Stauprimide
Modify Date: 2024-01-10 16:38:57
Stauprimide structure
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Common Name | Stauprimide | ||
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| CAS Number | 154589-96-5 | Molecular Weight | 584.621 | |
| Density | 1.5±0.1 g/cm3 | Boiling Point | N/A | |
| Molecular Formula | C35H28N4O5 | Melting Point | 145°C | |
| MSDS | Chinese USA | Flash Point | N/A | |
Use of StauprimideStauprimide is a staurosporine analog that promotes embryonic stem cell (ESC) differentiation. Stauprimide is a non-broad spectrum inhibitor that binds to the MYC transcription factor NME2 and blocks its nuclear localization in ESCs, which results in down-regulation of MYC transcription[1]. |
| Name | Stauprimide |
|---|---|
| Synonym | More Synonyms |
| Description | Stauprimide is a staurosporine analog that promotes embryonic stem cell (ESC) differentiation. Stauprimide is a non-broad spectrum inhibitor that binds to the MYC transcription factor NME2 and blocks its nuclear localization in ESCs, which results in down-regulation of MYC transcription[1]. |
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| Related Catalog | |
| In Vitro | Stauprimide (10 μM; 6 hours) suppresses MYC transcription in the majority of cell lines tested with an EC50 range of 30 nM-8 μM, and decreases MYC levels between 15% to over 90%[1]. Stauprimide (2-8 μM; 24-72 hours) down-regulates MYC leads to the inhibition of cell proliferation in vitro with an IC50 of 780 nM in RXF 393 cells[1]. Stauprimide (5 μM; 3 hours) suppresses MYC Transcription by decreasing NME2 Nuclear Translocation[1]. Stauprimide (4-10 μM; 6 hours) acts with different EC50s and with different degrees of maximal MYC mRNA down-regulation in different cell lines[1]. Cell Proliferation Assay[1] Cell Line: Renal cancer cell line RXF 393 cells Concentration: 2 μM, 4 μM, 8 μM Incubation Time: 24 hours, 48 hours, 72 hours Result: Inhibited cell proliferation at concentrations of 2-8 μM. Western Blot Analysis[1] Cell Line: Renal cancer cell line RXF 393 cells and CAKI-1 cells Concentration: 5 μM Incubation Time: 3 hours Result: Decreased nuclear localized NME2. RT-PCR[1] Cell Line: CA46 cells; Ramos cells; RXF393 cells; TK10 cells; KG1A cells; CAKI-1 cells Concentration: 4μM, 6μM, 8μM, 10μM Incubation Time: 6 hours Result: Suppressed MYC transcription in KG1A cells with an EC50 of 400±50 nM and a suppression of 90%; CA46 cells were resistant to stauprimide. |
| In Vivo | Stauprimide (oral administration; 50 mg/kg; once daily; 30 days, 55 days) blocks tumor growth, reduces MYC protein levels in xenograft mouse with RXF 393 or CAKI-1 cells and inhibits MYC transcription in the RXF 393 tumor[1]. Animal Model: Xenograft tumor models with RXF 393 and CAKI-1 cells in NOD/SCID mice[1] Dosage: 50 mg/kg Administration: Oral administration; 50 mg/kg; once daily; 30 days, 55 days Result: Blocked tumor growth in mice injected with either RXF 393 or CAKI-1 cells during the dosing periods. |
| References |
| Density | 1.5±0.1 g/cm3 |
|---|---|
| Melting Point | 145°C |
| Molecular Formula | C35H28N4O5 |
| Molecular Weight | 584.621 |
| Exact Mass | 584.205994 |
| PSA | 98.56000 |
| LogP | 6.13 |
| Index of Refraction | 1.783 |
| Storage condition | -20°C |
| RIDADR | NONH for all modes of transport |
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A small molecule primes embryonic stem cells for differentiation.
Cell Stem Cell 5 , 416-426, (2009) Embryonic stem cells (ESCs) are an attractive source of cells for disease modeling in vitro and may eventually provide access to cells/tissues for the treatment of many degenerative diseases. However,... |
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Using small molecules to great effect in stem cell differentiation.
Cell Stem Cell 5 , 373-374, (2009) Several recent reports, including two Cell Stem Cell papers (Zhu et al., 2009 [this issue]; Borowiak et al., 2009), screened small molecule libraries for compounds that promote embryonic stem cell dif... |
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