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Chemical Structure| 2688842-08-0 Chemical Structure| 2688842-08-0

Structure of UNC6852
CAS No.: 2688842-08-0

Chemical Structure| 2688842-08-0

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UNC6852 is a selective PRC2 degrader based on PROTAC technology. It contains an EED ligand and a von Hippel-Lindau ligand, with an IC50 value of 247 nM against EED.

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Product Details of UNC6852

CAS No. :2688842-08-0
Formula : C43H48N10O6S
M.W : 832.97
SMILES Code : CC1=C(SC=N1)C2=CC=C(C=C2)CNC([C@@H]3C[C@H](CN3C([C@H](C(C)(C)C)NC(CCCNC(C4=CC=C(C=C4)C5=CN=C(N6C=NN=C56)NCC7=CC=CO7)=O)=O)=O)O)=O
MDL No. :MFCD32701932
InChI Key :PPNNFXIBKLCMTI-WXEAQWFJSA-N
Pubchem ID :146014466

Safety of UNC6852

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H315-H319
Precautionary Statements:P264-P280-P302+P352-P337+P313-P305+P351+P338-P362+P364-P332+P313

Related Pathways of UNC6852

epigenetics

Isoform Comparison

Biological Activity

Description
UNC6852, a selective degrader of the polycomb repressive complex 2 (PRC2) employing PROTAC technology, incorporates an EED (embryonic ectoderm development) ligand and a von Hippel-Lindau ligand, exhibiting an IC50 of 247 nM for EED[1].
Target
  • bromodomain

    EED, IC50:247 nM

In Vitro:

Cell Line
Concentration Treated Time Description References
Pfeiffer cells (EZH2A677G mutation) 10 µM 24 hours To evaluate the degradation effect of UNC6852 on PRC2 components in Pfeiffer cells, results showed effective degradation of all three PRC2 subunits. Cell Chem Biol. 2020 Jan 16;27(1):47-56.e15.
HeLa cells 0.79 ± 0.14 µM (EED), 0.3 ± 0.19 µM (EZH2) 24 hours To evaluate the degradation effect of UNC6852 on PRC2 components, results showed that UNC6852 effectively degraded EED and EZH2 with maximal degradation rates of 92% and 75%, respectively. Cell Chem Biol. 2020 Jan 16;27(1):47-56.e15.

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Zebrafish Zebrafish larvae and adults Intravenous injection 0.075 mM, 0.15 mM, 0.3 mM, 0.6 mM Single injection, larvae for 2 hours, adults for 6 hours To evaluate the effect of UNC6852 on tfpia mRNA levels and thrombus formation time in zebrafish. Results showed that UNC6852 treatment increased tfpia mRNA levels and prolonged thrombus formation time. Sci Rep. 2021 Jul 27;11(1):15238

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