JQAD1 - ≥98% , CAS No.2417097-18-6

CAS: 2417097-18-6 Cat. No.: J650351 Molecular Weight: 932.95

GRADE & PURITY ≥98%

Storage

Store at -20°C

Shipped In

Ice chest + Ice pads

Application

PROTAC

Overview

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

JQAD1 suppresses EP300 expression, suppresses the H3K27ac modification, and induces apoptosis, marked by PARP1 cleavage in control Kelly NB cells, but not in CRBN-knockout cells. JQAD1 (0.5 or 1 μM; 6-96 h) treatment resulted in early time-dependent induction of a sub-G1 peak, suggestive of apoptotic cell death in Kelly and NGP cells. JQAD1 (1 μM; 12-36 h) induces Kelly NB cell apoptosis. JQAD1 (0.5 μM; 24 h)-treated cells exhibits upregulation of the proapoptotic BH3-only effectors BIM, BID, and PUMA together with the proapoptotic mediator BAX and its inhibitors BCL2 and MCL1. JQAD1 (0.5 and 1 μM; 24 h) disrupts MYCN expression. JQAD1 (0.5 μM; 24 h) causes loss of H3K27ac at chromatin. JQAD1 (1.2 nM-20 μM; 5 days) has broad CRBN-dependent antineoplastic activity across cancer cell lines. JQAD1 induces EP300 degradation in a time-dependent manner as early as 16 hours. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Western Blot AnalysisCell 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 AnalysisCell 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

JQAD1 (40 mg/kg; i.p.; daily, for 21 d) inhibits tumor growth in NSG mice with Kelly NB cell xenografts . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: NSG mice with Kelly NB cell xenografts Dosage: 40 mg/kg Administration: Intraperitoneal injection; daily, for 21 days Result: Suppressed tumor growth and prolonged survival. Animal Model: CD1 mice Dosage: 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 C max of 7 μmol/L.

Form:Solid

Specifications

Specifications & Purity

≥98%

Biochemical and Physiological Mechanisms

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.

Storage

Store at -20°C

Shipped In

Ice chest + Ice pads

This product requires cold chain shipping. Ground and other economy services are not available.

Action Type

INHIBITOR

Purity

≥98%

Names and Identifiers

• Molecular Weight: 932.95

Chemical and Physical Properties

• Solubility: DMSO : 100 mg/mL (107.19 mM; Need ultrasonic)