HDAC6 degrader-6
HDAC6 degrader-6 is a HyT degrader targeting HDAC6, with a DC50 of 6.357 μM in MOLT-4 cells. HDAC6 degrader-6 induces apoptosis. HDAC6 degrader-6 can be used for research on leukemia.
(Pink: HDAC6 Target protein ligand; Blue: HyT E3 ligase ligand; Black: linker (HY-W018678)).
For research use only. We do not sell to patients.
- Formula: C37H56N4O9
- Molecular Weight:700.86
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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]|
HDAC6 6.357 μM (DC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| MOLT-4 | IC50 |
0.18 μM
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Antiproliferative activity against human MOLT-4 leukemia cells assessed as reduction in cell viability incubated for 48 hrs by tetramethyl azole blue colorimetric method.
Antiproliferative activity against human MOLT-4 leukemia cells assessed as reduction in cell viability incubated for 48 hrs by tetramethyl azole blue colorimetric method.
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42556264 |
| K562 | IC50 |
0.76 μM
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Antiproliferative activity against human K562 leukemia cells assessed as reduction in cell viability incubated for 48 hrs by tetramethyl azole blue colorimetric method.
Antiproliferative activity against human K562 leukemia cells assessed as reduction in cell viability incubated for 48 hrs by tetramethyl azole blue colorimetric method.
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42556264 |
In Vitro
HDAC6 degrader-6 (compound Q5) (48 h) exhibits potent antiproliferative activity against MOLT-4 and K562 leukemia cell lines[1].
HDAC6 degrader-6 (0.01-100 μM; 24 h) selectively degrades HDAC6 with a DC50 of 6.357 μM and a Dmax of 87.31% in MOLT-4 cells[1].
HDAC6 degrader-6 (10 μM; 4-48 h) induces time-dependent degradation of HDAC6 in MOLT-4 cells, with effects persisting for 12 h after washout[1].
HDAC6 degrader-6 (10 μM; 24 h) effectively degrades HDAC6 in both MOLT-4 and K562 cell lines, demonstrating a broad mechanism of action[1].
HDAC6 degrader-6 (100 μM; 1 h) binds tightly to HDAC6, enhancing its thermal stability, but not to HDAC1[1].
HDAC6 degrader-6 (10 μM; 12 h) may disrupt the correct folding of HDAC6/HDAC1, making them unstable misfolded proteins[1].
HDAC6 degrader-6 (10 μM; 12 h) degrades HDAC6 via the ubiquitin-proteasome system, requiring Cullin-RING ligase-mediated ubiquitination[1].
HDAC6 degrader-6 shows selectivity for HDAC6 over HDAC1 due to structural differences in the binding pockets, with docking scores of −9.8076 and −7.1668, respectively[1].
HDAC6 degrader-6 (10 μM; 24 h) selectively targets HDAC6 over HDAC10[1].
HDAC6 degrader-6 (1-10 μM; 24 h) induces apoptosis in both K562 and MOLT-4 leukemia cell lines in a dose-dependent manner, with MOLT-4 cells exhibiting higher sensitivity[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MOLT-4
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Concentration:0.01 μM, 0.1 μM, 1μM, 10 μM, 100 μM
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Incubation Time:24 h
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Result:Displayed maximum HDAC1/6 protein degradation efficacy with a Dmax exceeding 87.31% at 100 μM and a DC50 of 6.357 μM toward HDAC6.
Induced significant downregulation of HDAC6 at 10 μM, while HDAC1 protein levels remained unchanged.
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Cell Line:MOLT-4
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Concentration:10 μM
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Incubation Time:4, 8, 12, 24, 48 h (continuous); 48 h (washout)
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Result:Induced a 68% reduction in HDAC6 levels after 24 h of incubation.
Induced HDAC6 degradation activity that persisted for 12 h after washout, with HDAC6 levels nearly fully recovering by 48 h.
HDAC1 protein levels remained unchanged throughout the observation period.
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Cell Line:MOLT-4 and K562
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Concentration:10 μM
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Incubation Time:24 h
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Result:Degraded HDAC6 in MOLT-4 and K562 cells with degradation rates of 84.9% and 67.3%, respectively.
Exhibited weaker HDAC1 degradation in MOLT-4 cells (34.7%) but relatively pronounced effects in K562 cells (69.5%).
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Cell Line:MOLT-4
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Concentration:10 μM
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Incubation Time:12 h
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Result:Induced degradation of both HDAC1 and HDAC6.
When Hsp70 inhibitor was added, HDAC1 could be reversed but HDAC6 was still degraded.
When Hsp90 inhibitor was added, the protein levels of both HDAC1 and HDAC6 were restored.
When both inhibitors were added, the protein level completely recovered.\nAttenuated the ability to induce HDAC6 degradation when pretreated with MG132 and/or MLN4924.
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Cell Line:K562 and MOLT-4
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Concentration:1 μM, 10 μM
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Incubation Time:24 h
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Result:Increased the population of apoptotic K562 cells in a dose-dependent manner, with a total apoptotic rate of approximately 45.5% at 10 μM.
Induced an apoptotic rate of 86.8% in MOLT-4 cells at 10 μM.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c nude mice (female)[1]
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Dosage:5 mg/kg; 10 mg/kg
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Administration:i.v.; every 2 days; 18 days
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Result:Inhibited tumor growth with a TGI of 84.21% at 10 mg/kg and 53.62% at 5 mg/kg.
Induced dose-dependent pathological damage in tumor tissues.
Reduced HDAC6 protein expression in tumor tissues in a dose-dependent manner without affecting HDAC1 levels.
Chemical Information
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Molecular Weight 700.86
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Formula C37H56N4O9
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SMILES
ONC(CCCCCCC(NC1=CC=C(NC(CCCCCCCNC([C@@]2(C)O[C@]3([H])O[C@@]4(C)CC[C@]5([H])[C@@]3(OO4)[C@@]2([H])CC[C@H]5C)=O)=O)C=C1)=O)=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)
HDAC6 degrader-6 Related Classifications
HY-189299 Related Classifications
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