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Merck
CN

SML3179

Homer

≥95% (HPLC)

Synonym(s):

6-Hydroxy-N-(4’-((5-(((S)-1-((2S,4R)-4-hydroxy-2-((4-(4-methylthiazol-5-yl)benzyl)carbamoyl)pyrrolidin-1-yl)-3,3-dimethyl-1-oxobutan-2-yl)amino)-5-oxopentyl)carbamoyl)-4-(4-methylpiperazin-1-yl)-[1,1’-biphenyl]-3-yl)-4-(trifluoromethyl)-nicotinamide, N-(4′-(5-((S)-1-((2S,4R)-4-Hydroxy-2-(4-(4-methylthiazol-5-yl)benzylcarbamoyl)pyrrolidin-1-yl)-3,3-dimethyl-1-oxobutan-2-ylamino)-5-oxopentylcarbamoyl)-4-(4-methylpiperazin-1-yl)biphenyl-3-yl)-6-oxo-4-(trifluoromethyl)-1,6-dihydropyridine-3-carboxamide, WD40 repeat domain protein 5 (WDR5) degrader 8g, WDR5 Degrader 8g, WDR5 PROTAC 8g

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About This Item

Empirical Formula (Hill Notation):
C52H60F3N9O7S
CAS Number:
2737222-94-3
Molecular Weight:
1012.15
UNSPSC Code:
12352107
NACRES:
NA.77

Key Documents

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SMILES string

CN1CCN(CC1)C2=C(NC(C3=CNC(C=C3C(F)(F)F)=O)=O)C=C(C4=CC=C(C(NCCCCC(N[C@@H](C(C)(C)C)C(N5C[C@H](O)C[C@H]5C(NCC6=CC=C(C=C6)C7=C(C)N=CS7)=O)=O)=O)=O)C=C4)C=C2

assay

≥95% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 2 mg/mL, clear

storage temp.

2-8°C

Quality Level

100

Biochem/physiol Actions

Homer (WDR5 Degrader 8g) is a cell-permeable highly efficacious and potent WDR5-selective heterobifunctional degrader composed of WDR5 antagonist OICR-9429 analog plus a butyl chain spacer linked to an E3 ubiquitin ligase von Hippel-Lindau (VHL)-binding ligand that effectively depletes WDR5 in various cancer cell lines (Dmax = 58% and DC50 = 53 nM in MV4-11WDR5-HiBiT cells, 24 h). Homer is shown to dose-dependently induce WDR5 ubiquitylation and proteasomal degradation (Kd = 18 nM; IC50 cellular & lysate = 13.6 & 2.15 μM, respectively, NanoBRET assay).
cell-permeable highly efficacious and potent WDR5-selective heterobifunctional degrader

Storage Class

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

Regulatory Information

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Certificates of Analysis (COA)

Lot/Batch Number
0000161718
0000161720
0000161718
0000147641

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Anja Dölle et al.
Journal of medicinal chemistry, 64(15), 10682-10710 (2021-05-14)
Histone H3K4 methylation serves as a post-translational hallmark of actively transcribed genes and is introduced by histone methyltransferase (HMT) and its regulatory scaffolding proteins. One of these is the WD-repeat-containing protein 5 (WDR5) that has also been associated with controlling

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