L-Prolinamide, N-[5-[[[3′-[[[1,6-dihydro-6-oxo-4-(trifluoromethyl)-3-pyridinyl]carbonyl]amino]-4′-(4-methyl-1-piperazinyl)[1,1′-biphenyl]-4-yl]carbonyl]amino]-1-oxopentyl]-3-methyl-L-valyl-4-hydroxy-N-[[4-(4-methyl-5-thiazolyl)phenyl]methyl]-, (4R)-

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L-Prolinamide, N-[5-[[[3′-[[[1,6-dihydro-6-oxo-4-(trifluoromethyl)-3-pyridinyl]carbonyl]amino]-4′-(4-methyl-1-piperazinyl)[1,1′-biphenyl]-4-yl]carbonyl]amino]-1-oxopentyl]-3-methyl-L-valyl-4-hydroxy-N-[[4-(4-methyl-5-thiazolyl)phenyl]methyl]-, (4R)- Suppliers list
Company Name: SHANGHAI FORTUNE CHEMICAL TECHNOLOGY CO., LTD  
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Products Intro: Product Name:Homer
CAS:2737222-94-3
Purity:98% Package:10mg，100mg，500mg，1g，10g
Company Name: Changzhou Chenhong Biotechnology Co., Ltd.  
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Products Intro: Product Name:Homer
CAS:2737222-94-3
Purity:99% Package:50mg;100mg;250mg;500mg;1g;5g
Company Name: Nantong QuanYi Biotechnology Co., Ltd  
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Products Intro: Product Name:Homer
CAS:2737222-94-3
Purity:98%HPLC Package:10mg，100mg，500mg，1g，2g，5g，10g，more
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Products Intro: Product Name:Homer
CAS:2737222-94-3
Purity:99.93% Package:50mg/RMB 16800;10mg/RMB 8620
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Products Intro: Product Name:Homer
CAS:2737222-94-3
L-Prolinamide, N-[5-[[[3′-[[[1,6-dihydro-6-oxo-4-(trifluoromethyl)-3-pyridinyl]carbonyl]amino]-4′-(4-methyl-1-piperazinyl)[1,1′-biphenyl]-4-yl]carbonyl]amino]-1-oxopentyl]-3-methyl-L-valyl-4-hydroxy-N-[[4-(4-methyl-5-thiazolyl)phenyl]methyl]-, (4R)- Basic information
Product Name:L-Prolinamide, N-[5-[[[3′-[[[1,6-dihydro-6-oxo-4-(trifluoromethyl)-3-pyridinyl]carbonyl]amino]-4′-(4-methyl-1-piperazinyl)[1,1′-biphenyl]-4-yl]carbonyl]amino]-1-oxopentyl]-3-methyl-L-valyl-4-hydroxy-N-[[4-(4-methyl-5-thiazolyl)phenyl]methyl]-, (4R)-
Synonyms:L-Prolinamide, N-[5-[[[3′-[[[1,6-dihydro-6-oxo-4-(trifluoromethyl)-3-pyridinyl]carbonyl]amino]-4′-(4-methyl-1-piperazinyl)[1,1′-biphenyl]-4-yl]carbonyl]amino]-1-oxopentyl]-3-methyl-L-valyl-4-hydroxy-N-[[4-(4-methyl-5-thiazolyl)phenyl]methyl]-, (4R)-
CAS:2737222-94-3
MF:C52H60F3N9O7S
MW:1012.15
EINECS:
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Mol File:2737222-94-3.mol
L-Prolinamide, N-[5-[[[3′-[[[1,6-dihydro-6-oxo-4-(trifluoromethyl)-3-pyridinyl]carbonyl]amino]-4′-(4-methyl-1-piperazinyl)[1,1′-biphenyl]-4-yl]carbonyl]amino]-1-oxopentyl]-3-methyl-L-valyl-4-hydroxy-N-[[4-(4-methyl-5-thiazolyl)phenyl]methyl]-, (4R)- Structure
L-Prolinamide, N-[5-[[[3′-[[[1,6-dihydro-6-oxo-4-(trifluoromethyl)-3-pyridinyl]carbonyl]amino]-4′-(4-methyl-1-piperazinyl)[1,1′-biphenyl]-4-yl]carbonyl]amino]-1-oxopentyl]-3-methyl-L-valyl-4-hydroxy-N-[[4-(4-methyl-5-thiazolyl)phenyl]methyl]-, (4R)- Chemical Properties
Boiling point 1179.9±65.0 °C(Predicted)
density 1.322±0.06 g/cm3(Predicted)
storage temp. 2-8°C
solubility DMSO: 2mg/mL, clear
pka8.63±0.10(Predicted)
form powder
color white to beige
SMILESCN1CCN(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
Safety Information
WGK Germany WGK 3
Storage Class11 - Combustible Solids
MSDS Information
L-Prolinamide, N-[5-[[[3′-[[[1,6-dihydro-6-oxo-4-(trifluoromethyl)-3-pyridinyl]carbonyl]amino]-4′-(4-methyl-1-piperazinyl)[1,1′-biphenyl]-4-yl]carbonyl]amino]-1-oxopentyl]-3-methyl-L-valyl-4-hydroxy-N-[[4-(4-methyl-5-thiazolyl)phenyl]methyl]-, (4R)- Usage And Synthesis
UsesPROTAC WDR5 degrader 1 (compound 8g) is a PROTAC degrader targeting WDR5. PROTAC WDR5 degrader 1 is composed of a target protein ligand (red part) WDR5 ligand 2 (HY-168488), a VHL-type E3 ligase ligand (blue part) (S,R,S)-AHPC (HY-125845), and a PROTAC linker (balck part) 5-Aminovaleric acid (HY-W015878), in which the VHL ligand and the PROTAC linker form a conjugate (HY-114176A)[1].
Biological ActivityHomer (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 th at 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).
References[1] Dlle A, et al. Design, Synthesis, and Evaluation of WD-Repeat-Containing Protein 5 (WDR5) Degraders. J Med Chem. 2021 Aug 12;64(15):10682-10710. DOI:10.1021/acs.jmedchem.1c00146
L-Prolinamide, N-[5-[[[3′-[[[1,6-dihydro-6-oxo-4-(trifluoromethyl)-3-pyridinyl]carbonyl]amino]-4′-(4-methyl-1-piperazinyl)[1,1′-biphenyl]-4-yl]carbonyl]amino]-1-oxopentyl]-3-methyl-L-valyl-4-hydroxy-N-[[4-(4-methyl-5-thiazolyl)phenyl]methyl]-, (4R)- Preparation Products And Raw materials
Tag:L-Prolinamide, N-[5-[[[3′-[[[1,6-dihydro-6-oxo-4-(trifluoromethyl)-3-pyridinyl]carbonyl]amino]-4′-(4-methyl-1-piperazinyl)[1,1′-biphenyl]-4-yl]carbonyl]amino]-1-oxopentyl]-3-methyl-L-valyl-4-hydroxy-N-[[4-(4-methyl-5-thiazolyl)phenyl]methyl]-, (4R)-(2737222-94-3) Related Product Information