Bioactivity | IACS-9571 (trifluoroacetate) is a potent and selective inhibitor of TRIM24 and BRPF1, with IC50 of 8 nM for TRIM24, and Kd of 31 nM and 14 nM for TRIM24 and BRPF1, respectively. |
Target | IC50: 8 nM (TRIM24)Kd: 31 nM (TRIM24), 14 nM (BRPF1) |
Invitro | IACS-9571 (trifluoroacetate) shows excellent cellular potency with EC50 of 50 nM. IACS-9571 (trifluoroacetate) (1 μM) has potent activities against a panel of 32 bromodomains. IACS-9571 (trifluoroacetate) is a selective dual TRIM24/BRPF1 inhibitor (Kd=1.3/2.1 nM) with 9- and 21-fold selectivity against BRPF2 and BRPF3, respectively. IACS-9571 (trifluoroacetate) does not interact with the BET sub-family of bromodomains, displaying greater than 7,700-fold selectivity versus BRD4 (1, 2) relative to TRIM24[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> IACS-9571 TFA 相关抗体: |
CAS | 1883598-69-3 |
Formula | C34H43F3N4O10S |
Molar Mass | 756.79 |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
Reference | [1]. Palmer WS, et al. Structure-Guided Design of IACS-9571, a Selective High-Affinity Dual TRIM24-BRPF1 Bromodomain Inhibitor. J Med Chem. 2016 Feb 25;59(4):1440-54. |