Merck, 916684-50MG, A1V2PF2-NHEt-C10-NH2

Name: A1V2PF2-NHEt-C10-NH2
Brand: Merck
SKU: 916684-50MG

Size:50 mg, (S)-1-((S)-2-((S)-2-((10-Aminodecyl)amino)propanamido)-2-cyclohexylacetyl)-N-((S)-1-(ethylamino)-3-(4-fluorophenyl)-1-oxopropan-2-yl)pyrrolidine-2-carboxamide, AVP conjugate for IAP-mediated degrader development" to "AVP conjugate for IAP-mediated protein degrader development, SNIPER building block, ≥95%

Catalog Number: 916684-50MG

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Category

Protein Crosslinkers

Pack Size50 mg

TagsChemistry & Biochemicals Chemical Biology Protein Degrader Building Blocks

CollectionsMerck Cell Culture Supplements & Reagents: Complete Solutions for Research & Bioproduction Merck Roche Life Science Products for PCR, RT‑PCR & Nucleic Acid Purification

Description

Application
Protein degrader building block A1V2PF2-NHEt-C₁₀-NH₂ enables the synthesis of molecules for targeted protein degradation and SNIPER (specific and non-genetic inhibitor of apoptosis protein (IAP)-dependent protein erasers) technology. Developed in partnership with ComInnex, this conjugate contains an in silico-derived IAP-recruiting ligand, an alkyl-chain crosslinker, and a pendant amine for reactivity with an acid on a target warhead. Because even slight alterations in ligands and crosslinkers can affect ternary complex formation between the target, E3 ligase, and protein degrader, many analogs are prepared to screen for optimal target degradation. When used with other protein degrader building blocks with a terminal amine, including CRBN and VHL targeted, parallel synthesis can be used to more quickly generate SNIPER and PROTAC® degrader libraries that feature variation in crosslinker length, composition, and E3 ligase ligand. Learn more about the novel IAP ligands generated through virtual screening of AVP mimetics in our Technology Spotlight.

Building blocks in this series:
916714 A1V2PF2-NHEt
917931 A1V2PF2-NHEt-C₆-NH₂
916684 A1V2PF2-NHEt-C₁₀-NH₂
916935 A1V2PF2-NHEt-PEG₁-NH₂
917192 A1V2PF2-NHEt-PEG₃-NH₂

Technology Spotlight: Degrader Building Blocks with Inhibitor of Apoptosis Protein (IAP) In Silico-Derived Ligands
Other Notes
In Vivo Knockdown of Pathogenic Proteins via Specific and Nongenetic Inhibitor of Apoptosis Protein (IAP)-dependent Protein Erasers (SNIPERs)

SNIPERs−Hijacking IAP activity to induce protein degradation

E3 Ligase Ligands for PROTACs: How They Were Found and How to Discover New Ones
Legal Information
PROTAC is a registered trademark of Arvinas Operations, Inc., and is used under license

Specifications

General

MDL number	MFCD33021729
UNSPSC Code	41116105
NACRES	NA.22
InChI	1S/C37H61FN6O4/c1-3-40-35(46)31(26-28-19-21-30(38)22-20-28)42-36(47)32-18-15-25-44(32)37(48)33(29-16-11-10-12-17-29)43-34(45)27(2)41-24-14-9-7-5-4-6-8-13-23-39/h19-22,27,29,31-33,41H,3-18,23-26,39H2,1-2H3,(H,40,46)(H,42,47)(H,43,45)/t27-,31-,32-,33-/m0/s1
InChI key	HWOUYPPQDSELDI-MKKRQWMVSA-N
SMILES string	C[C@H](NCCCCCCCCCCN)C(N[C@H](C(N1CCC[C@H]1C(N[C@H](C(NCC)=O)CC2=CC=C(C=C2)F)=O)=O)C3CCCCC3)=O
ligand	A1V2PF2
assay	≥95%
form	powder
reaction suitability	reactivity: carboxyl reactive
functional group	amine
storage temp.	2-8°C
Quality Level	100

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