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安全性情報

936472

Sigma-Aldrich

(S,R,S)-AHPC-pentanoic-acid

≥95%

別名:

6-[[(1S)-1-[[(2S,4R)-4-Hydroxy-2-[[[4-(4-methylthiazol-5-yl)phenyl]methyl]carbamoyl]pyrrolidin-1-yl]carbonyl]-2,2-dimethylpropyl]amino]-6-oxohexanoic acid, 6-[[(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]-6-oxohexanoic acid, L-Prolinamide, N-(5-carboxy-1-oxopentyl)-3-methyl-L-valyl-4-hydroxy-N-[[4-(4-methyl-5-thiazolyl)phenyl]methyl]-, (4R)-

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About This Item

実験式（ヒル表記法）:
C28H38N4O6S
CAS番号:
2172819-74-6
分子量:
558.69
MDL番号:
MFCD32693310
UNSPSCコード:
12352106
NACRES:
NA.22

ligand

VH032

品質水準

100

アッセイ

≥95%

フォーム

powder

色

white to light yellow

保管温度

2-8°C

SMILES記法

C([C@@H](NC(CCCCC(O)=O)=O)[C@](C)(C)C)(=O)N1[C@H](C(NCC2=CC=C(C=C2)C3=C(C)N=CS3)=O)C[C@@H](O)C1

InChI

1S/C28H38N4O6S/c1-17-24(39-16-30-17)19-11-9-18(10-12-19)14-29-26(37)21-13-20(33)15-32(21)27(38)25(28(2,3)4)31-22(34)7-5-6-8-23(35)36/h9-12,16,20-21,25,33H,5-8,13-15H2,1-4H3,(H,29,37)(H,31,34)(H,35,36)/t20-,21+,25-/m1/s1

InChI Key

DKSZOQIYZOVHOL-TYBLODHISA-N

アプリケーション

(S, R, S)-AHPC-pentanoic-acid is a functionalized von Hippel-Lindau (VHL) ligand. It contains a terminal carboxyl group for conjugation with amine linkers. A basic building block for development of a protein degrader library.

Technology Spotlight:

Degrader Building Blocks for Targeted Protein Degradation
Protein Degrader Building Blocks

その他情報

Targeted Protein Degradation by Small Molecules

Destruction of DNA-Binding Proteins by Programmable Oligonucleotide PROTAC (O′PROTAC): Effective Targeting of LEF1 and ERG

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

法的情報

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

保管分類コード

11 - Combustible Solids

WGK

WGK 3

引火点(°F)

Not applicable

引火点(℃)

Not applicable

適用法令

試験研究用途を考慮した関連法令を主に挙げております。化学物質以外については、一部の情報のみ提供しています。 製品を安全かつ合法的に使用することは、使用者の義務です。最新情報により修正される場合があります。WEBの反映には時間を要することがあるため、適宜SDSをご参照ください。

Jan Code

936472-VAR:
936472-BULK:
936472-50MG:

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試験成績書（COA）

Lot/Batch Number
0000303194
0000285132

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文書ライブラリにアクセスする

Jingwei Shao et al.
Advanced science (Weinheim, Baden-Wurttemberg, Germany), 8(20), e2102555-e2102555 (2021-08-17)
DNA-binding proteins, including transcription factors (TFs), play essential roles in various cellular processes and pathogenesis of diseases, deeming to be potential therapeutic targets. However, these proteins are generally considered undruggable as they lack an enzymatic catalytic site or a ligand-binding
Daniel P Bondeson et al.
Annual review of pharmacology and toxicology, 57, 107-123 (2016-10-13)
Protein homeostasis networks are highly regulated systems responsible for maintaining the health and productivity of cells. Whereas therapeutics have been developed to disrupt protein homeostasis, more recently identified techniques have been used to repurpose homeostatic networks to effect degradation of
Kedra Cyrus et al.
Molecular bioSystems, 7(2), 359-364 (2010-10-06)
Conventional genetic approaches have provided a powerful tool in the study of proteins. However, these techniques often preclude selective manipulation of temporal and spatial protein functions, which is crucial for the investigation of dynamic cellular processes. To overcome these limitations
Momar Toure et al.
Angewandte Chemie (International ed. in English), 55(6), 1966-1973 (2016-01-13)
The current inhibitor-based approach to therapeutics has inherent limitations owing to its occupancy-based model: 1) there is a need to maintain high systemic exposure to ensure sufficient in vivo inhibition, 2) high in vivo concentrations bring potential for off-target side effects, and 3) there is
Philipp M Cromm et al.
Cell chemical biology, 24(9), 1181-1190 (2017-06-27)
Traditional pharmaceutical drug discovery is almost exclusively focused on directly controlling protein activity to cure diseases. Modulators of protein activity, especially inhibitors, are developed and applied at high concentration to achieve maximal effects. Thereby, reduced bioavailability and off-target effects can

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