UNC6852

UNC6852 is a selective degrader that targets polycomb repressive complex 2 (PRC2) with IC50 of 247 nM for EED. UNC6852 is based on PROTAC and contains an EED226-derived ligand and a ligand for VHL.

Product information

Molecular Weight: 832.97

Formula: C43H48N10O6S

Synonym:

UNC-6852

UNC 6852

Chemical Name: (2S,4R)-1-((S)-2-(4-(4-(5-((Furan-2-ylmethyl)amino)-[1,2,4]triazolo[4,3-c]pyrimidin-8-yl)benzamido)butanamido)-3,3-dimethylbutanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide

Smiles: CC1N=CSC=1C1=CC=C(CNC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@@H](NC(=O)CCCNC(=O)C2C=CC(=CC=2)C2=CN=C(NCC3=CC=CO3)N3C=NN=C32)C(C)(C)C)C=C1

InChiKey: PPNNFXIBKLCMTI-WXEAQWFJSA-N

InChi: InChI=1S/C43H48N10O6S/c1-26-36(60-25-48-26)29-11-9-27(10-12-29)20-45-40(57)34-19-31(54)23-52(34)41(58)37(43(2,3)4)50-35(55)8-5-17-44-39(56)30-15-13-28(14-16-30)33-22-47-42(53-24-49-51-38(33)53)46-21-32-7-6-18-59-32/h6-7,9-16,18,22,24-25,31,34,37,54H,5,8,17,19-21,23H2,1-4H3,(H,44,56)(H,45,57)(H,46,47)(H,50,55)/t31-,34+,37-/m1/s1

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO 100 mg/mL (120.05 mM) Ethanol 100 mg/mL (120.05 mM)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

UNC6852 mediates PRC2 degradation. UNC6852 has no cytotoxicity when the concentration of HeLa cells is up to 30 μM. UNC6852 (10 μM; 1-72 hours) lead to a decrease in the levels of both EED and EZH2. UNC6852 facilitates PRC2 degradation via VHL recruitment. UNC6852 selectively degrades EED and EZH2.H3K27me3 levels and DLBCL cell proliferation reduced by UNC6852 .

References:

1. Potjewyd F, et al. Degradation of Polycomb Repressive Complex 2 with an EED-Targeted Bivalent Chemical Degrader. Cell Chem Biol. 2020 Jan 16;27(1):47-56.e15.

Products are for research use only. Not for human use.