DS96432529
Based on 1 Customer Validation
DS96432529 is an orally active CDK8 inhibitor with an IC50 of 33 nM. DS96432529 enhances ALPase activity, with an EC200 of 63 nM. DS96432529 inhibits TNF-α-induced activation of the RLR signaling pathway, activates mitophagy, accelerates mineralized nodule formation, and suppresses the proliferation of periodontal ligament stem cells. DS96432529 promotes bone formation, alleviates ligation-induced alveolar bone loss, and increases bone mineral density in ovariectomized animal models. DS96432529 can be used in studies related to periodontitis and osteoporosis.
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- Purity : 99.93%
- CAS No.: 2871872-79-4
- 화학식: C18H26N4O3S
- 분자량:378.49
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보관:
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
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
- Protocol
- 순도&문서
- References
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Help & FAQs
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Biological Activity
제품 설명
IC50 & Target
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CDK8 |
In Vitro
DS96432529 (0-4 μM; 1-5 days) inhibits the proliferation of human periodontal ligament stem cells (PDLSCs) at concentrations ≥ 31 nM over the incubation periods of 1, 3, and 5 days[1].
DS96432529 (125 nM-250 nM; 7-10 days) promotes osteogenic differentiation of human periodontal ligament stem cells (PDLSCs), enhances ALP activity, and facilitates the formation of mineralized nodules[1].
DS96432529 (125 nM-250 nM) alleviates TNF-α-induced inflammatory impairment of osteogenic differentiation in human periodontal ligament stem cells (PDLSCs) and restores ALP activity[1].
DS96432529 (125 nM-250 nM) protects human periodontal ligament stem cells (PDLSCs) against TNF-α-induced osteogenic differentiation impairment by inhibiting RIG-I[1].
DS96432529 (125 nM-500 nM; 24 h) does not induce significant apoptosis in human periodontal ligament stem cells (PDLSCs) at concentrations up to 250 nM following 24 h of incubation[1].
DS96432529 (125 nM-250 nM) activates mitophagy in human periodontal ligament stem cells (PDLSCs), upregulates the protein levels of PINK1, PARKIN and LC3B-II, and enhances mitochondria-lysosome colocalization[1].
DS96432529 (125 nM-250 nM) inhibits TNF-α-induced activation of the RIG-I-mediated RLR signaling pathway in human periodontal ligament stem cells (PDLSCs) and reduces RIG-I protein levels[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:human periodontal ligament stem cells (PDLSCs, passages 3-5)
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Concentration:125 nM and 500 nM
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Incubation Time:24 h
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Result:Did not induce significant apoptosis in PDLSCs at 125 nM and 250 nM.
Markedly increased the proportion of apoptotic cells at 500 nM.
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Cell Line:human periodontal ligament stem cells (PDLSCs, passages 3-5)
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Concentration:125 nM and 250 nM
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Incubation Time:7 days (ALP activity); 10 days (mineralized nodule formation)
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Result:Significantly enhanced ALP activity compared to untreated control cells.
Promoted mineralized nodule formation compared to untreated control cells.
Parmacokinetics
| Species | Dose | Route | Cmax | AUC0-t |
|---|---|---|---|---|
| Rat[2] | 3 mg/kg | p.o. | 0.804 μg/mL | 2.00 μg·h/mL |
In Vivo
DS96432529 (0.3-3 mg/kg; p.o.; q.d.; 14 weeks) acts as a bone anabolic agent in ovariectomized rats, enhancing both bone formation and resorption with net bone gain[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Sprague-Dawley (male, 11-13 weeks old, ligature-induced periodontal defect model)[1]
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Dosage:0.1 mg/kg
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Administration:local injection; twice weekly; 2 months
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Result:Alleviated ligature-induced alveolar bone loss.
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Animal Model:F344 rats[2]
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Dosage:0.3 mg/kg/day; 1 mg/kg/day; 3 mg/kg/day
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Administration:p.o.; q.d.; 14 weeks
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Result:Produced significant increases in areal bone mineral density in the humeral diaphysis and total humeri at doses from 1 mg/kg/day; recovered humeral diaphysis areal bone mineral density to nearly the level of sham-operated rats at 3 mg/kg/day.
Significantly improved bone strength measured via 3-point bending maximum load at doses from 1 mg/kg/day.
Caused a significant surge in serum osteocalcin (a bone formation biomarker) at 3 mg/kg/day.
Significantly increased urinary deoxypyridinoline (a bone resorption biomarker) compared to vehicle control at doses from 0.3 mg/kg/day.
