PROTAC HDAC8 Degrader-1

Cat. No.: HY-163920: Data Sheet Handling Instructions
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Degrader-1 (compound Z16) is a potent and selective HDAC8 PROTAC degrader with an DC₅₀ of 0.27 nM in A549 cells.

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PROTAC HDAC8 Degrader-1 Chemical Structure

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•Related Small Molecules:

•Related Proteins:

View All PROTACs Isoform Specific Products:

View All Isoforms

von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

View All HDAC Isoform Specific Products:

View All Isoforms

HDAC HDAC1 HDAC2 HDAC3 HDAC4 HDAC5 HDAC6 HDAC7 HDAC8 HDAC9 HDAC10 HDAC11 HD1 HD2

Biological Activity
Purity & Documentation
References
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Description

Degrader-1 (compound Z16) is a potent and selective HDAC8 PROTAC degrader with an DC₅₀ of 0.27 nM in A549 cells^[1].

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	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]
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]

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

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]