JQAD1( —— )

Catalog No. M35258 CAS 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.

Purity : >98% (HPLC)

COA

Datasheet

HNMR

HPLC

MSDS

Handing Instructions

Size	Price / USD	Stock	Quantity
5MG	312	In Stock
10MG	473	In Stock
25MG	771	In Stock
50MG	1051	In Stock
100MG	1414	In Stock
200MG	Get Quote	In Stock
500MG	Get Quote	In Stock
1G	Get Quote	In Stock

Get Quotation Bulk Inquiry Add to Cart

Biological Information

Product Name

JQAD1
Note

Research use only, not for human use.
Brief 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.
Description

JQAD1 is a CRBN-dependent PROTAC that selectively targets EP300 for degradation. JQAD1 suppresses EP300 expression and the H3K27ac modification. JQAD1 induces apoptosis. JQAD1 can be used in research of cancer.
In Vitro

Western Blot Analysis Cell Line:MYCN-amplified NB cells Concentration:0.1, 0.5, 1, 3, 5, and 10 μM Incubation Time:24 h Result:Demonstrated a dose-dependent decrease in EP300 expression along with a parallel loss of the H3K27ac modification. Induced selective loss of EP300 expression coincident with cleavage of PARP1, signaling the onset of apoptosis.Western Blot Analysis Cell Line:Kelly NB cells Concentration:1 μM Incubation Time:12, 24, and 36 hours Result:Increased the expression of cleaved caspase-3 and cleaved PARP1 in a dose-dependent manner.
In Vivo

Animal Model:NSG mice with Kelly NB cell xenograftsDosage:40 mg/kg Administration:Intraperitoneal injection; daily, for 21 days Result:Suppressed tumor growth and prolonged survival.Animal Model:CD1 miceDosage:10 mg/kg Administration:Intraperitoneal injection (Pharmacokinetic Analysis) Result:Had a half-life of 13.3 (±3.37 SD) hours in murine serum, with a Cmax of 7 μmol/L.
Synonyms

——
Pathway

Chromatin/Epigenetic
Target

Epigenetic Reader Domain
Recptor

Epigenetic Reader Domain | PROTACs
Research Area

——
Indication

——

Chemical Information

CAS Number

2417097-18-6
Formula Weight

932.95
Molecular Formula

C48H52F4N6O9
Purity

>98% (HPLC)
Solubility

In Vitro:?DMSO : 100 mg/mL (107.19 mM; Ultrasonic )
SMILES

O=C1[C@@]2(C=3C(CC2)=CC(NC(CCCCCCCCCCCNC=4C=C5C(=CC4)C(=O)N(C5=O)C6C(=O)NC(=O)CC6)=O)=CC3)OC(=O)N1CC(N(CC7=CC=C(F)C=C7)[C@H](C(F)(F)F)C)=O
Chemical Name

——

Shipping & Storage Information

Storage

(-20℃)
Shipping

With Ice Pack
Stability

≥ 2 years

Reference

1. Durbin AD, et, al. EP300 Selectively Controls the Enhancer Landscape of MYCN-Amplified Neuroblastoma. Cancer Discov. 2022 Mar 1;12(3):730-751.?

Calculator

Molecular Weight Calculator

Dilution Calculator

Molarity Calculator

molnova catalog

Product			Quantity Required*
Name *			E-mail Address *
Organization *			Phone Number
Remarks