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JQAD1

JQAD1
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Purity:99.75%
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JQAD1

Catalog No. T41180Cas No. 2417097-18-6
JQAD1 is a potent and selective histone acetyltransferase EP300 degrader (PROTAC®; DC50≤ 31.6 nM); comprises an EP300 inhibitor, A485, joined by a linker to a cereblon E3 ligase ligand. JQAD1 brings about degradation of EP300 in neuroblastoma cell lines in a proteasome-dependent manner. JQAD1 suppresses both H3K27ac and EP300 expression levels and induces apoptosis. JQAD1 suppresses tumors growth in NSG mice xenografted with Kelly cells. CRC and MYCN genes are downregulated in tumors treated with JQAD1. JQAD1 exhibits no significant effect on coactivator CBP at concentrations inducing EP300 degradation.
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Pack SizePriceAvailabilityQuantity
1 mg$131In Stock
5 mg$328In Stock
10 mg$498In Stock
25 mg$812In Stock
50 mg$1,130In Stock
100 mg$1,520In Stock
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Product Introduction

Bioactivity
Description
JQAD1 is a potent and selective histone acetyltransferase EP300 degrader (PROTAC®; DC50≤ 31.6 nM); comprises an EP300 inhibitor, A485, joined by a linker to a cereblon E3 ligase ligand. JQAD1 brings about degradation of EP300 in neuroblastoma cell lines in a proteasome-dependent manner. JQAD1 suppresses both H3K27ac and EP300 expression levels and induces apoptosis. JQAD1 suppresses tumors growth in NSG mice xenografted with Kelly cells. CRC and MYCN genes are downregulated in tumors treated with JQAD1. JQAD1 exhibits no significant effect on coactivator CBP at concentrations inducing EP300 degradation.
In vitro
JQAD1 (0.5 or 1 μ M; 6-96 h) treatment led to early time-dependent induction of sub-G1 peak, indicating that apoptosis of Kelly and NGP cells. JQAD1 (1 μ M; 12-36 h) induced apoptosis of Kelly NB cell. JQAD1 (0.5 μ M; 24 h) treated cells showed up-regulation of BH3 effectors BIM, BID and PUMA, pro-apoptotic mediator BAX and its inhibitors BCL2 and MCL1. JQAD1 (0.5 and 1 μ M; 24 h) destroy expression of MYCN. JQAD1 (0.5 μ M; 24 h) lead to H3K27ac deletion on chromatin. JQAD1 (1.2 nM-20 μ M; 5 days) has extensive CRBN-dependent anti-tumor activity across cancer cell lines. JQAD1 induced degradation of EP300 in a time-dependent manner, at the earliest 16 hours [1].
In vivo
JQAD1 (40 mg/kg; i.p.; once a day, for 21 days) inhibits the tumor growth in NSG mice transplanted with Kelly NB cells [1].
Chemical Properties
Molecular Weight932.95
FormulaC48H52F4N6O9
Cas No.2417097-18-6
Storage & Solubility Information
Storage Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Solubility Information
DMSO: 90.0 mg/mL (96.5 mM)
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM1.0719 mL5.3593 mL10.7187 mL53.5934 mL
5 mM0.2144 mL1.0719 mL2.1437 mL10.7187 mL
10 mM0.1072 mL0.5359 mL1.0719 mL5.3593 mL
20 mM0.0536 mL0.2680 mL0.5359 mL2.6797 mL
50 mM0.0214 mL0.1072 mL0.2144 mL1.0719 mL

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