Specifications

Cell penetrant Proteolysis Targeting Chimera (PROTAC) compound based on (+)-JQ1 conjugated to a von Hippel-Lindau (VHL) ligand. Retains high affinity for BRD2, BRD3 and BRD4 bromodomains (Kd = 13-60 nM) but induces preferential degradation of BRD4 over BRD2 and BRD3 (DC50 values for degradation of BRD4 are 8 and 23 nM in H661 and H838 cells, respectively). Exhibits potent cytotoxicity and anti-proliferative effects in AML cell lines (pEC50 = 7.6 in Mv4-11 cells).

Product Information

Purity:                                              >98.0%MW:                                                 1002.64Formula:                                          C49H60ClN9O8S2CAS No.                                           1797406-69-9Physical State:                                 Lyophilized white to off-white solidQuantity:                                         1mg; 5mgSolubility:                                        100 mg/mL in DMSO; or 100 mg/ml in ethanolStorage:                                           Store desiccated as supplied at -20°C for up to 3 years. Store solutions at -80°C for up to 6 months or -20°C for up to 1 month.

References

1. Zengerle et al (2015) Selective small molecule induced degradation of the BET bromodomain protein BRD4. ACS.Chem.Biol 10 1770 PMID: 260356252. Gadd et al (2017) Structural basis of PROTAC cooperative recognition for selective protein degradation. Nat.Chem.Biol. PMID: 282881083. Wurz et al (2017) A ” click chemistry platform” for the rapid synthesis of bispecific molecules for inducing protein degradation. J.Med.Chem. PMID: 28378579

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