DUSP6-IN-1 

DUSP6-IN-1 (compound 24) is an inhibitor targeting DUSP6, with IC₅₀ values of 1.3 nM, 4.7 nM and 0.3 nM for KRAS G12C, G12D and G12V, respectively; IC₅₀ values of 7 nM, 32 nM, 38 nM and 35 nM for the interaction of KRAS G12V, WT KRAS, WT HRAS and WT NRAS-BRAF with CYPA, respectively; IC₅₀ values of 9.7 nM, 49.5 nM and 7.1 nM for KRAS-BRAF and CYPA under G12C, G12D and G12V, respectively; when inhibiting pERK, IC₅₀ values for G12C and G12V are less than 0.6 nM, andIC₅₀value for G12D is 0.9 nM^[1].

DUSP6-IN-1 inhibits the proliferation of NCI-H23, NCI-H358, NCI-H2444, RKN, and SW620 cells with IC₅₀of 0.17 nM, 0.12 nM, 0.17 nM, 0.045 nM, and 0.1 nM^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

DUSP6-IN-1 (30 mg/kg, oral, once daily) inhibits tumor growth and promoted tumor regression in a brain tumor mouse model^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

837.08

C₄₆H₆₀N₈O₅S

O=C(OCC(C)(C)CC1=[C@@]([C@@]2=C([C@@H](OC)C)N=CC(N3CCN(C)CC3)=C2)N4C5=C1C=C6C=C5CCC4)[C@H]7NN(C([C@@H](NC([C@H]8[C@H](C)[C@@H]8C)=O)CC9=NC6=CS9)=O)CCC7

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Jianguo Chen, et al. Design, Tricyclic compounds for the treatment of cancer. WO2024169914A1. 2024-02-08