-
Src/c-Abl inhibitor
1-Naphthyl PP1 hydrochloride is a selective inhibitor of src family kinases v-Src and c-Fyn as well as the tyrosine kinase c-Abl (IC50 values are 1.0, 0.6, 0.6, 18 and 22 μM for v-Src, c-Fyn, c-Abl, CDK2 and CAMK II respectively). -
Src kinase inhibitor
7-Hydroxychromone is a Src kinase inhibitor with an IC50 of <300 μM. -
fMLP inhibitor
Larixol is an fMLP inhibitor that also suppresses key signaling pathways involved in immune regulation, including Src kinase, ERK1/2, p38, and AKT phosphorylation. It disrupts the interaction between the βγ subunit of the fMLP receptor Gi protein and downstream effectors, thereby inhibiting fMLP-induced respiratory burst. Larixol effectively inhibits fMLP (0.1 μM)-induced superoxide anion production (IC50: 1.98 μM), cathepsin G release (IC50: 2.76 μM), and neutrophil chemotaxis. It mitigates neutrophil hyperactivation and helps reduce inflammation and tissue damage. Additionally, Larixol derivatives have shown inhibitory activity against TRPC6 functional mutants associated with focal segmental glomerulosclerosis (FSGS). -
multi-kinase PROTAC degrader
SB1-G-187 is a multifunctional PROTAC designed as a multi-kinase degrader, capable of inducing the selective degradation of multiple kinase targets through the ubiquitin–proteasome system. In addition to its targeted degradation activity, SB1-G-187 features an alkyne functional group, enabling its use as a click chemistry reagent. It can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAC) with azide-containing molecules, allowing for versatile applications in chemical biology, such as probe development, conjugation, and target identification. -
PROTAC c-Src kinase degrader
DAS-5-oCRBN is a selective and potent PROTAC degrader of c-Src kinase, acting through CRBN-mediated ubiquitination. It effectively reduces c-Src levels and inhibits proliferation in c-Src-dependent cancer cell lines, making it a useful tool for targeted protein degradation research. -
Src/Akt Inhibitor
Chrysotoxine is a dual inhibitor of the Src and Akt signaling pathways. It effectively suppresses cancer stem cell phenotypes by down-regulating the Src/Akt pathway, leading to reduced cell viability and increased apoptosis in H460 and H23 cancer cell lines, while sparing non-tumor cell lines. Due to its rapid excretion and low bioavailability in animal studies, Chrysotoxine serves as a valuable tool in cancer research, particularly for investigating therapies targeting cancer stem cells. -
Src Inhibitor
Si306 is a selective Src inhibitor known for its antitumor properties. It effectively reduces the phosphorylation of focal adhesion kinase (FAK) and downregulates the expression of epidermal growth factor receptor (EGFR), thereby inhibiting the invasion of human glioblastoma (GBM) cells. This compound is valuable for research focused on understanding Src-related signaling pathways and developing targeted cancer therapies. -
Src Kinase Inhibitor
SKS-927 is a potent Src kinase inhibitor with an IC50 value of 3.9 nM, demonstrating significant inhibition of Src-transformed cell proliferation in rat fibroblasts, with an IC50 of 73 nM. Additionally, SKS-927 shows activity against EGFR at an IC50 of 720 nM. This compound is applicable in research focused on cancer and osteoporosis, making it a valuable tool for investigating therapeutic pathways in these conditions. -
Src Inhibitor
β-Hydroxyisovalerylshikonin is a natural product derived from Lithospermum erythrorhizon, functioning as a potent Src inhibitor. It exhibits significant inhibitory activity against protein tyrosine kinases, with IC50 values of 0.7 μM for EGFR and 1 μM for the v-Src receptor. This compound demonstrates broad anticancer activity, particularly inducing cell death in various tumor cell lines, most notably in NCI-H522 and DMS114 cells, making it a valuable tool for cancer research applications. -
Src Inhibitor
Peruvoside is a potent Src inhibitor that also targets PI3K, JNK, STAT, and EGFR pathways. This compound induces apoptosis and autophagy, demonstrating a broad spectrum of anticancer activity in various cancers, including breast, lung, liver, and leukemia. Additionally, Peruvoside exhibits significant antiviral activity against positive-sense RNA viruses and can sensitize Gefitinib-resistant tumor cells, such as A549, PC9/gef, and H1975, to Gefitinib treatment. -
Src/Tubulin Inhibitor
