DDR

DDR-TRK-1 is a selective Discoidin Domain Receptor 1 (DDR1) inhibitor, with an IC50 value of 9.4 nM. DDR-TRK-1 also inhibits TRK family.

DDR1-IN-1 is a potent and selective DDR1 receptor tyrosine kinase inhibitor with IC50/EC50 of 105 nM/87 nM, 4-fold less potent for DDR2 (IC50= 413 nM).

FGFR1/DDR2 inhibitor 1 is an inhibitor of fibroblast growth factor receptor 1 (FGFR1) and discoindin domain receptor 2 (DDR2), with IC50 values of 31.1 nM, 108.4 nM and 3.2 nM for FGFR1, KG-1, and DDR2, respectively.

WRG-28 is a novel, potent and selective, allosteric inhibitor of discoidin domain receptor 2 (ddr2).

DDR1-IN-1 dihydrochloride is a potent and selective DDR1 receptor tyrosine kinase inhibitor with an IC50 of 105 nM; 4-fold less potent for DDR2 (IC50 = 413 nM).

CIDD-8633 is a potent inhibitor of DDR2, exhibiting an IC50 value of 6.105 μM. This compound effectively inhibits cell migration, induces cell cycle arrest, and promotes apoptosis, leading to significant suppression of pancreatic ductal adenocarcinoma (PDAC) tumor growth. CIDD-8633 is valuable for research applications focused on understanding and combating pancreatic cancer, particularly in the context of PDAC.

PHI-501 is a dual inhibitor targeting RAF and DDR pathways. It demonstrates potent anti-proliferative effects in melanoma cell lines, effectively inhibiting colony formation in drug-resistant cells. PHI-501 disrupts ERK and AKT phosphorylation and downregulates key gene sets associated with TNFA-NFKB, IL6-JAK-STAT3, and KRAS signaling pathways, as well as pathways involved in epithelial-mesenchymal transition. In vivo studies show significant anti-tumor efficacy in the SK-MEL3DR xenograft model, making PHI-501 valuable for research on drug resistance in melanoma.

SR-302 is a selective DDR/p38 inhibitor that exhibits potent biological activity with IC50 values of 0.125 μM for p38α, 0.023 μM for DDR1, and 0.018 μM for DDR2. This compound is valuable for investigating fibrotic disorders, including renal and pulmonary fibrosis, atherosclerosis, and various types of cancer. SR-302 serves as a key tool for elucidating the roles of DDR and p38 signaling pathways in disease progression and therapeutic intervention.

7rh is a selective inhibitor of discoidin domain receptor 1 (DDR1), exhibiting an IC50 of 13.1 nM, and also demonstrates moderate inhibitory activity against DDR2 with an IC50 of 203 nM. This compound serves as a valuable tool for the study of receptor signaling and cellular processes associated with DDRs. Additionally, 7rh incorporates an alkyne functional group, enabling it to participate in copper-catalyzed azide-alkyne cycloaddition (CuAAc) reactions, making it suitable for applications in click chemistry.

TPKI-39 is an inhibitor of DDR1, DDR2, and FLT1, demonstrating a human DDR1 IC50 of 380 nM and human DDR2 IC50 of 120 nM. It effectively inhibits enzymatic activity and autophosphorylation of DDR1 and DDR2, as well as FLT1 enzymatic activity, with an IC50 of 65 nM. This compound is useful for studies focused on the modulation of receptor tyrosine kinases and collagen-mediated signaling pathways.

VU6015929 is a potent and selective dual inhibitor of discoidin domain receptors 1 and 2 (DDR1/2), exhibiting IC50 values of 4.67 nM and 7.39 nM, respectively. This compound effectively inhibits collagen-induced activation of DDR1 and reduces collagen-IV production, making it a valuable tool for research on fibrosis and extracellular matrix remodeling. VU6015929 is suitable for studying the roles of DDR1/2 in various pathological processes and therapeutic interventions.

DDR1-IN-4 is a selective inhibitor of Discoidin Domain Receptor 1 (DDR1), effectively blocking its autophosphorylation with an IC50 of 29 nM. This compound exhibits significantly lower activity against DDR2, with an IC50 of 1.9 μM. DDR1-IN-4 is utilized in research applications focusing on cell signaling, extracellular matrix interactions, and cancer biology, providing valuable insights into the role of DDR1 in various pathological conditions.

DDR2-IN-1 is a potent inhibitor of the Discoidin Domain Receptor 2 (DDR2) with an IC50 of 26 nM. This compound plays a significant role in research related to osteoarthritis by modulating collagen signaling pathways and potentially influencing cartilage degradation and repair. Its application in studying DDR2-mediated processes makes it a valuable tool for investigating therapeutic strategies in bone and joint diseases.

