MS6105 

MS6105 is an LDH protein hydrolysis-targeted chimera (PROTAC) that effectively degrades LDHA and LDHB in a time- and ubiquitin-proteasome system-dependent manner and has anticancer activity^[1]. MS6105 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

MS6105 (compound 22) (10 nM-10 μM, 48 h) can effectively induce LDHA and LDHB degradation in PANC1 cells in a time- and concentration-dependent manner, with DC₅₀ values of 38 nM and 74 nM for LDHA and LDHB, respectively^[1].
MS6105 (compound 22) (0.1-1 μM, 48 h) effectively inhibits the proliferation of PANC1 cells with a GI₅₀ value of 16.1 μM and the growth of MiaPaca2 cells with a GI₅₀ value of 12.2 μM^[1].

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

1228.59

C₆₅H₈₁N₉O₉S₃

2891709-58-1

Solid

White to off-white

CC1=C(SC=N1)C2=CC=C(C=C2)CNC([C@@H]3C[C@H](CN3C([C@H](C(C)(C)C)NC(CCCCCCCCCCCC(NCCCCC#CC4=CC=CC(C5=NN(C(CC6CC6)=C5CC7=CC=C(C=C7)S(N)(=O)=O)C8=NC(C(O)=O)=CS8)=C4)=O)=O)=O)O)=O

Room temperature in continental US; may vary elsewhere.

-20°C, protect from light, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

• [1]. Ning Sun, et al. Discovery of the First Lactate Dehydrogenase Proteolysis Targeting Chimera Degrader for the Treatment of Pancreatic Cancer. J Med Chem. 2023 Jan 12;66(1):596-610.   [Content Brief]