KX2-361 is an inhibitor of Src-kinase and tubulin polymerization. This compound exhibits significant anti-tumor activity and induces apoptosis in glioblastoma (GBM) cells. With good oral bioavailability and the ability to cross the blood-brain barrier in murine models, KX2-361 is a valuable tool for investigating Src-related signaling pathways and therapeutic strategies in cancer research. -
Src/Abl tyrosine kinase inhibitor
Bosutinib hydrate is an orally active Src/Abl tyrosine kinase inhibitor, demonstrating IC50 values of 1.2 nM and 1 nM for Src and Abl, respectively. This compound effectively disrupts signaling pathways involved in cell proliferation and survival, making it valuable for research in cancer biology, particularly in the study of chronic myeloid leukemia (CML) and other malignancies characterized by aberrant Src/Abl activity. Its potent inhibitory profile supports investigations into therapeutic interventions targeting these kinases. -
Src/Abl Inhibitor
Pro-Dasatinib is a potent Src/Abl kinase inhibitor that functions as an amino acid analog of Dasatinib. It exhibits significant antiproliferative activity against K652 leukemia cancer cells, with an IC50 of 0.21 nM. This compound serves as a valuable tool for research in cancer biology and therapeutic development, particularly in understanding and targeting pathways associated with leukemogenesis. -
Src-Abl Inhibitor
AP 24149 is a potent Src-Abl dual inhibitor that targets the Src and Abl kinases, exhibiting IC50 values of 9.1 nM and 3.6 nM, respectively. This compound demonstrates significant inhibitory activity against these kinases, making it a valuable tool for research in cancer biology and signal transduction. It is particularly useful in studies exploring the mechanisms of oncogenesis and therapeutic interventions in Src- and Abl-related malignancies. -
BCR-ABL/SRC/p38 Inhibitor
CHMFL-ABL-053 is a potent, selective inhibitor targeting BCR-ABL, SRC, and p38 kinases, exhibiting IC50 values of 70 nM, 90 nM, and 62 nM, respectively. This compound demonstrates significant antiproliferative activity, making it a valuable tool in cancer research, particularly in studies focusing on chronic myeloid leukemia and related malignancies. Its oral bioavailability enhances its utility in in vivo research applications. -
c-Src/Abl Inhibitor
BCR-ABL-IN-13 is a dual inhibitor of c-Src and Abl, exhibiting a Ki value of 0.55 μM against c-Src and 0.10 μM against wild-type Abl, with a Ki of 0.40 μM against the drug-resistant AblT315I mutant. This compound demonstrates competitive to mixed-type inhibition of wild-type Abl and non-competitive inhibition of the AblT315I mutant. BCR-ABL-IN-13 is suitable for research applications related to chronic myeloid leukemia, particularly in studies targeting resistant forms of the disease. -
SRC Inhibitor
SI-2 is a selective inhibitor of steroid receptor coactivator-3 (SRC-3), effectively reducing both its transcriptional activity and protein levels in cells. This compound exhibits significant cytotoxicity against cancer cells and inhibits the migration of MDA-MB-468 breast cancer cells, promoting apoptosis in these cells. In vivo studies demonstrate that SI-2 suppresses tumor growth in mouse models while showing minimal toxicity to the heart and other vital organs at a dosage of 20 mg/kg. -
IGF-1R/SRC Inhibitor
IGF-1R/SRC-IN-1 is a selective inhibitor targeting insulin-like growth factor 1 receptor (IGF-1R) and SRC. This compound demonstrates an IC50 value of 63 μM for IGF-1R, making it a valuable tool in the study of signal transduction pathways involved in cancer and metabolic disorders. Its application extends to evaluating the role of IGF-1R and SRC in cellular proliferation, differentiation, and survival, providing insights into potential therapeutic interventions for related diseases. -
Lck/Src/KDR/VEGF2R/Tie-2/BLK/Csk/Fyn/Lyn Inhibitor
RK-20448 is an ATP-competitive inhibitor targeting Lck, Src, KDR/VEGF2R, and Tie-2, demonstrating IC50 values of 0.24, 1.19, 10.74, and 5.85 µM, respectively. Additionally, it inhibits BLK, Csk, Fyn, and Lyn, with IC50 values of 0.37, 4.27, 2.03, and 0.43 µM, respectively. This compound is valuable for research involving signal transduction pathways mediated by receptor tyrosine kinases and may contribute to studies on cancer and vascular biology. -
SRC/Raf/VEGFR2 Inhibitor
