Discoidin Domain Receptor (DDR)

DDR inhibitor is a potent discidin domain receptor (DDR) inhibitor. The IC50 of DDR2 is 3.3 nM, and DDR1 has 53% inhibition at 1.5 nM.

Merestinib (LY2801653) is an orally available, small molecule inhibitor of the proto-oncogene c-Met (Ki: 2 nM) with potential antineoplastic activity. Merestinib electively binds to c-Met, thereby inhibiting c-Met phosphorylation and disrupting c-Met signal transduction pathways. This may induce cell death in tumor cells overexpressing c-Met protein or expressing the constitutively activated c-Met protein.

MitoBloCK-6 is an effective inhibitor of Erv1 ALR with IC50 values of 900 nM and 700 nM, respectively. Additionally, MitoBloCK-6 inhibits Erv2 (IC50=1.4 μM). It induces apoptosis in hESCs by promoting the release of cytochrome c.

DDR1-IN-1 is an effective and specific DDR1 receptor tyrosine kinase inhibitor (IC50: 105 nM), about 3-fold selectivity over DDR2.

WRG-28 is a potent and selective, allosteric discoidin domain receptor 2 (ddr2) inhibitor(IC50 : 230 nM)

VU6015929 is an inhibitor of active dual discoidin domain receptor 1 2 (DDR1 2)( IC50s of 4.67 nM and 7.39 nM, respectively).

DDR-TRK-1, a selective discoid domain receptor 1 (DDR1) inhibitor, exhibits an IC50 value of 9.4 nM and also inhibits the TRK family.

Sitravatinib (MGCD516) is an inhibitor targeting multiple RTKs involved in driving sarcoma cell growth, including c-Met, c-Kit, PDGFRα β, PDGFR, and Axl.

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

LCB 03-0110 (3-(2-(3-(Morpholinomethyl)phenyl)thieno[3,2-b]pyridin-7-ylamino)phenol) is a potent inhibitor of discoidin domain receptor family tyrosine kinases and strongly inhibits several tyrosine kinases, including the c-Src family, spleen tyrosine kinase, Bruton's tyrosine kinase, and vascular endothelial growth factor receptor 2, which are important for immune cell signaling and inflammatory reactions.

DDR1-IN-2 (DDR1 inhibitor 7rh) (DDR1 inhibitor 7rh) is a potent, selective, ATP-competitive Discoidin domain receptor 1 (DDR1) inhibitor (IC50: 6.8 nM in cell-free kinase assays).

BAY-826 is a novel, potent and selective TIE-2 inhibitor that inhibits TIE-2 phosphorylation and can be used to study tumors.

Merestinib dihydrochloride (LY2801653 dihydrochloride) is an orally available kinase inhibitor with antitumor activity that inhibits MET, AXL, RON, and MKNK1/2, and inhibits the growth of NTRK fusion-carrying tumors.

DDR1-IN-4 (Compound 2.45) is a highly potent inhibitor that selectively targets Discoidin Domain Receptor 1 (DDR1) autophosphorylation, demonstrating exceptional efficacy with IC50 values of 29 nM for DDR1 and 1.9 μM for DDR2.

DDR1-IN-10 (compound 7q) is an inhibitor of DDR1. It is applicable in research related to pancreatic cancer, non-small cell lung cancer, and gastric cancer.

DDR Inhibitor 2 (compound 5a) is a potent inhibitor of the discoidin domain receptor (DDR) with an IC50 value of 0.125 μM, and it is applicable in fibrotic disease research.

DDR1 2 Inhibitor-2 (Example 31) serves as an inhibitor of DDR1 DDR2, exhibiting IC50 values below 100 nM. It is applicable in cancer and fibrotic disease research [1].

GW694590A (UNC10112731) functions as a MYC protein stabilizer that enhances the levels of endogenous MYC protein. It also acts on receptor tyrosine kinases, inhibiting DDR2, KIT, and PDGFRα by 81%, 68%, and 67% at a concentration of 1 μM, respectively. As a protein kinase inhibitor, GW694590A affects both ATP-dependent and ATP-independent luciferases, potentially influencing the Fluc reporter gene [1].

Sitravatinib malate is an orally bioavailable receptor inhibitor of tyrosine kinase (RTK) (IC50s of 1.5 nM, 2 nM, 2 nM, 5 nM, 6 nM, 6 nM, 8 nM, 0.5 nM, 29 nM, 5 nM, and 9 nM for Axl, MER, VEGFR3, VEGFR2, VEGFR1, KIT, FLT3, DDR2, DDR1, TRKA, TRKB, respectively.) , shows potent single-agent antitumor efficacy and enhances the activity of PD-1 blockade through promoting an antitumor immune microenvironment.

SR-302 is a potent and selective inhibitor of DDR p38, with IC50 values of 0.125 μM for p38α, 0.023 μM for DDR1, and 0.018 μM for DDR2. It is utilized in research related to fibrotic diseases, such as kidney and lung fibrosis, atherosclerosis, and various types of cancer.

DDR1 2 inhibitor-3 (5n) is an inhibitor of DDR1 2, with IC50 values of 9.4 nM and 20.4 nM, respectively. It is applicable in anti-inflammatory research.

PROTACDDR1 degrader-1 is a PROTAC degrader specifically targeting DDR1.

DDR2-IN-1 (Compound 129) is recognized as a highly effective DDR2 inhibitor, displaying an IC50 value of 26 nM. It is a suitable choice for conducting osteoarthritis research.

JNK3 inhibitor-2 is a potent and selective JNK3 inhibitor with IC50 values of >100 μM for JNK1, >100 μM for JNK2, and 0.25 μM for JNK3. JNK3 inhibitor-2 also inhibits DDR1 and EGFR (T790M, L858R) [1].