| Bioactivity | UCB-5307 is a potent TNF signaling inhibitor with a KD of 9 nM for human TNFα. UCB-5307 can penetrate the preformed hTNF/hTNFR1 complex[1]. |
| Invitro | UCB-5307 inhibits wild-type TNF but does not inhibit L57F TNF. The T1/2 of UCB-5307 is 3.3 h[1].UCB-5307 disrupts a preformed hTNF/hTNFR1 complex, can penetrate the preformed complex, dislodging one of the receptors. Preloading hTNF with UCB-5307 blocks one receptor from binding[1].UCB-5307 binds to a pocket in the centre of the TNF trimer formed by the movement of the TNF monomers, stabilising the distorted trimer, which leads to reduced signalling through TNFR1[1]. |
| Name | UCB-5307 |
| CAS | 1515887-44-1 |
| Formula | C22H21N3O |
| Molar Mass | 343.42 |
| Appearance | Solid |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | 4°C, sealed storage, away from moisture and light *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light) |
| Reference | [1]. O'Connell J, et al. Small molecules that inhibit TNF signalling by stabilising an asymmetric form of the trimer. Nat Commun. 2019 Dec 19;10(1):5795. |