UNC10088

UNC10088 (0.5 μM, 15 min) drives the SCF^FBXO22-dependent polyubiquitination of the NSD2 PWWP1 domain by binding to C326 of FBXO22 to mediate a stable ternary complex, a process reliant on key interacting residues (e.g., FBXO22's E362, K229, E169, and NSD2's F266, E272, K253) wherein mutations disrupt complex stability or degrader positioning and inhibit ubiquitination^[1].
UNC10088's (5 μM, 1 h) binding to the FBXO22 FIST domain is exclusively dependent on Cys326, as complex formation is abolished by the C326A mutation and restored by its singular reintroduction into a cysteine-null background^[1].
UNC10088 (1 h) exhibits a 2.5-fold reduction in IC₅₀ (from 248 nM to 101 nM) upon the addition of FBXO22, indicating positive cooperative binding with an α-factor of 3.3^[1].
UNC10088 significantly increases the melting temperature (Tm) of the FIST domain in wild-type FBXO22; the addition of UNC10088 had almost no effect on the Tm of the C326A mutant^[1].

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