| Bioactivity | GNE-371 is a potent and selective chemical probe for the second bromodomains of human transcription-initiation-factor TFIID subunit 1 and transcription-initiation-factor TFIID subunit 1-like, with an IC50 of 10 nM for TAF1(2). Storage: protect from light. |
| Target | IC50: 10 nM (TAF1(2)). |
| Invitro | GNE-371 (compound 27) binds TAF1(2) with an IC50 of 10 nM while maintaining excellent selectivity over other bromodomain-family members. GNE-371 is also active in a cellular-TAF1(2) target-engagement assay (IC50=38 nM) and exhibits anti-proliferative synergy with the BET inhibitor JQ1, suggesting engagement of endogenous TAF1 by GNE-371 and further supporting the use of GNE-371 in mechanistic and target-validation studies[1]. |
| Name | GNE-371 |
| CAS | 1926986-36-8 |
| Formula | C24H25N5O3 |
| Molar Mass | 431.49 |
| Appearance | Solid |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | 4°C, protect from light, stored under argon *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under argon) |
| Reference | [1]. Wang S, et al. GNE-371, a Potent and Selective Chemical Probe for the Second Bromodomains of Human Transcription-Initiation-Factor TFIID Subunit 1 and Transcription-Initiation-Factor TFIID Subunit 1-like. J Med Chem. 2018 Oct 25;61(20):9301-9315. |