LP99
Based on 1 Customer Validation
LP99, an epigenetic probe, is a potent and selective inhibitor of the BRD7 and BRD9 bromodomains with a Kd of 99 nM against BRD9. LP99 disrupts the binding of BRD7 and BRD9 to chromatin in cells.
연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.
- Purity: 99.18%
- CAS No.: 1808951-93-0
- 화학식: C26H30ClN3O4S
- 분자량:516.05
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보관: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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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
Biological Activity
제품 설명
IC50 & Target
Kd: 99 nM (BRD9)[1]
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
5.1 μM
Compound: LP99
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Inhibition of human BRD9 isoform 1 co-expressed with H3 histone family 3A in HEK293 cells preincubated for 18 hrs followed by addition of nano-BRET furimazine as substrate measured within 5 mins by nanoBRET assay
Inhibition of human BRD9 isoform 1 co-expressed with H3 histone family 3A in HEK293 cells preincubated for 18 hrs followed by addition of nano-BRET furimazine as substrate measured within 5 mins by nanoBRET assay
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[PMID: 26914985] |
| HEK293 | IC50 |
6.2 μM
Compound: LP99
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Inhibition of human BRD9 isoform 1 co-expressed with H4 histone in HEK293 cells preincubated for 18 hrs followed by addition of nano-BRET furimazine as substrate measured within 5 mins by nanoBRET assay
Inhibition of human BRD9 isoform 1 co-expressed with H4 histone in HEK293 cells preincubated for 18 hrs followed by addition of nano-BRET furimazine as substrate measured within 5 mins by nanoBRET assay
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[PMID: 26914985] |
| HL-60 | GI50 |
5.028 μM
Compound: Chemical probe: LP99
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Antiproliferative activity against human HL-60 cells assessed as inhibition of cell growth for 7 days by cell titre glo assay
Antiproliferative activity against human HL-60 cells assessed as inhibition of cell growth for 7 days by cell titre glo assay
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[PMID: 27376689] |
| HL-60 | GI50 |
5.03 μM
Compound: 18; LP99
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Growth inhibition of human HL60 cells after 72 hrs by CellTiter 96S AQeous non-radioactive cell proliferation assay
Growth inhibition of human HL60 cells after 72 hrs by CellTiter 96S AQeous non-radioactive cell proliferation assay
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[PMID: 33275431] |
| Jurkat | GI50 |
10.51 μM
Compound: Chemical probe: LP99
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Antiproliferative activity against human Jurkat cells assessed as inhibition of cell growth for 7 days by cell titre glo assay
Antiproliferative activity against human Jurkat cells assessed as inhibition of cell growth for 7 days by cell titre glo assay
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[PMID: 27376689] |
| THP-1 | IC50 |
<10 μM
Compound: LP99
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Inhibition of LPS-stimulated IL-6 secretion in human THP1 cells by ELISA
Inhibition of LPS-stimulated IL-6 secretion in human THP1 cells by ELISA
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[PMID: 29170712] |
In Vitro
LP99 disrupts BRD9 interactions with chromatin at a concentration of 0.8 μM. BRD7- and BRD9-NanoLuc luciferase fusion proteins and fluorescently labelled histone H3.3- and H4-HaloTag fusions were expressed in HEK293 cells. The addition of LP99 decreased BRET for both BRD7 and BRD9 in both the H3.3 and H4 systems in a dose-dependent manner, with cellular IC50 values in the low micromolar range for both histone. Cytotoxicity tests in U2OS cells for 24 and 72 hours shows the inhibitor to be non-toxic at concentrations of <33 μM. LP99 inhibits IL-6 secretion from THP-1 cells in a dose-dependent manner[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1808951-93-0
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Appearance Solid
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분자량 516.05
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화학식 C26H30ClN3O4S
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Color White to light yellow
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SMILES
O=C1N(C2=CC(N(C)C(C=C3C)=O)=C3C=C2)[C@H](C4=CC=C(Cl)C=C4)[C@@H](NS(CC(C)C)(=O)=O)CC1
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
용액&용해도
In Vitro:
DMSO : 50 mg/mL (96.89 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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
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 (4.84 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.
In Vivo Dissolution Calculator
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.
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.
순도&문서
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Data Sheet (276 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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Handling Instructions (2659 KB)
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 | 1.9378 mL | 9.6890 mL | 19.3780 mL | 48.4449 mL |
| 5 mM | 0.3876 mL | 1.9378 mL | 3.8756 mL | 9.6890 mL | |
| 10 mM | 0.1938 mL | 0.9689 mL | 1.9378 mL | 4.8445 mL | |
| 15 mM | 0.1292 mL | 0.6459 mL | 1.2919 mL | 3.2297 mL | |
| 20 mM | 0.0969 mL | 0.4844 mL | 0.9689 mL | 2.4222 mL | |
| 25 mM | 0.0775 mL | 0.3876 mL | 0.7751 mL | 1.9378 mL | |
| 30 mM | 0.0646 mL | 0.3230 mL | 0.6459 mL | 1.6148 mL | |
| 40 mM | 0.0484 mL | 0.2422 mL | 0.4844 mL | 1.2111 mL | |
| 50 mM | 0.0388 mL | 0.1938 mL | 0.3876 mL | 0.9689 mL | |
| 60 mM | 0.0323 mL | 0.1615 mL | 0.3230 mL | 0.8074 mL | |
| 80 mM | 0.0242 mL | 0.1211 mL | 0.2422 mL | 0.6056 mL |
LP99 Related Classifications
HY-19553 Related Classifications
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