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YX968

Chemical Structure : YX968

CAS No.: 2742732-92-7

YX968 (YX-968, YX 968)

Catalog No.: PC-21143Not For Human Use, Lab Use Only.

YX968 is a potent, selecive HDAC3/8 dual PROTAC degrader with DC50 of 1.7 and 6.1 nM in degrading HDAC3 and HDAC8 respectively (MDA-MD-231 cell, 8 h).

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

YX968 is a potent, selecive HDAC3/8 dual PROTAC degrader with DC50 of 1.7 and 6.1 nM in degrading HDAC3 and HDAC8 respectively (MDA-MD-231 cell, 8 h).
YX968 induces highly potent, rapid, and selective degradation of both HDAC3/8 without triggering pan-HDAC inhibitory effects.
YX968 shows HDAC1 and HDAC3 enzyme inhibition (IC50 = 591 nM and 284 nM, respectively).
YX968 rapidly degrades HDAC3 and HDAC8 via the ubiquitin-proteasome system (UPS).
YX968 is highly specific in targeted HDAC3/8 degradation, with no effect on HDAC2, HDAC4, HDAC6, and HDAC7.
YX968 does not significantly alter transcriptome.
YX968 is highly potent on suppressing the growth of cancer cell lines, YX968 (125 nM) estrogen receptor-positive BC cell lines MCF7 and T47D as well as the TNBC cell lines BT549, MDA-MB-468 and HCC1806.

Physicochemical Properties

M.Wt 831.13
Formula C45H66N8O5S
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

(2S,4R)-1-((S)-3,3-dimethyl-2-(8-(4-(4-(2-propylhydrazine-1-carbonyl)phenyl)piperazin-1-yl)octanamido)butanoyl)-4-hydroxy-N-((S)-1-(4-(4-methylthiazol-5-yl)phenyl)ethyl)pyrrolidine-2-carboxamide

References

1. Yufeng Xiao, et al. Cell Chem Biol. 2023 Aug 8;S2451-9456(23)00240-4.

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