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Merck

주요 문서

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901493

(S,R,S)-AHPC-PEG1-NH2 hydrochloride

≥95%

동의어(들):

(2S,4R)-1-((S)-2-(2-(2-Aminoethoxy)acetamido)-3,3-dimethylbutanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide hydrochloride, Crosslinker–E3 Ligase ligand conjugate, Protein degrader building block for PROTAC® research, Template for synthesis of targeted protein degrader, VH032 conjugate

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제품정보 (DICE 배송 시 비용 별도)

실험식(Hill 표기법):
C26H37N5O5S · xHCl
Molecular Weight:
531.67 (free base basis)
MDL number:
MFCD32173775
UNSPSC Code:
12352101
NACRES:
NA.22
Assay:
≥95%
Form:
powder or crystals
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도움 문의

ligand

VH032

Quality Level

100

assay

≥95%

form

powder or crystals

reaction suitability

reactivity: carboxyl reactive, reagent type: ligand-linker conjugate

functional group

amine

storage temp.

2-8°C

SMILES string

O=C(NCC1=CC=C(C2=C(C)N=CS2)C=C1)[C@H](C[C@@H](O)C3)N3C([C@H](C(C)(C)C)NC(COCCN)=O)=O.Cl

InChI

1S/C26H37N5O5S.ClH/c1-16-22(37-15-29-16)18-7-5-17(6-8-18)12-28-24(34)20-11-19(32)13-31(20)25(35)23(26(2,3)4)30-21(33)14-36-10-9-27;/h5-8,15,19-20,23,32H,9-14,27H2,1-4H3,(H,28,34)(H,30,33);1H/t19-,20+,23-;/m1./s1

InChI key

NUIXHEJNWPHAAZ-XUXADIIKSA-N

Application

Protein degrader builiding block (S,R,S)-AHPC-PEG1-NH2 (HCl salt) enables the synthesis of molecules for targeted protein degradation and PROTAC (proteolysis-targeting chimeras) technology. This conjugate contains a von Hippel-Lindau (VHL)-recruiting ligand and a PEGylated crosslinker with pendant amine for reactivity with a carboxyl group on the target ligand. Because even slight alterations in ligands and crosslinkers can affect ternary complex formation between the target, E3 ligase, and PROTAC, many analogs are prepared to screen for optimal target degradation. When used with other protein degrader building blocks with a pendant amine, parallel synthesis can be used to more quickly generate PROTAC libraries that feature variation in crosslinker length, composition, and E3 ligase ligand.

Automate your VHL-PEG based PROTACs with Synple Automated Synthesis Platform (SYNPLE-SC002)

Other Notes

Technology Spotlight: Degrader Building Blocks for Targeted Protein Degradation

Portal: Building PROTAC® Degraders for Targeted Protein Degradation

Targeted Protein Degradation by Small Molecules

Small-Molecule PROTACS: New Approaches to Protein Degradation

Targeted Protein Degradation: from Chemical Biology to Drug Discovery

Impact of linker length on the activity of PROTACs

Legal Information

PROTAC is a registered trademark of Arvinas Operations, Inc., and is used under license

저장 등급

11 - Combustible Solids

flash_point_f

Not applicable

flash_point_c

Not applicable

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시험 성적서(COA)

Lot/Batch Number

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SKUGTIN
901493-50MG04061834671541