| Size | Price | Stock | Qty |
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| 50mg |
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| 100mg |
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| Other Sizes |
Purity: ≥98%
| Targets |
p38α MAPK (IC50 = 3.2 nM); p38β MAPK (IC50 = 122 nM)
SD169 targets p38α mitogen-activated protein kinase (MAPK), a key signaling molecule involved in the regulation of inflammatory responses, cell differentiation, and apoptosis. By acting as an ATP-competitive inhibitor, SD169 binds to the ATP-binding pocket of p38α, preventing its phosphorylation and activation. The compound exhibits an IC50 of 3.2 nM for p38α and shows weak inhibition of p38β (IC50 = 122 nM). SD169 is highly selective and does not inhibit p38γ, ERK2, JNK-1, or MAPKAPK-2. |
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| ln Vitro |
SD-169 significantly lowers the expression of p38 and HSP60 in pancreatic beta islet T cells[1].
SD-169 demonstrates 38-fold more potency against p38α MAP kinase (IC50=3.2 nM) than p38β MAP kinase (IC50=122 nM)[1]. In vitro, SD169 acts as a selective inhibitor of p38α MAPK with an IC50 of 3.2 nM. It weakly inhibits p38β with an IC50 of 122 nM and has no inhibitory effect against p38γ, ERK2, JNK-1, or MAPKAPK-2. The compound's high selectivity for p38α over other kinases makes it a valuable tool for studying the role of p38α in inflammatory and autoimmune diseases. In T cells, SD169 reduces p38 and HSP60 expression. |
| ln Vivo |
In vivo, SD169 prevents the development and progression of diabetes in nonobese diabetic (NOD) mice by inhibiting T cell infiltration and activation. The compound decreases p38 MAP kinase expression in T cells, lowers blood glucose, and reduces the risk of diabetes. These in vivo studies demonstrate the compound's potential as a therapeutic agent for autoimmune diseases, particularly type 1 diabetes.
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| Enzyme Assay |
The in vitro enzyme/receptor binding (non-cellular) assays for SD169 are kinase activity assays using purified recombinant p38α, p38β, p38γ, ERK2, JNK-1, and MAPKAPK-2. The compound's ability to inhibit the phosphorylation of a peptide substrate by these kinases in the presence of ATP is measured. The IC50 for inhibition of p38α is determined from the dose-response curve. These assays confirm the compound's selective inhibition of p38α MAPK.
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| Cell Assay |
In vitro cellular assays for SD169 are performed using immune cells, such as T cells, or other cell types. Cells are treated with SD169 and stimulated with inflammatory agents or other activators of the p38 MAPK pathway. The phosphorylation of p38 and its downstream substrates is assessed by Western blotting. Cytokine production is measured by ELISA. Cell viability is evaluated using MTT assays. These assays confirm the compound's ability to inhibit p38α MAPK signaling in cells.
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| Animal Protocol |
In vivo animal experiments for SD169 are conducted in nonobese diabetic (NOD) mice, a model of type 1 diabetes. Mice are administered SD169 orally, and the development of diabetes is monitored by measuring blood glucose levels. T cell infiltration into the pancreatic islets is assessed by histopathology. The expression of p38 and HSP60 in T cells is measured by Western blotting or immunohistochemistry. These studies demonstrate the compound's efficacy in preventing autoimmune diabetes.
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| ADME/Pharmacokinetics |
SD169 has a molecular weight of 160.17 g/mol and a molecular formula of C9H8N2O. The compound is orally active. Detailed pharmacokinetic parameters such as half-life, Cmax, and bioavailability have not been extensively reported in the available literature. However, the compound's in vivo efficacy in NOD mice suggests adequate systemic exposure following oral administration. SD169 is soluble in DMSO and other organic solvents.
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| Toxicity/Toxicokinetics |
SD169 has been evaluated in preclinical studies and has been reported to be well-tolerated at effective doses. No significant toxicity has been reported in the available literature. However, comprehensive toxicology studies would be necessary to fully assess the compound's safety profile for clinical development. As a selective p38α inhibitor, SD169 may have a favorable safety profile with reduced risk of off-target effects.
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| References | |
| Additional Infomation |
1H-indole-5-carboxamide is an indolecarboxamide.
SD169 is a selective, orally active, ATP-competitive inhibitor of p38α MAPK with an IC50 of 3.2 nM. It weakly inhibits p38β and has no effect on p38γ, ERK2, JNK-1, or MAPKAPK-2. SD169 prevents the development and progression of diabetes in NOD mice by inhibiting T cell infiltration and activation. The compound reduces p38 expression in T cells and lowers blood glucose. SD169 is a research compound with potential applications in autoimmune diseases, particularly type 1 diabetes. |
| Molecular Formula |
C9H8N2O
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|---|---|
| Molecular Weight |
160.17
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| Exact Mass |
160.063
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| Elemental Analysis |
C, 67.49; H, 5.03; N, 17.49; O, 9.99
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| CAS # |
1670-87-7
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| Related CAS # |
1670-87-7
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| PubChem CID |
14973220
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| Appearance |
White to yellow solid powder
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| Density |
1.3±0.1 g/cm3
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| Boiling Point |
457.6±18.0 °C at 760 mmHg
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| Melting Point |
159-163ºC
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| Flash Point |
230.6±21.2 °C
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| Vapour Pressure |
0.0±1.1 mmHg at 25°C
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| Index of Refraction |
1.717
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| LogP |
0.88
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
1
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| Rotatable Bond Count |
1
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| Heavy Atom Count |
12
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| Complexity |
193
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1=C(C=C2C=CNC2=C1)C(=O)N
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| InChi Key |
GQMYQEAXTITUAE-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C9H8N2O/c10-9(12)7-1-2-8-6(5-7)3-4-11-8/h1-5,11H,(H2,10,12)
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| Chemical Name |
1H-indole-5-carboxamide
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| Synonyms |
SD-169; SD 169; SD169
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| HS Tariff Code |
2934.99.03.00
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: 32~100 mg/mL (199.8~624.3 mM)
Ethanol: ~32 mg/mL (~199.8 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (12.99 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (12.99 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (12.99 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 6.2434 mL | 31.2168 mL | 62.4337 mL | |
| 5 mM | 1.2487 mL | 6.2434 mL | 12.4867 mL | |
| 10 mM | 0.6243 mL | 3.1217 mL | 6.2434 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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