ddr1/2

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.

DDR1/2 IN-4 (Compound 37) is a selective dual inhibitor targeting DDR1 and DDR2 kinases, with a pKi of 8.6 for DDR1 and 8.2 for DDR2. This compound functionally suppresses the kinase activity of both DDR1 and DDR2 and inhibits MCP-1 release. DDR1/2 IN-4 is applicable for research related to idiopathic pulmonary fibrosis.

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].

Anti-DDR1/CD167a Antibody 2 is an antibody targeting DDR1/CD167a. It can be used for oncology, immunology, and antibody drug development research.

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.

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.

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.

DDR1-IN-8 (compound 7s) is a potent inhibitor of DDR1/2, exhibiting IC50 values of 0.045 μM and 0.126 μM, respectively, and possesses antitumor activity.

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

TA-02 is a p38 MAPK inhibitor with IC50 of 20 nM.TA-02 especially inhibits TGFBR-2.

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).

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].

S 16020-2 is an olivacine derivative, and DNA topoisomerase II inhibitor endowed with a remarkable antitumor activity against various experimental tumors.

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