BRD5529
Based on 4 publication(s) in Google Scholar
BRD5529 is an effective dose-dependent CARD9-TRIM62 protein–protein interaction (PPI) inhibitor with an IC50 value of 8.6 μM. BRD5529 has potency and complete inhibition of CARD9 ubiquitinylation in vitro, also has favorable solubility. BRD5529 can be used for the research of inflammatory bowel disease (IBD) such as Crohn’s disease (CD) and ulcerative colitis (UC).
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 98.94%
- CAS. Nr.: 1358488-78-4
- Formel: C25H31N5O4
- Molecular Weight:465.54
-
Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
-
Biologische Aktivität
-
Chemical Information
-
Lösungsmittel & Löslichkeit
- Reinheit & Dokumentation
- Verweise
-
Help & FAQs
-
Immunology/Inflammation Compound Library
HY-L007
-
Metabolism/Protease Compound Library
HY-L012
-
Oxygen Sensing Compound Library
HY-L045
-
Ubiquitination Compound Library
HY-L050
-
Targeted Diversity Library
HY-L099
-
Anti-Liver Cancer Compound Library
HY-L101
-
Heterocyclic Compound Library
HY-L138
-
Metabolic Enzyme Compound Library
HY-L146
-
Mitophagy Compound Library
HY-L180
-
Bioactive Compound Library Max
HY-L181
-
MCE Bioactive Compound Library
HY-L001V
-
Bioactive Compound Library
HY-L001
-
Amino Acid Metabolism Compound Library
HY-L189
-
Cell Proliferation Compound Library
HY-L201
-
High-Throughput Bioactive Compound Library
HY-L205
-
Posttranslational Modification Library
HY-L226
Publications Citing Use of MedChemExpress (MCE) BRD5529
More
Biologische Aktivität
IC50: 8.6 μM (CARD9-TRIM62)[1]
BRD5529 has effective dose-dependent CARD9-TRIM62 inhibitory activity with an IC50 value of 8.6 μM[1].
BRD5529 directly binds CARD9, but not TRIM62, and disrupt its ubiquitinylation in vitro[1].
BRD5529 (40 μM) produces dose-dependent inhibition of TRIM62-mediated CARD9 ubiquitinylation in vitro[1].
BRD5529 (200 μM, 0-50 min; 200μM, 2-4 h) inhibits CARD9-dependent signaling in innate immune cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Cell Line:HEK293F cells
-
Concentration:40 μM
-
Incubation Time:
-
Result:Inhibited CARD9 ubiquitinylation reaction in vitro.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:Pneumocystis pneumonia (PCP) model[2]
-
Dosage:0.1 or 1.0 mg/kg
-
Administration:intraperitoneally (IP), daily, for 2 weeks
-
Result:Resulted no significant changes in daily or final weight gain and proinflammatory cytokines showed no major differences.
Showed no significant change of lung, liver, and kidney in pathology scoring.
Chemical Information
-
CAS. Nr. 1358488-78-4
-
Appearance Solid
-
Molecular Weight 465.54
-
Formel C25H31N5O4
-
Color Light yellow to yellow
-
SMILES
O=C(C1=CC(NC(C2=CC=C(C)C=C2)=O)=CN=C1N3CCC(N4CCCCC4)(C(N)=O)CC3)O
-
Versand
Room temperature in continental US; may vary elsewhere.
-
Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (4)
-
Journal Impact Factor
-
Most Recent
-
Immunity
Microbiota translocation following intestinal barrier disruption promotes Mincle-mediated training of myeloid progenitors in the bone marrow. [Abstract]2025 Feb 11;58(2):381-396.e9. PMID: 39848243 -
JCI Insight
2026 Mar 10:e190690. PMID: 41805789 -
Int J Biochem Cell Biol
MIEN1 on the 17q12 amplicon facilitates the malignant behaviors of gastric cancer via activating IL-6/JAK2/STAT3 pathway. [Abstract]2024 Nov:176:106666. PMID: 39343060 -
bioRxiv
MALT1 protease inhibition restrains glioblastoma progression by reversing tumor-associated macrophage-dependent immunosuppression. [Abstract]2024 Sep 27:2024.09.26.614808. PMID: 39386586
Lösungsmittel & Löslichkeit
DMSO : 125 mg/mL (268.51 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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: ≥ 2.08 mg/mL (4.47 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (4.47 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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: 0.5% CMC-Na/saline water
Solubility: 20 mg/mL (42.96 mM); Suspended solution; Need ultrasonic
Please enter the basic information of animal experiments:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
-
%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
-
%+
-
+%Tween-80 + +
-
%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.
Reinheit & Dokumentation
-
Data Sheet (278 KB)
-
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)
- Portuguese - PT (393 KB)
-
Handling Instructions (2659 KB)
Verweise
[1]. Leshchiner ES, et al. Small-molecule inhibitors directly target CARD9 and mimic its protective variant in inflammatorybowel disease. Proc Natl Acad Sci U S A. 2017 Oct 24;114(43):11392-11397. [Content Brief]
[2]. Theodore J Kottom, et al. Preclinical and Toxicology Studies of BRD5529, a Selective Inhibitor of CARD9. Drugs R D. 2022 Jun;22(2):165-173. [Content Brief]
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.1480 mL | 10.7402 mL | 21.4804 mL | 53.7011 mL |
| 5 mM | 0.4296 mL | 2.1480 mL | 4.2961 mL | 10.7402 mL | |
| 10 mM | 0.2148 mL | 1.0740 mL | 2.1480 mL | 5.3701 mL | |
| 15 mM | 0.1432 mL | 0.7160 mL | 1.4320 mL | 3.5801 mL | |
| 20 mM | 0.1074 mL | 0.5370 mL | 1.0740 mL | 2.6851 mL | |
| 25 mM | 0.0859 mL | 0.4296 mL | 0.8592 mL | 2.1480 mL | |
| 30 mM | 0.0716 mL | 0.3580 mL | 0.7160 mL | 1.7900 mL | |
| 40 mM | 0.0537 mL | 0.2685 mL | 0.5370 mL | 1.3425 mL | |
| 50 mM | 0.0430 mL | 0.2148 mL | 0.4296 mL | 1.0740 mL | |
| 60 mM | 0.0358 mL | 0.1790 mL | 0.3580 mL | 0.8950 mL | |
| 80 mM | 0.0269 mL | 0.1343 mL | 0.2685 mL | 0.6713 mL | |
| 100 mM | 0.0215 mL | 0.1074 mL | 0.2148 mL | 0.5370 mL |
Powered by Bioz