HDAC1 Degrader-1
HDAC1 Degrader-1 is a HDAC1 degrader with an IC50 of 192.3 nM. HDAC1 Degrader-1 induces degradation of HDAC1 in multiple myeloma cells via the proteasome system and enhances apoptosis of multiple myeloma cells. HDAC1 Degrader-1 can be used for research on multiple myeloma.
For research use only. We do not sell to patients.
- Formula: C26H37N3O4
- Molecular Weight:455.59
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
IC50 & Target
[1]|
HDAC1 192.3 nM (IC50) |
HDAC2 295.0 nM (IC50) |
HDAC6 5.2 nM (IC50) |
α-Tubulin |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
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| MM.1S | IC50 |
3.97 μM
Compound: 1a
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Antiproliferative activity against human MM.1S cells assessed as inhibition of cell growth incubated for 72 hrs by microplate photometer analysis
Antiproliferative activity against human MM.1S cells assessed as inhibition of cell growth incubated for 72 hrs by microplate photometer analysis
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[PMID: 38116436] |
In Vitro
HDAC1 Degrader-1 (compound 1A) inhibits the viability of MM.1S multiple myeloma cells with an IC50 of 3.97 μM; it also inhibits intracellular HDAC activity in MM.1S multiple myeloma cells with an IC50 of 1.12 μM[1].
HDAC1 Degrader-1 inhibits the activity of purified HDAC1 protein with an IC50 of 192.3 nM; it inhibits the activity of purified HDAC2 protein with an IC50 of 295.0 nM; and it inhibits the activity of purified HDAC6 protein with an IC50 of 5.2 nM[1].
HDAC1 Degrader-1 (20 μM; 24 h) significantly degrades HDAC1 protein in MM.1S multiple myeloma cells, slightly reduces HDAC2 levels, but has no effect on HDAC6 levels[1].
HDAC1 Degrader-1 (20 μM; 24 h) induces significant hyperacetylation of α-tubulin and histone H3 in MM.1S multiple myeloma cells, confirming its ability to bind HDAC6 and HDAC1-3 intracellularly[1].
HDAC1 Degrader-1 (20 μM; 48 h) significantly increases early and late apoptosis in MM.1S multiple myeloma cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MM.1S multiple myeloma cells
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Concentration:20 μM
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Incubation Time:24 h
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Result:Induced significant degradation of HDAC1 protein, reducing HDAC1 levels to approximately 50% of vehicle control levels.
Caused a slight reduction in HDAC2 protein levels.
Had no effect on HDAC6 protein levels.\nInduced pronounced hyperacetylation of α-tubulin (confirming HDAC6 target engagement).
Induced hyperacetylation of histone H3 (confirming HDAC1-3 target engagement).
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Cell Line:MM.1S multiple myeloma cells
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Concentration:20 μM
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Incubation Time:48 h
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Result:Significantly increased the percentage of early and late apoptotic MM.1S cells, with an apoptosis potency matching its cell viability inhibitory activity.
Chemical Information
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Molecular Weight 455.59
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Formula C26H37N3O4
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SMILES
O=C(NCCCCCCC(NO)=O)C1=CC=C(NC(CC2(C3)C[C@@H](C4)C[C@H]3C[C@@H]4C2)=O)C=C1
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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)
HDAC1 Degrader-1 Related Classifications
HY-157216 Related Classifications
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