Chemical Information
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CAS No. 2871872-79-4
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Appearance Solid
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분자량 378.49
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화학식 C18H26N4O3S
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Color Off-white to pink
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SMILES
O=C(C1=C(N)C2=C(N3C[C@@H](COCCOCC)CCC3)C=CN=C2S1)N
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선적
Room temperature in continental US; may vary elsewhere.
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보관
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
용액&용해도
In Vitro:
DMSO : 100 mg/mL (264.21 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 (sealed storage, away from moisture and light). 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 (sealed storage, away from moisture and light). 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 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (6.61 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 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.
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. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
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.
Protocol
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Mitophagy Solutions
Mitophagy is the selective autophagic degradation of mitochondria and functions as a mitochondrial quality-control pathway that removes damaged, depolarized, excess, or developmentally programmed mitochondria. The pathway links mitochondrial damage recognition, autophagosome recruitment, lysosomal delivery, and mitochondrial turnover to phenotypes such as mitochondrial homeostasis, oxidative-stress control, metabolic remodeling, differentiation, and neurodegeneration-related mitochondrial fidelity. The best-characterized damage-induced pathway is the PINK1-Parkin axis. Parkin is recruited selectively to impaired mitochondria and promotes their autophagic elimination, while mitochondrial depolarization stabilizes PINK1 on damaged mitochondria, recruits Parkin, and activates Parkin-dependent mitophagy. PINK1 also phosphorylates ubiquitin to activate Parkin E3 ubiquitin ligase activity, and PINK1-driven ubiquitin phosphorylation creates a feed-forward signal for recruiting autophagy machi
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Cell Viability Determination by MTT Colorimetric Assay
The following protocol uses the MTT colorimetric assay as a classic literature-established method for assessing cell viability/metabolic activity in cultured mammalian cells. MTT[3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] is reduced by metabolically active cells to a colored formazan product; the amount of formazan is quantified spectrophotometrically and provides an indirect measure of metabolically active viable cells. Importantly, MTT reduction reflects cellular oxidoreductase/metabolic activity rather than an absolute direct count of living cells, so changes in cellular metabolism can alter the signal independently of cell number.
순도&문서
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Data Sheet (289 KB)
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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)
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Handling Instructions (2659 KB)
References
[1]. He H, et al. DS96432529 enhances osteogenic differentiation and mitigates inflammatory damage in periodontal ligament stem cells involving mitophagy-related processes. Stem cell research & therapy. 2026 Mar 20;17(1):159. [Content Brief]
[2].
Saito K, et al. Discovery of 3-amino-4-{(3S)-3-[(2-ethoxyethoxy)methyl]piperidin-1-yl}thieno[2,3-b]pyridine-2-carboxamide (DS96432529): A potent and orally active bone anabolic agent. Bioorg Med Chem Lett. 2021 Dec 15;54:128440.
[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, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). 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 | 2.6421 mL | 13.2104 mL | 26.4208 mL | 66.0519 mL |
| 5 mM | 0.5284 mL | 2.6421 mL | 5.2842 mL | 13.2104 mL | |
| 10 mM | 0.2642 mL | 1.3210 mL | 2.6421 mL | 6.6052 mL | |
| 15 mM | 0.1761 mL | 0.8807 mL | 1.7614 mL | 4.4035 mL | |
| 20 mM | 0.1321 mL | 0.6605 mL | 1.3210 mL | 3.3026 mL | |
| 25 mM | 0.1057 mL | 0.5284 mL | 1.0568 mL | 2.6421 mL | |
| 30 mM | 0.0881 mL | 0.4403 mL | 0.8807 mL | 2.2017 mL | |
| 40 mM | 0.0661 mL | 0.3303 mL | 0.6605 mL | 1.6513 mL | |
| 50 mM | 0.0528 mL | 0.2642 mL | 0.5284 mL | 1.3210 mL | |
| 60 mM | 0.0440 mL | 0.2202 mL | 0.4403 mL | 1.1009 mL | |
| 80 mM | 0.0330 mL | 0.1651 mL | 0.3303 mL | 0.8256 mL | |
| 100 mM | 0.0264 mL | 0.1321 mL | 0.2642 mL | 0.6605 mL |
DS96432529 Related Classifications
HY-145121 Related Classifications
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Keywords
- DS96432529
- 2871872-79-4
- DS 96432529
- DS-96432529
- CDK
- Phosphatase
- Mitophagy
- RIG-I-like receptor (RLR)
- osteogenic differentiation
- mitophagy
- osteoporosis
- periodontitis
- RLR signaling pathway
- mouse bone marrow-derived ST2 cells
- RIG-I
- cyclin-dependent kinase 8
- periodontal ligament stem cell
- HEK293 cells
- Inhibitor
- inhibitor
- inhibit