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Cat. No.: 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)).

연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.

CAS No.: 2133321-59-0
화학식: C₃₆H₄₇N₅O₅S
분자량:661.85

보관:

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

PROTAC HTT Degrader-1 Chemical Structure

CAS No.: 2133321-59-0

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- 제품 설명
- In Vitro
Chemical Information
순도&문서
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

제품 설명

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)).

In Vitro

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.

Chemical Information

CAS No. 2133321-59-0
분자량 661.85
화학식 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
선적

Room temperature in continental US; may vary elsewhere.
보관

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

순도&문서

Handling Instructions (2659 KB)

References

[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]

Calculators

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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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MOQ

Minimum order quantity

100 mg

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