DDR1-IN-6 is a selective inhibitor of Discoidin Domain Receptor 1 (DDR1), exhibiting an IC50 of 9.72 nM. This compound effectively inhibits auto-phosphorylation at the Y513 site of DDR1b, also with an IC50 of 9.7 nM, demonstrating significant anti-cancer activity. Additionally, DDR1-IN-6 serves as a click chemistry reagent due to its alkyne group, enabling it to participate in copper-catalyzed azide-alkyne cycloaddition (CuAAc) reactions with azide-containing molecules, facilitating diverse research applications in chemical biology and drug discovery.

DDR Inhibitor is a highly selective inhibitor of the discoidin domain receptors (DDRs), specifically demonstrating an IC50 of 3.3 nM for DDR2. Additionally, it exhibits a significant inhibitory effect on DDR1, with 53% inhibition at a concentration of 1.5 nM. This compound is valuable for investigating the role of DDRs in cellular processes and may have applications in cancer research and fibrosis studies.

DDR1/2 inhibitor-2 is a selective inhibitor of the DDR1 and DDR2 receptor tyrosine kinases, demonstrating IC50 values of less than 100 nM. This compound is primarily utilized in research related to cancer and fibrotic diseases, providing insights into the role of these receptors in tumor progression and fibrosis. Its potent inhibitory effects make it a valuable tool for studying DDR signaling pathways and their contributions to disease mechanisms.

DDR1-IN-5 is a selective inhibitor of Discoidin Domain Receptor 1 (DDR1), demonstrating an IC50 of 7.36 nM. It effectively inhibits the auto-phosphorylation of DDR1b at Y513, with an IC50 of 4.1 nM. DDR1-IN-5 exhibits anti-cancer activity, making it a valuable tool for cancer research. Additionally, this compound features an alkyne group, allowing it to participate in copper-catalyzed azide-alkyne cycloaddition for further biochemical applications.

DDR1-IN-9 is a selective inhibitor of the Discoidin Domain Receptor 1 (DDR1), known for its significant suppression of kinase activity, with a Kd value of 4.7 nM and an IC50 value of 9.4 nM. Demonstrating reduced activity against a broad panel of 400 nonmutated kinases, DDR1-IN-9 exhibits a favorable specificity profile. This compound also possesses beneficial pharmacokinetic properties and has displayed potential therapeutic effects in experimental models of pulmonary fibrosis, making it a valuable tool for researching fibrotic diseases and DDR1-related signaling pathways.

DDR1-IN-10 is a selective inhibitor of Discoidin Domain Receptor 1 (DDR1). It exhibits significant potential in the modulation of DDR1-mediated signaling pathways, making it a valuable tool in cancer research. DDR1-IN-10 is particularly useful for studying various malignancies, including pancreatic cancer, non-small cell lung cancer, and gastric carcinoma, where DDR1 plays a critical role in tumor progression and metastasis.

DDR1/2 IN-4 is a selective dual inhibitor targeting DDR1 and DDR2 kinases, demonstrating a pKi of 8.6 for DDR1 and 8.2 for DDR2. This compound effectively inhibits the kinase activities of both DDR1 and DDR2, leading to a reduction in the release of MCP-1. DDR1/2 IN-4 is suitable for research applications focused on idiopathic pulmonary fibrosis and related cellular mechanisms.

DDR1-IN-12 is a selective inhibitor of discoidin domain receptor 1 (DDR1), exhibiting an IC50 of 0.126 μM. This compound effectively blocks receptor tyrosine kinase autophosphorylation, thereby inhibiting downstream signaling pathways, including the suppression of TGF-β1-induced fibroblast activation. DDR1-IN-12 demonstrates significant potential in research applications related to tumor cell migration and the progression of pulmonary fibrosis, making it particularly relevant for studies involving lung cancer, including lung adenocarcinoma.

DDR1-IN-8 is a potent dual inhibitor of DDR1 and DDR2, demonstrating IC50 values of 0.045 μM and 0.126 μM, respectively. This compound exhibits significant anti-tumor activity, making it a valuable tool for studies related to cancer research. DDR1-IN-8 can be utilized to explore the role of DDR signaling in tumor progression and therapeutics targeting the DDR pathway.

DDR1/2 inhibitor-3 is a selective inhibitor of discoidin domain receptor 1 and 2 (DDR1/2), exhibiting IC50 values of 9.4 nM and 20.4 nM, respectively. This compound is primarily utilized in anti-inflammatory research, targeting the DDR pathways involved in cellular responses to inflammation. Its potent inhibitory effects make it a valuable tool for elucidating the role of DDR receptors in various biological processes.