RNA polymerase II-IN-2 

RNA polymerase II-IN-2 is a RNA polymerase II inhibitor with a K_i value of 74.1 nM. RNA polymerase II-IN-2 inhibits Pol II-mediated transcription and induces cytotoxicity in mammalian cells. RNA polymerase II-IN-2 serves as a payload for antibody-drug conjugates (ADC) and is applicable for cancer research^[1].

RNA polymerase II-IN-2 (20iii) is nearly twice as cytotoxic to CHO cells as α-amanitin, with a normalized IC₅₀ value of 0.61^[1].
RNA polymerase II-IN-2 is 5-fold more cytotoxic to HEK293 cells than α-amanitin, with a normalized IC₅₀ value of 0.20^[1].
RNA polymerase II-IN-2 is more cytotoxic to HeLa cells than α-amanitin, with a normalized IC₅₀ value of 0.60^[1].
RNA polymerase II-IN-2 is significantly less cytotoxic to HepG2 liver-derived cells than α-amanitin, with a normalized IC₅₀ value of 2.7^[1].

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

915.02

C₄₁H₅₈N₁₀O₁₂S

2891451-33-3

O=C([C@H](C(CC)CC)NC(CNC1=O)=O)NCC(N[C@@H]2C(N[C@H](C(N3C[C@@H](C[C@H]3C(N[C@H](C(N[C@H]1CC4=C(S[C@H]2C)NC5=C4C=CC=C5)=O)[C@H]([C@H](CO)O)C)=O)O)=O)CC(N)=O)=O)=O

Room temperature in continental US; may vary elsewhere.

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

• [1]. Todorovic M, et al. Rationally Designed Amanitins Achieve Enhanced Cytotoxicity. J Med Chem. 2022;65(15):10357-10376.  [Content Brief]