2. PROTAC Epigenetics
  3. PROTACs Epigenetic Reader Domain
  4. QA-68

QA-68 (QA-68-ZU81) is an effective PROTAC-class BRD9 degrader. QA-68 can inhibit cell cycle progression and cell colony formation. QA-68 has antiproliferative activity against acute myeloid leukemia (AML) cell lines. QA-68 can be formed by a target protein ligand (red part) EA-89 (HY-170314), an E3 ubiquitin ligase ligand (blue part) Lenalidomide-I (HY-131318), and a PROTAC linker (black part) Ethyne-C2-Pip-CO-Pip-Boc (HY-170315). E3 ubiquitin ligase and linker can form Lenalidomide-ethyne-C2-Pip-CO-Pip (HY-170319); the active control for the target protein ligand is EA-89-Succinic acid (HY-170317).

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QA-68 Chemical Structure

QA-68 Chemical Structure

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QA-68 Related Antibodies

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Description

QA-68 (QA-68-ZU81) is an effective PROTAC-class BRD9 degrader. QA-68 can inhibit cell cycle progression and cell colony formation. QA-68 has antiproliferative activity against acute myeloid leukemia (AML) cell lines[1]. QA-68 can be formed by a target protein ligand (red part) EA-89 (HY-170314), an E3 ubiquitin ligase ligand (blue part) Lenalidomide-I (HY-131318), and a PROTAC linker (black part) Ethyne-C2-Pip-CO-Pip-Boc (HY-170315). E3 ubiquitin ligase and linker can form Lenalidomide-ethyne-C2-Pip-CO-Pip (HY-170319); the active control for the target protein ligand is EA-89-Succinic acid (HY-170317).

IC50 & Target[1]

BRD9

 

In Vitro

QA-68 (0-1000 nM; 24 h) exhibits antiproliferative activity against MV4-11, SKM-1 and Kasumi-1-luc+ cells, and inhibits BRD9 protein expression in MV4-11, SKM-1, SEM, NALM6, RS4;11[1].
QA-68 (0.1-1000 nM; 4 days) effectively inhibits SKM-1 cell cycle progression[1].
QA-68 (1000 nM; 12 days) inhibits colony formation of additional primary AML bone marrow and PBMC cells[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

QA-68 Related Antibodies

Cell Proliferation Assay[1]

Cell Line: MV4-11, SKM-1 and Kasumi-1-luc+ cells
Concentration: 0-1000 nM
Incubation Time: 24 h
Result: Exhibited concentration-dependent inhibition of proliferation of MV4-11, SKM-1 and Kasumi-1-luc+ cells with IC50s of 1-10 nM in MV4;11 and SKM-1, and IC50 of 10-100 nM in Kasumi-1-luc +, respectively.

Cell Cycle Analysis[1]

Cell Line: SKM-1cells
Concentration: 0.1, 1, 10, 100 and 1000 nM
Incubation Time: 6 days
Result: Effectively inhibited SKM-1 cell cycle progression.

Western Blot Analysis[1]

Cell Line: MV4-11, SKM-1, SEM, NALM6, RS4;11
Concentration: 0, 1, 10, 100 and 1000 nM
Incubation Time: 24 h
Result: Inhibited BRD9 protein in all tested cell lines.
Molecular Weight

1169.42

Formula

C61H72N10O10S2
SMILES

CCCN1C=C(C2=C(C1=O)C=C(C(NC3CCS(CC3)(=O)=O)=O)S2)C4=CC=C(C5=C4)N(C=C5C)CC6CCN(CC6)C(CCC(N7CCN(CC7)C(N8CCN(CC8)CCC#CC9=CC=CC%10=C9CN(C%10=O)C%11CCC(NC%11=O)=O)=O)=O)=O
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Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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QA-68 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

QA-68QA-68-ZU81QA68QA 68PROTACsEpigenetic Reader Domainacute myeloid leukemiaAMLantiproliferativeMV4-11SKM-1SEMNALM6RS4;11Inhibitorinhibitorinhibit

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