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Cat. No.: HY-189151

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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

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

PROTAC HDAC8 Degrader-5 Chemical Structure

CAS No.: 3057302-21-0

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

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.^[1]. (Pink: HDAC8 ligand (HY-124782); Blue: Cereblon ligand (HY-10984); Black: linker).

IC₅₀ & Target

^[1]

HDAC8

1.8 nM (DC₅₀)

HDAC8

4.7 nM (DC₅₀)

HDAC6

38 nM (DC₅₀)

Caspase-3

Caspase-7

α-Tubulin

All PROTACs Isoforms :

All HDAC Isoforms :

All Caspase Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
Jurkat	GI50	2.4 μM	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.	37098288

In Vitro

OthersAnti-cancerApoptosis

Others

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 D_max 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].

Anti-cancer

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].

Anti-cancer

Apoptosis

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.

Western Blot Analysis^[1]

Cell Line:

MDA-MB-231
Concentration:

1 μM; 10 μM
Incubation Time:

24 h
Result:

Decreased HDAC8 levels by 94% at 1 μM.
Decreased HDAC8 levels by 62% at 10 μM.

Western Blot Analysis^[1]

Cell Line:

MDA-MB-231
Concentration:

0.5 μM
Incubation Time:

0, 2, 4, 6, 8, 24, and 48 h
Result:

Showed rapid degradation with a maximum effect of 98% reached after 4 h and remained up to 48 h.

Western Blot Analysis^[1]

Cell Line:

Jurkat
Concentration:

1.52, 4.57, 13.7, 41.2, 123.5, 370.4, 1111, 3333, 10000 nM
Incubation Time:

24 h
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.

Cell Migration Assay ^[1]

Cell Line:

MDA-MB-231
Concentration:

0.5, 2.5, 5 μM
Incubation Time:

24 h
Result:

Inhibited migration over 40% at 2.5 and 5 μM.

Apoptosis Analysis^[1]

Cell Line:

Jurkat
Concentration:

1, 3, 10 μM
Incubation Time:

48 h
Result:

Induced over 40% Jurkat cell apoptosis at 3 μM.
Induced over 60% Jurkat cell apoptosis at 10 μM.

Related Protocols :

Chemical Information

CAS No. 3057302-21-0
Molecular Weight 699.75
Formula C₃₇H₄₁N₅O₉
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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Zhao C, et al. Discovery of highly potent HDAC8 PROTACs with anti-tumor activity. Bioorganic chemistry. 2023 Jul;136:106546.

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Bioz

MOQ

Minimum order quantity

100 mg

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Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
Chemical Information
Purity & Documentation
References

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PROTAC HDAC8 Degrader-5

All PROTACs Isoforms

All HDAC Isoforms

All Caspase Isoforms