SM1-71

Research use only, not for human use.

SM1-71 is a potent multi-targeted acrylamide-modified TAK1 inhibitor that inhibits MKNK2, MAP2K1/2/3/4/6/7, GAK, AAK1, BMP2K, MAP3K7, MAPKAPK5, GSK3A/B, MAPK1/3, SRC, YES1, FGFR1, ZAK (MLTK), MAP3K1, LIMK1 and RSK2.

SM1-71 (compound 5) is a potent TAK1 inhibitor, with a Ki of 160 nM, it also can covalently inhibit MKNK2, MAP2K1/2/3/4/6/7, GAK, AAK1, BMP2K, MAP3K7, MAPKAPK5, GSK3A/B, MAPK1/3, SRC, YES1, FGFR1, ZAK (MLTK), MAP3K1, LIMK1 and RSK2. SM1-71 can inhibit proliferation of multiple cancer cell lines.

SM1-71 (0.001-100 μM; 72 h) potently inhibits the proliferation of H23 and Calu-6 non-small cell lung cancer cell lines with a concentration-dependent manner.SM1-71 (72 h) induces potent cytotoxicity with nanomolar values for GR50 and negative GRmax values in eight of 11 cancer cell lines.Cell Viability Assay Cell Line:H23-KRASG12C and Calu-6-KRASQ61K cells Concentration:0.001, 0.01, 0.1, 1, 10, 100 μM Incubation Time:72 hours Result:Inhibited proliferation of H23-KRASG12C and Calu-6-KRASQ61K cells with IC50s of 0.4 and 0.3 μM, respectively.

——

——

MAPK/ERK Signaling

p38 MAPK

MAPK | AAK1 (AP2 associated kinase 1) | TGF-beta/Smad | LIM Kinase | Serine/threonin kinase

——

——

2088179-99-9

463.96

C24H26ClN7O

>98% (HPLC)

In Vitro:?DMSO : 125 mg/mL (269.42 mM; Ultrasonic )

CN1CCN(CC1)c1ccc(Nc2ncc(Cl)c(Nc3ccccc3NC(=O)C=C)n2)cc1

——

(-20℃)

With Ice Pack

≥ 2 years