1. PROTAC Neuronal Signaling
  2. SNIPERs Huntingtin
  3. 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)).

For research use only. We do not sell to patients.

PROTAC HTT Degrader-1

PROTAC HTT Degrader-1 Chemical Structure

CAS No. : 2133321-59-0

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Description

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.
Molecular Weight

661.85

Formula

C36H47N5O5S

CAS No.
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

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

Purity & Documentation
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PROTAC HTT Degrader-1
Cat. No.:
HY-184480
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