SKLB646 is a multi-target kinase inhibitor with a focus on SRC, Raf, and VEGFR2. It exhibits potent inhibitory activity against SRC and VEGFR2, with IC50 values of 0.002 μmol/L and 0.012 μmol/L, respectively, as well as significant effects on B-Raf and C-Raf. SKLB646 disrupts SRC signaling and inhibits the MAPK pathway by targeting Raf kinases, leading to decreased proliferation, migration, and invasion in human umbilical vein endothelial cells (HUVEC), thereby impeding tumor-induced angiogenesis. It also demonstrates significant anti-proliferative and anti-survival effects on triple-negative breast cancer (TNBC) cell lines, making it a valuable tool for cancer research. -
Src Inhibitor
Saracatinib difumarate is a selective Src inhibitor, effectively targeting multiple Src family kinases, including c-Src, Lck, c-YES, Lyn, Fyn, Fgr, and Blk, with IC50 values ranging from 2.7 to 11 nM. This compound demonstrates significant potential in modulating signaling pathways associated with cancer and other diseases driven by Src family kinases. It is commonly utilized in research focusing on cancer biology, cell signaling, and the development of targeted therapies. -
Src
3'-Demethylnobiletin is a flavonoid derivative that targets the Src kinase. This compound has demonstrated notable anticancer activity by inhibiting tumor angiogenesis through modulation of Src, FAK, and STAT3 signaling pathways. It is useful in cancer research for studying mechanisms of tumor growth and progression. -
RET/BRAF/S6K/Src Inhibitor
AD57 is an orally active multikinase inhibitor that targets RET, BRAF, S6K, and Src, effectively reducing mTOR activity. This compound demonstrates significant biological activity by interfering with critical signaling pathways involved in cancer proliferation and survival. AD57 is suitable for research applications focused on cancer biology and therapeutic development against malignancies driven by these kinases. -
Src SH2 Inhibitor
pYEEI is a phosphotyrosine-containing tetrapeptide that selectively inhibits the Src SH2 domain with a Kd of 100 nM and an IC50 of 6.5 μM. This compound is pivotal for studying the role of Src signaling pathways in cancer biology and can aid in the development of targeted therapies. Its ability to modulate Src activity makes pYEEI a valuable tool for researchers investigating tumorigenesis and related processes. -
SRC-3 Inhibitor
SRC-3-IN-2 is a selective inhibitor of steroid receptor coactivator 3 (SRC-3), demonstrating potent antitumor activity. This compound is utilized in research focusing on cancer biology and hormone receptor signaling pathways. Its ability to modulate SRC-3 activity makes it a valuable tool for studying SRC-3's role in tumorigenesis and therapeutic resistance. -
Src inhibitor
Fenlean is a natural squamosamide derivative that acts as a Src tyrosine kinase inhibitor. It demonstrates the ability to inhibit over-activated microglia, thereby providing protective effects on dopaminergic neurons. Its anti-inflammatory properties support its potential application in the study and treatment of neuroinflammation in models of Parkinson's disease. -
Control Substrate For c-Src Assay
Tyrosine Kinase Peptide 1 serves as a control substrate specifically designed for c-Src assay applications. Its primary mechanism involves interacting with c-Src kinase, facilitating the assessment of kinase activity. This peptide is critical for validating experimental conditions and ensuring accurate measurement of c-Src-mediated phosphorylation events in biological research. -
Src Inhibitor
LDDN-0003499 is a Src family tyrosine kinase inhibitor that exhibits anti-inflammatory properties. This compound effectively reduces both basal and amyloid-beta (Aβ)-stimulated levels of active phosphorylated Lyn and Src kinases, leading to diminished secretion of pro-inflammatory cytokines such as TNFα and IL-6 in microglial cells. LDDN-0003499 is particularly valuable for research focused on the pathophysiology of Alzheimer's disease. -
pp60c-src SH2 Domain Inhibitor
N-Acetyl-O-phosphono-Tyr-Glu dipentylamide is an inhibitor of the pp60c-src SH2 domain. Its primary biological activity involves modulating signaling pathways associated with cancer progression and metastasis. This compound is valuable for research applications aimed at understanding Src family tyrosine kinases and developing targeted cancer therapies. -
p60v-src Inhibitor
