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製品番号: HY-184480

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PROTAC HTT Degrader-1

PROTAC HTT Degrader-1 is a cIAP1-recruiting Htt PROTAC degrader. PROTAC HTT Degrader-1 recruits cIAP1 to mHtt or wtHtt and induces their degradation via the ubiquitin-proteasome system. PROTAC HTT Degrader-1 can be used in research related to Huntington's disease.
(Pink: Huntingtin ligand (HY-W040269); Blue: cIAP1 ligand (HY-B0134); Black: linker (HY-W007545)).

商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。

CAS 番号: 2133321-59-0
分子式: C₃₆H₄₇N₅O₅S
分子量:661.85

保管条件:

Please store the product under the recommended conditions in the Certificate of Analysis.

PROTAC HTT Degrader-1 構造式

CAS 番号: 2133321-59-0

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製品説明

PROTAC HTT Degrader-1 is a cIAP1-recruiting Htt PROTAC degrader. PROTAC HTT Degrader-1 recruits cIAP1 to mHtt or wtHtt and induces their degradation via the ubiquitin-proteasome system. PROTAC HTT Degrader-1 can be used in research related to Huntington's disease^[1]. (Pink: Huntingtin ligand (HY-W040269); Blue: cIAP1 ligand (HY-B0134); Black: linker (HY-W007545)).

体外実験

PROTAC HTT Degrader-1 (Compound 1) (10 μM; 24-48 h) post-transcriptionally reduces both mHtt levels in HD patient fibroblasts and wtHtt levels in normal fibroblasts, with observable reduction at 10 μM after 24 h and 48 h incubation, and exhibits a dose-dependent effect on mHtt levels^[1].
PROTAC HTT Degrader-1 binds to in vitro-formed 62Q peptide aggregates^[1].
PROTAC HTT Degrader-1 (3-30 μM) induces interaction between 62Q aggregates and cIAP1's BIR3 domain at concentrations of 3 μM, 10 μM, and 30 μM, as measured by ELISA absorbance at 450 nm^[1].
PROTAC HTT Degrader-1 selectively reduces levels of both pathogenic 145QHtt-EGFP and non-pathogenic 23QHtt-EGFP in transiently transfected HeLa cells, reduces 145QHtt-EGFP aggregate numbers, and does not affect standalone EGFP levels, tubulin levels, or cell viability^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis^[1]

Cell Line:

Huntington's disease patient fibroblasts (HD fb), normal subject fibroblasts (normal fb)
Concentration:

10 μM; dose-dependent concentrations (unspecified)
Incubation Time:

24 h, 48 h; unspecified
Result:

Reduced mutant huntingtin (mHtt) levels in both HD patient fibroblast lines at 10 μM after 24 h and 48 h incubation.
Reduced wild-type Htt (wtHtt) levels in normal fibroblasts at 10 μM after 24 h and 48 h incubation.
Induced dose-dependent reduction in mHtt levels in HD fibroblasts.
Did not affect HTT gene mRNA abundance in HD fibroblasts, as confirmed by quantitative PCR analysis.

化学情報

CAS 番号 2133321-59-0
分子量 661.85
分子式 C₃₆H₄₇N₅O₅S
SMILES

O=C(N[C@@H](CC(C)C)C(NCCOCCOCCNC(C=C1)=CC=C1C2=NC3=CC=C(C)C=C3S2)=O)[C@@H](O)[C@H](N)CC4=CC=CC=C4
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件

Please store the product under the recommended conditions in the Certificate of Analysis.

純度とドキュメンテーション

取扱説明書 (2659 KB)

参考文献

[1]. Tomoshige S, et al. Discovery of Small Molecules that Induce the Degradation of Huntingtin. Angew Chem Int Ed Engl. 2017 Sep 11;56(38):11530-11533. [Content Brief]

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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