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.
- CAS No.: 2133321-59-0
- Formula: C36H47N5O5S
- Molecular Weight:661.85
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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.
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Cell Line:Huntington's disease patient fibroblasts (HD fb), normal subject fibroblasts (normal fb)
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Concentration:10 μM; dose-dependent concentrations (unspecified)
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Incubation Time:24 h, 48 h; unspecified
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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
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CAS No. 2133321-59-0
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Molecular Weight 661.85
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Formula C36H47N5O5S
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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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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
PROTAC HTT Degrader-1 Related Classifications
Cat. No.: HY-184480
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- PROTAC HTT Degrader-1
- 2133321-59-0
- PROTAC HTT Degrader1
- PROTAC HTT Degrader 1
- SNIPERs
- Huntingtin
- BIR3 domain
- Huntington's disease
- HeLa cells
- patient-derived fibroblasts
- mutant huntingtin
- 62Q peptide aggregates
- HD patient fibroblasts
- cellular inhibitor of apoptosis protein 1
- normal fibroblasts
- ubiquitin-proteasome system
- Inhibitor
- inhibitor
- inhibit