-α, Src and Syk. TOP1362 can be used in the research of dry eye syndrome.

K882 (Compound 4e) is a Src inhibitor, with K_D of 0.315 μM. K882 induces Apoptosis. K882 inhibits XIAP and Survivin. K882 inhibits the activation of PI3K/Akt/mTOR, Jak1/Stat3, Ras/MAPK signaling pathways. K882 shows anti-tumor activity against non-small cell lung cancer.

Protein kinase inhibitor 11 (Compound I-96) is a protein kinase inhibitor that can inhibit the activity of PIM-1, CDK-2, GSK-3, and SRC. Protein kinase inhibitor 11 holds promise for research in cancer, immune disorders, and neurodegenerative diseases.

c-Src Kinase-IN-1 is a highly selective, cell-permeable inhibitor of c-Src kinase that suppresses cancer cell growth. c-Src Kinase-IN-1 has a K_i of 44 nM and a K_d value of 86 nM against chicken-derived c-Src. c-Src Kinase-IN-1 interacts with the phosphate-binding loop of c-Src and exhibits selectivity toward homologous Src family kinases and c-Abl. c-Src Kinase-IN-1 can be used in cancer-related research.