PROTAC HDAC8 Degrader-5
PROTAC HDAC8 Degrader-5 is a selective HDAC8 PROTAC degrader that mediates ubiquitination and proteasomal degradation through the formation of a ternary complex. PROTAC HDAC8 Degrader-5 degrades HDAC8 with a DC50 of 1.8 nM in MDA-MB-231 cells and a DC50 of 4.7 nM in Jurkat cells. PROTAC HDAC8 Degrader-5 inhibits cancer cell migration and proliferation, induces apoptosis through caspase 3/7 activation, and increases acetylated SMC3 and α-tubulin. PROTAC HDAC8 Degrader-5 is useful for cancer-related research, such as leukemia, triple-negative breast cancer, etc..
(Pink: HDAC8 ligand (HY-124782); Blue: Cereblon ligand (HY-10984); Black: linker).
For research use only. We do not sell to patients.
- CAS No.: 3057302-21-0
- Formula: C37H41N5O9
- Molecular Weight:699.75
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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]|
HDAC8 1.8 nM (DC50) |
HDAC8 4.7 nM (DC50) |
HDAC6 38 nM (DC50) |
Caspase-3 |
Caspase-7 |
α-Tubulin |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
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| Jurkat | GI50 |
2.4 μM
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Antiproliferative activity against human Jurkat cells assessed as reduction in cell viability incubated for 72 hrs by MTS assay.
Antiproliferative activity against human Jurkat cells assessed as reduction in cell viability incubated for 72 hrs by MTS assay.
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37098288 |
In Vitro
PROTAC HDAC8 Degrader-5 (CT-4) (1-10 μM; 24 h) significantly induces HDAC8 degradation in MDA-MB-231 cells; and its DC50 in MDA-MB-231 cells is 1.8 nM, showing 21-fold selectivity over HDAC6[1].
PROTAC HDAC8 Degrader-5 (0.5 μM; 0-48 h) induces rapid, potent, and proteasome-dependent HDAC8 degradation in MDA-MB-231 cells[1].
PROTAC HDAC8 Degrader-5 (1.52-10000 nM; 24 h) effectively degrades HDAC8 in Jurkat cells with a DC50 of 4.7 nM and a Dmax of 95%, demonstrating moderate selectivity over HDAC6 and good selectivity over HDAC1 and HDAC3[1].
PROTAC HDAC8 Degrader-5 inhibits human recombinant HDAC8 with an IC50 of 1.6 μM[1].
PROTAC HDAC8 Degrader-5 (0.5-5 μM; 24 h) effectively inhibits the migration of MDA-MB-231 cells in a dose-dependent manner[1].
PROTAC HDAC8 Degrader-5 (72 h) potently inhibits Jurkat cell viability with a GI50 of 2.4 μM; it shows limited antiproliferative activity against MDA-MB-231 cells[1].
PROTAC HDAC8 Degrader-5 (3-10 μM; 48 h) induces apoptosis in Jurkat cells in a dose-dependent manner, with an apoptosis rate exceeding 60% at 10 μM; it induces apoptosis through dose-dependent activation of caspase 3/7[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MDA-MB-231
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Concentration:1 μM; 10 μM
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Incubation Time:24 h
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Result:Decreased HDAC8 levels by 94% at 1 μM.
Decreased HDAC8 levels by 62% at 10 μM.
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Cell Line:MDA-MB-231
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Concentration:0.5 μM
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Incubation Time:0, 2, 4, 6, 8, 24, and 48 h
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Result:Showed rapid degradation with a maximum effect of 98% reached after 4 h and remained up to 48 h.
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Cell Line:Jurkat
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Concentration:1.52, 4.57, 13.7, 41.2, 123.5, 370.4, 1111, 3333, 10000 nM
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Incubation Time:24 h
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Result:Reduced HDAC8 levels with a DC50 value of 4.7 nM and Dmax of 95%.
Showed HDAC6 degradation with a DC50 of 78.5 nM and Dmax of 76%.
Did not show significant impact on the levels of HDAC1 and HDAC3.
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Cell Line:MDA-MB-231
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Concentration:0.5, 2.5, 5 μM
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Incubation Time:24 h
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Result:Inhibited migration over 40% at 2.5 and 5 μM.
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Cell Line:Jurkat
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Concentration:1, 3, 10 μM
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Incubation Time:48 h
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Result:Induced over 40% Jurkat cell apoptosis at 3 μM.
Induced over 60% Jurkat cell apoptosis at 10 μM.
Chemical Information
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CAS No. 3057302-21-0
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Molecular Weight 699.75
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Formula C37H41N5O9
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SMILES
O=C(C1=CC=C(C(OCC2=CC=C(C(NCCCCCCCCNC3=CC=CC(C(N4C5C(NC(CC5)=O)=O)=O)=C3C4=O)=O)C=C2)=C1)OC)NO
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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 HDAC8 Degrader-5 Related Classifications
HY-189151 Related Classifications
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