P60v-src(137-157) is a synthetic peptide specifically designed to inhibit the tyrosine kinase activity of the p60v-src protein, exhibiting an IC50 value of 7.5 μM. This peptide serves as a valuable tool in research related to cancer biology and signal transduction pathways, allowing for investigation into the role of p60v-src in cellular processes. Its inhibition capability makes it ideal for studies assessing the effects of p60v-src on cell growth, differentiation, and oncogenesis. -
Src Inhibitor
Antiallergic agent-1 is a Src-family kinase inhibitor, demonstrating potential as a lead compound for the development of novel antiallergic therapies. This compound features an alkyne functional group that allows it to participate in copper-catalyzed azide-alkyne cycloaddition (CuAAc) reactions, making it a valuable tool for click chemistry applications. Its unique properties support research into allergic response mechanisms and therapeutic interventions. -
Src Inhibitor
LCB 03-0110 is a thienopyridine derivative that serves as a potent inhibitor of Src family tyrosine kinases and pan-discoidin domain receptors. This compound is effective in suppressing scar formation by inhibiting the activation of fibroblasts and macrophages. Its key biological activity makes it a valuable tool for research applications focused on tissue repair and fibrosis. -
Src Inhibitor
KL-1156 is a selective Src inhibitor that demonstrates potent activity with an IC50 of 1 nM and a Ki of 540 pM. This compound effectively inhibits T cell proliferation, with an IC50 value of 262 nM. KL-1156 is useful for research applications focused on immune response modulation and the investigation of Src-related signaling pathways in cancer and other diseases. -
Src
TOP1210 is a selective tyrosine kinase inhibitor that targets Src, P38α, and Syk kinases. It demonstrates significant anti-inflammatory activity by effectively reducing the release of proinflammatory cytokines from various immune and inflammatory cell types, including peripheral blood monocytes and primary macrophages. TOP1210 shows promise in research applications related to inflammatory conditions, particularly ulcerative colitis, by offering a broader therapeutic potential through its multi-kinase inhibition profile, which may enhance the modulation of autoimmune responses. -
Src Inhibitor
DC-Srci-6649 is a selective inhibitor of c-Src kinase, designed to impede its phosphorylation and maintain c-Src in an inactive conformation. This compound demonstrates significant potential in studies of cancer biology and cell signaling, making it a valuable tool for investigating the role of c-Src in tumorigenesis and other pathological conditions. Researchers can utilize DC-Srci-6649 to explore therapeutic strategies targeting Src-mediated pathways. -
Src Inhibitor
LCB 03-0110 dihydrochloride is a potent inhibitor of Src family tyrosine kinases, functioning primarily by targeting their catalytic activity. This compound exhibits significant biological activity, making it valuable for research in cancer biology and cellular signaling pathways. It is particularly useful for studying the role of Src in tumorigenesis and metastasis, as well as in assessing therapeutic strategies for Src-related disorders. -
src SH3-SH2:Phosphoprotein Inhibitor
Ac-Tyr(PO3H2)-Glu-Glu-Ile-Glu-OH is a high-affinity pentapeptide targeting the src SH2 domain, exhibiting an IC50 of approximately 1 µM. This compound serves as an effective inhibitor of src SH3-SH2:phosphoprotein interactions. It is valuable in research applications focused on signaling pathways and protein-protein interactions involving src family kinases. -
RET/BRAF/S6K/Src Inhibitor
AD57 hydrochloride is a multikinase inhibitor that targets RET, BRAF, S6K, and Src pathways. This orally active compound demonstrates significant biological activity in modulating aberrant signaling pathways associated with various cancers. Research applications include studying the effects of combined inhibition on tumor growth and resistance mechanisms in cancer cell lines and animal models. -
Src SH2 Domain Inhibitor
AP-22161 is a selective inhibitor of the Src SH2 domain, exhibiting an IC50 of 0.24 µM. It demonstrates over 120-fold selectivity against Yes SH2 (IC50 = 29.38 µM) and ZAP SH2 (IC50 = 421.86 µM). This compound effectively inhibits Src-dependent cellular functions and reduces osteoclast resorptive activity, making it a valuable tool for research in osteoporosis and related bone disorders. -
Src Family Kinases Inhibitor
