1. PROTAC Epigenetics Apoptosis Cell Cycle/DNA Damage
  2. PROTACs Histone Acetyltransferase Apoptosis Caspase PARP
  3. JQAD1

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.

For research use only. We do not sell to patients.

JQAD1 Chemical Structure

JQAD1 Chemical Structure

CAS No. : 2417097-18-6

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Based on 1 publication(s) in Google Scholar

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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[1].

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[1].
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[1].
JQAD1 (1 μM; 12-36 h) induces Kelly NB cell apoptosis[1].
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[1].
JQAD1 (0.5 and 1 μM; 24 h) disrupts MYCN expression[1].
JQAD1 (0.5 μM; 24 h) causes loss of H3K27ac at chromatin[1].
JQAD1 (1.2 nM-20 μM; 5 days) has broad CRBN-dependent antineoplastic activity across cancer cell lines[1].
JQAD1 induces EP300 degradation in a time-dependent manner as early as 16 hours[1].

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

Western Blot Analysis[1]

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[1]

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

JQAD1 (40 mg/kg; i.p.; daily, for 21 d) inhibits tumor growth in NSG mice with Kelly NB cell xenografts[1].

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

Animal Model: NSG mice with Kelly NB cell xenografts[1]
Dosage: 40 mg/kg
Administration: Intraperitoneal injection; daily, for 21 days
Result: Suppressed tumor growth and prolonged survival.
Animal Model: CD1 mice[1]
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 Cmax of 7 μmol/L.
Molecular Weight

932.95

Formula

C48H52F4N6O9

CAS No.
Appearance

Solid

Color

Light yellow to green yellow

SMILES

O=C(N1CC(N([C@@H](C)C(F)(F)F)CC(C=C2)=CC=C2F)=O)[C@](CCC3=C4)(OC1=O)C3=CC=C4NC(CCCCCCCCCCCNC5=CC=C(C6=O)C(C(N6C(CCC7=O)C(N7)=O)=O)=C5)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (107.19 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.0719 mL 5.3593 mL 10.7187 mL
5 mM 0.2144 mL 1.0719 mL 2.1437 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.0719 mL 5.3593 mL 10.7187 mL 26.7967 mL
5 mM 0.2144 mL 1.0719 mL 2.1437 mL 5.3593 mL
10 mM 0.1072 mL 0.5359 mL 1.0719 mL 2.6797 mL
15 mM 0.0715 mL 0.3573 mL 0.7146 mL 1.7864 mL
20 mM 0.0536 mL 0.2680 mL 0.5359 mL 1.3398 mL
25 mM 0.0429 mL 0.2144 mL 0.4287 mL 1.0719 mL
30 mM 0.0357 mL 0.1786 mL 0.3573 mL 0.8932 mL
40 mM 0.0268 mL 0.1340 mL 0.2680 mL 0.6699 mL
50 mM 0.0214 mL 0.1072 mL 0.2144 mL 0.5359 mL
60 mM 0.0179 mL 0.0893 mL 0.1786 mL 0.4466 mL
80 mM 0.0134 mL 0.0670 mL 0.1340 mL 0.3350 mL
100 mM 0.0107 mL 0.0536 mL 0.1072 mL 0.2680 mL
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  • 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.

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JQAD1
Cat. No.:
HY-145765
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