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)).
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 98.24%
- CAS 番号: 2417097-18-6
- 分子式: C48H52F4N6O9
- 分子量:932.95
-
保管条件: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]
-
生物活性
-
化学情報
-
溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
-
Help & FAQs
-
Apoptosis Compound Library
HY-L003
-
Cell Cycle/DNA Damage Compound Library
HY-L004
-
Epigenetics Compound Library
HY-L005
-
Histone Modification Research Compound Library
HY-L024
-
Anti-Cancer Compound Library
HY-L025
-
Anti-Aging Compound Library
HY-L034
-
Anti-Breast Cancer Compound Library
HY-L074
-
Anti-Pancreatic Cancer Compound Library
HY-L077
-
PROTAC Library
HY-L151
-
Highly Selective Inhibitors Library
HY-L158
-
Highly Selective Activators Library
HY-L159
-
Cell Death Library
HY-L162
-
Multi-Target Compound Library
HY-L176
-
Bioactive Compound Library Max
HY-L181
-
MCE Bioactive Compound Library
HY-L001V
-
Bioactive Compound Library
HY-L001
-
Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library
HY-L199
-
High-Throughput Bioactive Compound Library
HY-L205
-
Posttranslational Modification Library
HY-L226
MedChemExpress（MCE）の使用を引用している文献 JQAD1
MorePROTACs アイソフォーム固有の製品をすべて表示
MoreCaspase アイソフォーム固有の製品をすべて表示
More
生物活性
|
p300 |
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| RS4-11 | IC50 |
91 nM
Compound: JQAD1
|
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
|
[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.
-
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.
-
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.
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.
化学情報
-
CAS 番号 2417097-18-6
-
性状 Solid
-
分子量 932.95
-
分子式 C48H52F4N6O9
-
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
-
輸送条件
Room temperature in continental US; may vary elsewhere.
-
保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (2)
-
Journal Impact Factor
-
Most Recent
-
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
溶剤 & 溶解度
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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
-
データシート (275 KB)
-
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
-
取扱説明書 (2659 KB)
参考文献
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 関連分類
HY-145765 関連分類
Powered by Bioz