SNIPER(BRD)-1
Based on 1 Customer Validation
SNIPER (BRD)-1 is a BRD2/3/4 SNIPER degrader. SNIPER (BRD)-1 induces ubiquitin-proteasome-dependent degradation of the epigenetic regulatory proteins BRD2/3/4 as well as the IAP family E3 ligase itself with its IC50 values for cIAP1, cIAP2 and XIAP of 6.8 nM, 17 nM and 49 nM, respectively. SNIPER (BRD)-1 can be used in the research of prostate cancer.
(Pink: BRD4 ligand (HY-13030); Blue: IAP ligand (HY-15518); Black: linker (HY-W008005)).
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: 99.68%
- CAS 番号: 2095244-54-3
- 分子式: C53H66ClN9O8S2
- 分子量:1056.73
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保管条件:
-20°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
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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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
|
BRD2 |
BRD3 |
BRD4 |
cIAP1 6.9 nM (IC50) |
cIAP2 17 nM (IC50) |
XIAP 49 nM (IC50) |
SNIPER (BRD)-1 (0-3 μM; 6-24 h) induces proteasomal degradation of BRD4, BRD2, BRD3, cIAP1, and XIAP in LNCaP cells, with preferential utilization of XIAP as the E3 ligase for BRD4 degradation; a hook effect is observed for BRD4 and BRD2 but not for BRD3, cIAP1, or XIAP[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:human prostate carcinoma LNCaP cells
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Concentration:0, 0.01, 0.03, 1 and 3 μM
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Incubation Time:6 and 24 h
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Result:Reduced BRD4/actin ratio to 28% at 0.1 μM for 6 h, and to 27% at 0.1 μM for 24 h.
Reduced cIAP1/actin ratio to 15% at 0.1 μM for 6 h, and to 15% at 0.1 μM for 24 h.
Reduced XIAP/actin ratio to 10% at 0.1 μM for 6 h, and to 8% at 0.1 μM for 24 h.
Reduced BRD2/actin ratio to 42% at 0.1 μM for 6 h, and BRD3/actin ratio to 57% at 0.1 μM for 6 h.
Induced a pharmacological hook effect for BRD4 and BRD2, but not for BRD3, cIAP1, or XIAP.
化学情報
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CAS 番号 2095244-54-3
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性状 Solid
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分子量 1056.73
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分子式 C53H66ClN9O8S2
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Color Off-white to light yellow
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SMILES
O=C(C[C@H]1C2=NN=C(C)N2C(SC(C)=C3C)=C3C(C4=CC=C(Cl)C=C4)=N1)NCCOCCOCCOCCOC5=CC(C(C6=CSC([C@H]7N(C([C@@H](NC([C@H](C)NC)=O)C8CCCCC8)=O)CCC7)=N6)=O)=CC=C5
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
-20°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
溶剤 & 溶解度
DMSO : 66.67 mg/mL (63.09 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 (stored under nitrogen). 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 (stored under nitrogen). 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)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (2.37 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
純度とドキュメンテーション
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データシート (271 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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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 (stored under nitrogen). 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 | 0.9463 mL | 4.7316 mL | 9.4632 mL | 23.6579 mL |
| 5 mM | 0.1893 mL | 0.9463 mL | 1.8926 mL | 4.7316 mL | |
| 10 mM | 0.0946 mL | 0.4732 mL | 0.9463 mL | 2.3658 mL | |
| 15 mM | 0.0631 mL | 0.3154 mL | 0.6309 mL | 1.5772 mL | |
| 20 mM | 0.0473 mL | 0.2366 mL | 0.4732 mL | 1.1829 mL | |
| 25 mM | 0.0379 mL | 0.1893 mL | 0.3785 mL | 0.9463 mL | |
| 30 mM | 0.0315 mL | 0.1577 mL | 0.3154 mL | 0.7886 mL | |
| 40 mM | 0.0237 mL | 0.1183 mL | 0.2366 mL | 0.5914 mL | |
| 50 mM | 0.0189 mL | 0.0946 mL | 0.1893 mL | 0.4732 mL | |
| 60 mM | 0.0158 mL | 0.0789 mL | 0.1577 mL | 0.3943 mL |
SNIPER(BRD)-1 関連分類
HY-111875 関連分類
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