SD169 is an indole-5-carboxamide, orally-available, ATP-competitive, a-selective p38 MAPK inhibitor that targets a wide variety of inflammatory cells, including neutrophils, monocytes, macrophages, B and CD4+ T cells, and endothelial cells. [1] Through interactions with Schwann cell and TNF activity, SD169 promotes axonal regeneration in peripheral nerves. [2]
SD169 has been shown to reduce myeloma-induced osteolytic bone lesions and restored bone mass by downregulating osteoclastogenesis and osteoblastogenesis in xenografted primary myeloma-SCID-hu or myeloma cell line-SCID mouse models. [3] SD169 was also shown downregulates pp38 in myeloma cells in vitro and in vivo.
In the diabetes therapeutic area, SD169 significantly reduces p38 and HSP60 expression in T cells of the pancreatic beta islets. In studies using hyperglycemic NOD mice, SD169 treatment lowered blood glucose and improved glucose homeostasis. [4]
Technical information:
Chemical Formula: | C9H8N2O | |
CAS #: | 1670-87-7 | |
Molecular Weight: | 160.17 | |
Purity: | >98% | |
Appearance: | White | |
Chemical Name: | 1H-indole-5-carboxamide | |
Solubility: | Up to 22 mM in DMSO | |
Synonyms: | SD-169, SD169 |
Shipping Condition: The product is shipped in a glass vial at ambient temperature.
Storage condition: For longer shelf life, store solid powder at 4oC desiccated, or store DMSO solution at -20oC.
Reference:
1. | Medicherla et al., p38 MAPK inhibition reduces diabetes-induced impairment of wound healing. Diabetes, Metab. Syndr. Obes. 2009, 2, 91-100. Pubmed ID: 21437122 |
2. | Myers et al., Inhibition of p38 MAP kinase activity enhances axonal regeneration. Exp. Neurol. 2003, 184, 606-614. Pubmed ID: 14769353 |
3. | Yang et al., Constitutive activation of p38 MAPK in tumor cells contributes to osteolytic bone lesions in multiple myeloma. Leukemia, 2012, 26, 2114-2123. Pubmed ID: 22425892 |
4. | Medicherla et al., J. Pharmacol. Exp. Ther. 2006, 318(1), 99-107. Pubmed ID: 14769353 |
Other Information:
Product Specification (pdf)
MSDS (pdf)
Certificate of Analysis is available upon request.