C199 is a PROTAC targeting PRMT4. C199 is composed of the PRMT4 inhibitor EZM2302, a linker, and a von Hippel-Lindau (VHL)E3 ligase ligand. C199 demonstrated potent cellular degradation (DC50 = 106 nM, Dmax =93.1%) and showed high selectivity for PRMT4 over other protein argininemethyltransferases. Importantly, in vivo studies showed that C199 had a relatively longhalf-life (10.10 h versus 4.89 h for EZM2302) and demonstrated strong antitumor activity(TGI = 78% versus 49% for EZM2302) without significant toxicity even at high doses.
MedKoo Cat#: 129047
Name: C199
CAS#: N/A
Chemical Formula: C67H95ClN10O8S
Exact Mass: 1234.6700
Molecular Weight: 1236.07
Elemental Analysis: C, 65.10; H, 7.75; Cl, 2.87; N, 11.33; O, 10.35; S, 2.59
The following data is based on the product molecular weight 1,236.07 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
1: Delva-Wiley J, Ekhator ES, Adams LL, Patwardhan S, Dong M, Newman RH. Redox
Modification of PKA-Cα Differentially Affects Its Substrate Selection. Life
(Basel). 2023 Aug 26;13(9):1811. doi: 10.3390/life13091811. PMID: 37763215;
PMCID: PMC10532679.
