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Cat. No.: HY-163920

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PROTAC HDAC8 Degrader-1

Degrader-1 (compound Z16) is a potent and selective HDAC8 PROTAC degrader with an DC₅₀ of 0.27 nM in A549 cells.
(Pink: HDAC8 ligand (HY-163921); Blue: Cereblon ligand (HY-150799); Black: linker).

For research use only. We do not sell to patients.

CAS No.: 3057302-08-3
Formula: C₃₂H₄₄N₆O₄
Molecular Weight:576.73

Storage:

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

Data Sheet (262 KB)

PROTAC HDAC8 Degrader-1 Chemical Structure

CAS No.: 3057302-08-3

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Fluorescent Dye

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

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

Biological Activity

Description

Degrader-1 (compound Z16) is a potent and selective HDAC8 PROTAC degrader with an DC₅₀ of 0.27 nM in A549 cells^[1]. (Pink: HDAC8 ligand (HY-163921); Blue: Cereblon ligand (HY-150799); Black: linker).

IC₅₀ & Target

HDAC8

All PROTACs Isoforms :

All HDAC Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	17.5 μM Compound: Z16; CZH-726	Antiproliferative activity against human A549 cells assessed as inhibition of cell viability preincubated with Z-VAD-FMK for 1 hr followed by compound addition and measured after 72 hrs by CellTiter 96 Aqueous One Solution Cell Proliferation Assay Antiproliferative activity against human A549 cells assessed as inhibition of cell viability preincubated with Z-VAD-FMK for 1 hr followed by compound addition and measured after 72 hrs by CellTiter 96 Aqueous One Solution Cell Proliferation Assay	[PMID: 39089850]
A549	IC₅₀	7.5 μM Compound: Z16; CZH-726	Antiproliferative activity against human A549 cells assessed as inhibition of cell viability preincubated with necrostatin-1 for 1 hr followed by compound addition and measured after 72 hrs by CellTiter 96 Aqueous One Solution Cell Proliferation Assay Antiproliferative activity against human A549 cells assessed as inhibition of cell viability preincubated with necrostatin-1 for 1 hr followed by compound addition and measured after 72 hrs by CellTiter 96 Aqueous One Solution Cell Proliferation Assay	[PMID: 39089850]
A549	IC₅₀	7.7 μM Compound: Z16; CZH-726	Antiproliferative activity against human A549 cells assessed as inhibition of cell growth measured after 72 hrs by MTS assay Antiproliferative activity against human A549 cells assessed as inhibition of cell growth measured after 72 hrs by MTS assay	[PMID: 39089850]
HCT-116	IC₅₀	1.4 μM Compound: Z16; CZH-726	Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell growth measured after 72 hrs by MTS assay Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell growth measured after 72 hrs by MTS assay	[PMID: 39089850]
HCT-116	IC₅₀	1.5 μM Compound: Z16; CZH-726	Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell viability preincubated with chloroquine for 1 hr followed by compound addition and measured after 72 hrs by CellTiter 96 Aqueous One Solution Cell Proliferation Assay Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell viability preincubated with chloroquine for 1 hr followed by compound addition and measured after 72 hrs by CellTiter 96 Aqueous One Solution Cell Proliferation Assay	[PMID: 39089850]
HCT-116	IC₅₀	1.7 μM Compound: Z16; CZH-726	Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell viability preincubated with ferrostatin-1 for 1 hr followed by compound addition and measured after 72 hrs by CellTiter 96 Aqueous One Solution Cell Proliferation Assay Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell viability preincubated with ferrostatin-1 for 1 hr followed by compound addition and measured after 72 hrs by CellTiter 96 Aqueous One Solution Cell Proliferation Assay	[PMID: 39089850]
HCT-116	IC₅₀	1.8 μM Compound: Z16; CZH-726	Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell viability preincubated with necrostatin-1 for 1 hr followed by compound addition and measured after 72 hrs by CellTiter 96 Aqueous One Solution Cell Proliferation Assay Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell viability preincubated with necrostatin-1 for 1 hr followed by compound addition and measured after 72 hrs by CellTiter 96 Aqueous One Solution Cell Proliferation Assay	[PMID: 39089850]
HCT-116	IC₅₀	3.8 μM Compound: Z16; CZH-726	Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell viability preincubated with Z-VAD-FMK for 1 hr followed by compound addition and measured after 72 hrs by CellTiter 96 Aqueous One Solution Cell Proliferation Assay Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell viability preincubated with Z-VAD-FMK for 1 hr followed by compound addition and measured after 72 hrs by CellTiter 96 Aqueous One Solution Cell Proliferation Assay	[PMID: 39089850]
