KRM-III
Based on 1 Customer Validation
KRM-III is an orally active TCR inhibitor and NFAT inhibitor with an IC50 of 5 μM against NFAT. KRM-III has no effect on the activation of nuclear factor-κB. KRM-III inhibits T cell proliferation induced by T cell antigen receptor stimulation. KRM-III abrogates anti-CD3 antibody-induced cell activation in vivo. KRM-III reduces paw pad swelling in delayed-type hypersensitivity induced by Bovine serum albumin (HY-D0842). KRM-III alleviates the severity of experimental autoimmune encephalomyelitis (EAE) in mice. KRM-III can be used in studies related to experimental autoimmune encephalomyelitis.
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- Pureza: 98.08%
- No. CAS: 79220-94-3
- Fòrmula: C15H12N2S
- Peso molecular:252.33
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Almacenamiento: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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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Immunology/Inflammation Compound Library
HY-L007
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NF-κB Signaling Compound Library
HY-L014
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Orally Active Compound Library
HY-L061
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Targeted Diversity Library
HY-L099
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Extracellular Vesicles (EVs) Compound Library
HY-L168
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Bioactive Compound Library Max
HY-L181
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MCE Bioactive Compound Library
HY-L001V
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Bioactive Compound Library
HY-L001
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High-Throughput Bioactive Compound Library
HY-L205
Actividad biológica
KRM-III (0.4-50 μM; 3 h) specifically inhibits NFAT activation induced by TCR and PMA/Ionomycin (HY-13434) (but does not inhibit NF-κB activation) in Jurkat T cells, with an IC50 of 5 μM[1].
KRM-III (0.16-100 μM; 3 h) inhibits TCR-induced proliferation of splenocytes from C57BL/6 mice, with an IC50 of 4 μM, and shows no non-specific cytotoxicity[1].
KRM-III (0.8-50 μM) inhibits the one-way mixed lymphocyte reaction with an IC50 of 5 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| Species | Dose | Route | Tmax | Cmax | T1/2 | AUCall | AUCinf |
|---|---|---|---|---|---|---|---|
| Mice[1] | 10 mg/kg | p.o. | 4.00 h | 0.23 μg/mL | 7.09 h | 1.54 μg·h/mL | 1.69 μg·h/mL |
KRM-III (10-90 mg/kg; p.o.; daily; 10 days) reduces footpad swelling in a murine delayed-type hypersensitivity model by 45.8% at a daily oral dose of 90 mg/kg[1].
KRM-III (20-100 mg/kg; p.o.; daily; up to 30 days) reduces clinical severity, inflammatory cell infiltration, and MOG-specific T-cell proliferation in a murine experimental autoimmune encephalomyelitis model, with significant efficacy at 90 and 100 mg/kg daily doses[1].
KRM-III (100 mg/kg; p.o.; daily; 20 days) significantly reduces clinical severity in established murine experimental autoimmune encephalomyelitis[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c (6- to 10-week-old female; intravenous inoculation of anti-CD3 antibody)[1]
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Dosage:10 mg/kg; 30 mg/kg; 90 mg/kg
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Administration:p.o.; single dose
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Result:Achieved an ED50 of 9.9 mg/kg for inhibition of anti-CD3-induced IL-2 production.
Suppressed IL-2 production by up to 98% (p < 0.01) compared to vehicle controls at 90 mg/kg.
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Animal Model:C57BL/6 (6- to 10-week-old female; intradermal immunization with methylated bovine serum albumin in complete Freund's adjuvant, followed by footpad challenge)[1]
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Dosage:10 mg/kg; 30 mg/kg; 90 mg/kg
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Administration:p.o.; daily; 10 days
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Result:Reduced footpad swelling by 45.8% (p < 0.01) compared to vehicle controls at 90 mg/kg/day.
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Animal Model:C57BL/6 (6- to 10-week-old female; subcutaneous immunization with MOG35-55 peptide in complete Freund's adjuvant, plus intraperitoneal pertussis toxin on day 0 and day 2; prophylactic treatment)[1]
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Dosage:20 mg/kg; 90 mg/kg; 100 mg/kg
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Administration:p.o.; daily; up to 30 days
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Result:Reduced mean maximal clinical score to 2.36 (p < 0.05 vs. vehicle) and resulted in 25% of mice with no disease, 37.5% with mild disease, and 37.5% with severe disease at 90 mg/kg/day.
Reduced mean maximal clinical score to 1.85 (p < 0.05 vs. vehicle), resulted in 12.5% of mice with no disease, 62.5% with mild disease, and 25% with severe disease, significantly reduced clinical score curves from day 11 (p < 0.01 vs. vehicle), and reduced inflammatory cell infiltration in lumbar spinal cord segments (p = 0.01 vs. vehicle) at 100 mg/kg/day.
Strongly reduced draining lymph node cell proliferation in response to MOG35-55 peptide (p < 0.01 vs. vehicle) at 100 mg/kg/day.
Did not produce a significant effect on proliferation or clinical severity at 20 mg/kg/day.
Chemical Information
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No. CAS 79220-94-3
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Appearance Solid
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Peso molecular 252.33
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Fòrmula C15H12N2S
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Color Off-white to light brown
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SMILES
S=C1NC(C2=CC=CC=C2)=CN1C3=CC=CC=C3
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
DMSO : 100 mg/mL (396.31 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)
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 (9.91 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (9.91 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
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.
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.
Pureza y Documentación
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Ficha de datos (281 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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Instrucciones de manejo (2659 KB)
Referencias
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 | 3.9631 mL | 19.8153 mL | 39.6306 mL | 99.0766 mL |
| 5 mM | 0.7926 mL | 3.9631 mL | 7.9261 mL | 19.8153 mL | |
| 10 mM | 0.3963 mL | 1.9815 mL | 3.9631 mL | 9.9077 mL | |
| 15 mM | 0.2642 mL | 1.3210 mL | 2.6420 mL | 6.6051 mL | |
| 20 mM | 0.1982 mL | 0.9908 mL | 1.9815 mL | 4.9538 mL | |
| 25 mM | 0.1585 mL | 0.7926 mL | 1.5852 mL | 3.9631 mL | |
| 30 mM | 0.1321 mL | 0.6605 mL | 1.3210 mL | 3.3026 mL | |
| 40 mM | 0.0991 mL | 0.4954 mL | 0.9908 mL | 2.4769 mL | |
| 50 mM | 0.0793 mL | 0.3963 mL | 0.7926 mL | 1.9815 mL | |
| 60 mM | 0.0661 mL | 0.3303 mL | 0.6605 mL | 1.6513 mL | |
| 80 mM | 0.0495 mL | 0.2477 mL | 0.4954 mL | 1.2385 mL | |
| 100 mM | 0.0396 mL | 0.1982 mL | 0.3963 mL | 0.9908 mL |
KRM-III Related Classifications
HY-136427 Related Classifications
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- KRM-III
- 79220-94-3
- Nuclear Factor of activated T Cells (NFAT)
- nuclear factor-κB
- murine experimental autoimmune encephalomyelitis
- T-cell antigen receptor
- myelin oligodendrocyte glycoprotein peptide
- Jurkat T cells
- mixed lymphocyte reactions
- T-cell proliferation
- delayed-type hypersensitivity
- C57BL/6 mouse splenocytes
- NFAT
- Inhibitor
- inhibitor
- inhibit