PROTAC HDAC6 degrader 1
PROTAC HDAC6 degrader (Compound A6) is a potent and selective PROTAC HDAC6 degrader with a DC50 of 3.5 nM. PROTAC HDAC6 degrader shows promising antiproliferative activity via inducing apoptosis in myeloid leukemia cell lines.
For research use only. We do not sell to patients.
- CAS No.: 2785404-76-2
- Formula: C37H46N6O10
- Molecular Weight:734.80
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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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Biological Activity
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HDAC6 3.5 nM (DC50) |
HDAC6 4.86 nM (IC50) |
HDAC1 0.1 μM (IC50) |
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Cell Line
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Type | Value | Description | References |
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| MOLM-13 | IC50 |
17.4 μM
Compound: A6
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Cytotoxicity against human MOLM-13 cells assessed as reduction in cell viability incubated for 72 hrs by ATP based Celltiter-glo luminescent assay
Cytotoxicity against human MOLM-13 cells assessed as reduction in cell viability incubated for 72 hrs by ATP based Celltiter-glo luminescent assay
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[PMID: 36473103] |
PROTAC HDAC6 degrader (Compound A6) (0.1-10 μM; 6 h) does not degrade HDAC1 but displays inhibitory activity toward HDAC1. PROTAC HDAC6 degrader demonstrates potent HDAC6 degradation as well as hyperacetylation of α-tubulin in U266 and HL-60 cells, confirming that the activity is not restricted to leukemia cell lines[1].
PROTAC HDAC6 degrader (0.5-50 μM) inhibits leukemia cells viability with log IC50 values of 1.2-1.7 μM[1].
PROTAC HDAC6 degrader (8-24 μM; 48 h) induces MOLM13 cell apoptosis and arrests cell cycle at sub-G1 phase[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HL-60 cells
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Concentration:100 nM, 1 μM, 10 μM
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Incubation Time:6 h
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Result:Degraded HDAC6 but not HDAC1. Induced hyperacetylation of α-tubulin and caused hyperacetylation of histone H3.
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Cell Line:Acute myeloid leukemia or AML (HL-60, Kasumi, THP-1, HL-60, SKNO1, and MOLM13) and B-cell acute lymphoblastic leukemia or B-ALL (REH and 697)
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Concentration:0.5-50 μM
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Incubation Time:72 h
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Result:Inhibited cell viability with log IC50 values of 1.2-1.7 μM.
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Cell Line:MOLM13
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Concentration:8, 16 and 24 μM
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Incubation Time:48 h
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Result:Induced caspase 3/7-dependent apoptosis in dose-dependent fashion.
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Cell Line:MOLM13
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Concentration:8, 16 and 24 μM
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Incubation Time:48 h
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Result:Induced a dose-dependent increase in the sub-G1 fraction with a concomitant reduction of cell population in G2/M phase.
Chemical Information
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CAS No. 2785404-76-2
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Molecular Weight 734.80
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Formula C37H46N6O10
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SMILES
O=C(C1=CC=C(C=C1)NC(CCCCCCCNC(COC2=CC=CC(C(N3C4CCC(NC4=O)=O)=O)=C2C3=O)=O)=O)NCCCCCCC(NO)=O
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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 HDAC6 degrader 1 Related Classifications
HY-152133 Related Classifications
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