HEL	IC₅₀	7.7 μM Compound: Z16; CZH-726	Antiproliferative activity against HEL cells assessed as inhibition of cell growth measured after 72 hrs by MTS assay Antiproliferative activity against HEL cells assessed as inhibition of cell growth measured after 72 hrs by MTS assay	[PMID: 39089850]
Jurkat	IC₅₀	1.5 μM Compound: Z16; CZH-726	Antiproliferative activity against human Jurkat cells assessed as inhibition of cell viability preincubated with Z-VAD-FMK for 1 hr followed by compound addition and measured after 72 hrs by CellTiter 96 Aqueous One Solution Cell Proliferation Assay Antiproliferative activity against human Jurkat cells assessed as inhibition of cell viability preincubated with Z-VAD-FMK for 1 hr followed by compound addition and measured after 72 hrs by CellTiter 96 Aqueous One Solution Cell Proliferation Assay	[PMID: 39089850]
Jurkat	IC₅₀	1.7 μM Compound: Z16; CZH-726	Antiproliferative activity against human Jurkat cells assessed as inhibition of cell growth measured after 72 hrs by MTS assay Antiproliferative activity against human Jurkat cells assessed as inhibition of cell growth measured after 72 hrs by MTS assay	[PMID: 39089850]
Jurkat	IC₅₀	2 μM Compound: Z16; CZH-726	Antiproliferative activity against human Jurkat cells assessed as inhibition of cell viability preincubated with necrostatin-1 for 1 hr followed by compound addition and measured after 72 hrs by CellTiter 96 Aqueous One Solution Cell Proliferation Assay Antiproliferative activity against human Jurkat cells assessed as inhibition of cell viability preincubated with necrostatin-1 for 1 hr followed by compound addition and measured after 72 hrs by CellTiter 96 Aqueous One Solution Cell Proliferation Assay	[PMID: 39089850]
Jurkat	IC₅₀	2.5 μM Compound: Z16; CZH-726	Antiproliferative activity against human Jurkat cells assessed as inhibition of cell viability preincubated with chloroquine for 1 hr followed by compound addition and measured after 72 hrs by CellTiter 96 Aqueous One Solution Cell Proliferation Assay Antiproliferative activity against human Jurkat cells assessed as inhibition of cell viability preincubated with chloroquine for 1 hr followed by compound addition and measured after 72 hrs by CellTiter 96 Aqueous One Solution Cell Proliferation Assay	[PMID: 39089850]
Jurkat	IC₅₀	2.8 μM Compound: Z16; CZH-726	Antiproliferative activity against human Jurkat cells assessed as inhibition of cell viability preincubated with ferrostatin-1 for 1 hr followed by compound addition and measured after 72 hrs by CellTiter 96 Aqueous One Solution Cell Proliferation Assay Antiproliferative activity against human Jurkat cells assessed as inhibition of cell viability preincubated with ferrostatin-1 for 1 hr followed by compound addition and measured after 72 hrs by CellTiter 96 Aqueous One Solution Cell Proliferation Assay	[PMID: 39089850]
THP-1	IC₅₀	>33.3 μM Compound: Z16; CZH-726	Antiproliferative activity against human THP-1 cells assessed as inhibition of cell viability preincubated with Z-VAD-FMK for 1 hr followed by compound addition and measured after 72 hrs by CellTiter 96 Aqueous One Solution Cell Proliferation Assay Antiproliferative activity against human THP-1 cells assessed as inhibition of cell viability preincubated with Z-VAD-FMK for 1 hr followed by compound addition and measured after 72 hrs by CellTiter 96 Aqueous One Solution Cell Proliferation Assay	[PMID: 39089850]
THP-1	IC₅₀	1.8 μM Compound: Z16; CZH-726	Antiproliferative activity against human THP-1 cells assessed as inhibition of cell growth measured after 72 hrs by MTS assay Antiproliferative activity against human THP-1 cells assessed as inhibition of cell growth measured after 72 hrs by MTS assay	[PMID: 39089850]

Chemical Information

CAS No. 3057302-08-3
Molecular Weight 576.73
Formula C₃₂H₄₄N₆O₄
SMILES

O=C(NCC1=CC=C(C(NNCCCCCC)=O)C=C1)CN2CCC(C3=CC=C(NC(CC4)C(NC4=O)=O)C=C3)CC2
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

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (262 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Zhao C, et al. Exploration of Hydrazide-Based HDAC8 PROTACs for the Treatment of Hematological Malignancies and Solid Tumors. J Med Chem. 2024 Aug 1. [Content Brief]

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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.

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MOQ

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100 mg

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

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PROTAC HDAC8 Degrader-1

All PROTACs Isoforms

All HDAC Isoforms

Biological Activity

Chemical Information

Purity & Documentation

References

Calculators

Help & FAQs

PROTAC HDAC8 Degrader-1 Related Classifications

HY-163920 Related Classifications