For research use only. Not for therapeutic Use.
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].
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].
| Catalog Number | I043533 |
| CAS Number | 1515887-44-1 |
| Synonyms | [1-[(2,5-dimethylphenyl)methyl]benzimidazol-2-yl]-pyridin-4-ylmethanol |
| Molecular Formula | C22H21N3O |
| Purity | ≥95% |
| InChI | InChI=1S/C22H21N3O/c1-15-7-8-16(2)18(13-15)14-25-20-6-4-3-5-19(20)24-22(25)21(26)17-9-11-23-12-10-17/h3-13,21,26H,14H2,1-2H3 |
| InChIKey | MKABLXAUPLCAHG-UHFFFAOYSA-N |
| SMILES | CC1=CC(=C(C=C1)C)CN2C3=CC=CC=C3N=C2C(C4=CC=NC=C4)O |
| 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. |