PP2 Analog is an ATP-competitive inhibitor targeting Src family kinases, demonstrating IC50 values of 0.22 µM for Lck, 0.15 µM for Src, 2.68 µM for Kdr, and 7 µM for Tie-2. This compound is utilized in research for its ability to modulate kinase activity, aiding in the study of signal transduction pathways and cancer biology. It is particularly useful in delineating the roles of Src family kinases in various cellular processes and disease states. -
pp60c-src Substrate
p60c-src substrate II is a specific pentapeptide substrate designed for the tyrosine kinase pp60c-src. This substrate facilitates the study of tyrosine phosphorylation mediated by pp60c-src, enabling key insights into its role in cell signaling pathways. It is ideally suited for research applications involving cancer biology and other cellular processes regulated by pp60c-src activity. -
Src SH2 Ligand
ISO24 is a potent ligand targeting the Src SH2 domain, exhibiting an IC50 of 4.4 mM as determined by BIAcore assays. This compound provides valuable insights into Src signaling pathways, making it suitable for research applications in cancer biology and signal transduction studies. Its specificity for the Src SH2 domain enhances its utility in exploring protein-protein interactions and downstream signaling cascades. -
Src Inhibitor
Hibarimicin G is a selective Src inhibitor derived from Microbispora rosea subsp. Hibaria. It exhibits potent activity against Src family tyrosine kinases, playing a crucial role in cell signaling pathways involved in cancer progression and metastasis. Hibarimicin G is utilized in research to elucidate the function of Src in various biological processes and to explore therapeutic strategies for targeting Src-mediated pathways in cancer treatment. -
Src Inhibitor
TOP1288 is a selective Src inhibitor, demonstrating potent activity against P38α, Src, and Syk kinases, with IC50 values of 116 nM, 24 nM, and 659 nM, respectively. This compound effectively inhibits the release of inflammatory cytokines from inflamed biopsies and myofibroblasts, making it a valuable tool for research on inflammation and related pathways. Its targeted action supports investigations into the modulation of kinase activity in various cellular contexts. -
c-Src Inhibtior
CGP062464 is a potent inhibitor of the tyrosine kinase c-Src, exhibiting an IC50 of less than 50 nM. This compound is primarily utilized in research related to osteoporosis and tumor-induced hypercalcemia, offering valuable insights into the signaling pathways involved in these conditions. Its selective inhibition of c-Src makes it a useful tool for investigating the role of this kinase in various biological processes. -
Src Inhibitor
Hibarimicin A is a selective Src tyrosine kinase inhibitor derived from Microbispora rosea subsp. hibaria. It effectively inhibits Src activity while sparing protein kinases A and C, making it a valuable tool for studying cellular signaling pathways involving Src. In addition to its role as a kinase inhibitor, Hibarimicin A exhibits moderate antibacterial activity against Gram-positive bacteria, with a minimum inhibitory concentration (MIC) ranging from 0.8 to 12.56 μg/mL, broadening its potential applications in microbiology and pharmacology research. -
Src SH2 Inhibitor
AP22408 is a potent nonpeptide inhibitor of the Src SH2 domain, exhibiting an IC50 value of 0.3 μM. This compound effectively inhibits osteoclast-mediated resorption of dentine in rabbits and demonstrates strong bone-targeting properties. In vivo studies reveal its antiresorptive activity in a parathyroid hormone-induced rat model, indicating potential applications in osteoporosis research and other bone-related diseases, including Paget’s disease, osteolytic bone metastasis, and malignancy-associated hypercalcemia. -
Src Inhibitor
Rhodomycin A is a potent Src inhibitor that modulates Src-related signaling pathways. This compound demonstrates significant biological activity by suppressing cancer cell proliferation, migration, invasion, and clonogenicity in vitro, as well as inhibiting tumor growth in vivo. Rhodomycin A is valuable for research applications targeting lung cancer and investigating the role of Src in tumor progression. -
Src Kinase Inhibitors
Saracatinib-d3 is a deuterium-labeled analog of Saracatinib and acts as an inhibitor of Src kinase. This compound exhibits significant anti-inflammatory properties, making it relevant in studies related to severe sepsis triggered by bacterial and microbial infections. Saracatinib-d3 is a valuable tool for research applications focused on Src kinase pathways and their implications in various disease states.

