JQAD1
Based on 2 publication(s) in Google Scholar
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.
(Pink: CBP/p300 ligand (HY-107455); Blue: Cereblon ligand (HY-W087383); Black: linker (HY-W105740)).
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 98.24%
- CAS. Nr.: 2417097-18-6
- Formel: C48H52F4N6O9
- Molecular Weight:932.95
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
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Help & FAQs
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Apoptosis Compound Library
HY-L003
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Cell Cycle/DNA Damage Compound Library
HY-L004
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HY-L024
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HY-L074
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Publications Citing Use of MedChemExpress (MCE) JQAD1
MoreAlle PROTACs Isoform-spezifische Produkte anzeigen
MoreAlle Caspase Isoform-spezifische Produkte anzeigen
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Biologische Aktivität
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p300 |
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Cell Line
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Type | Value | Description | References |
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| RS4-11 | IC50 |
91 nM
Compound: JQAD1
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Cytotoxicity against human RS4-11 cells assessed as inhibition of cell growth incubated for 4 days by cellTiter-Glo assay
Cytotoxicity against human RS4-11 cells assessed as inhibition of cell growth incubated for 4 days by cellTiter-Glo assay
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[PMID: 37276143] |
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.
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Cell Line:MYCN-amplified NB cells
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Concentration:0.1, 0.5, 1, 3, 5, and 10 µM
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Incubation Time:24 h
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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.
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Cell Line:Kelly NB cells
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Concentration:1 µM
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Incubation Time:12, 24, and 36 hours
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Result:Increased the expression of cleaved caspase-3 and cleaved PARP1 in a dose-dependent manner.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:NSG mice with Kelly NB cell xenografts[1]
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Dosage:40 mg/kg
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Administration:Intraperitoneal injection; daily, for 21 days
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Result:Suppressed tumor growth and prolonged survival.
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Animal Model:CD1 mice[1]
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Dosage:10 mg/kg
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Administration:Intraperitoneal injection (Pharmacokinetic Analysis)
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Result:Had a half-life of 13.3 (±3.37 SD) hours in murine serum, with a Cmax of 7 μmol/L.
Chemical Information
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CAS. Nr. 2417097-18-6
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Appearance Solid
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Molecular Weight 932.95
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Formel C48H52F4N6O9
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Color Light yellow to green yellow
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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
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (2)
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Journal Impact Factor
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Most Recent
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Cell Death Dis
PDHA1-acetylation signaling suppresses cuproptosis to attenuate anti-androgen effect in prostate cancer. [Abstract]2026 Feb 23;17(1):243. PMID: 41730841 -
Proc Natl Acad Sci U S A
A MOZ-TIF2 leukemia mouse model displays KAT6-dependent H3K23 propionylation and overexpression of a set of active developmental genes. [Abstract]2024 Jun 25;121(26):e2405905121. PMID: 38889153
Lösungsmittel & Löslichkeit
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)
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.
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.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Reinheit & Dokumentation
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Data Sheet (275 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
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Handling Instructions (2659 KB)
Verweise
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 |
JQAD1 Related Classifications
HY-145765 Related Classifications
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