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 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].

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).

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.

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).