Small Molecules / NSA, Spautin-1 & SU5402
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Small Molecules / NSA, Spautin-1 & SU5402
Product Name: Necrosulfonamide (NSA)
Necrosulfonamide (NSA) is a very specific and potent necrosis inhibitor with an IC50 less than 0.2 µM. It specifically blocks necrosis downstream of receptor-interacting serine-threonine kinase 3 (RIP3) activation. RIP3 is a key signaling molecule in the programmed necrosis pathway. Treating cells with NSA arrested necrosis at a specific step at which RIP3 formed
discrete punctae in cells. Different from Necrostatin-1, NSA does not inhibit the necrosis-induced RIP1 and RIP3
interactions. NSA targets MLKL, a critical substrate of RIP3 during induction of necrosis. It binds the N-terminal of MLKL,
covalently modifies Cys86 of human MLKL, and prevents necrosome from interacting with its downstream effectors.
Reference
- Sun L., et al. Mixed Lineage Kinase Domain-like Protein Mediates Necrosis Signaling Downstream of RIP3 Kinase. Cell (2012), 148(1):213-227.
- Wang Z., et al. The mitochondrial phosphatase PGAM5 functions at the convergence point of multiple necrotic death pathways. Cell (2012), 148(1):228-243
Ordering information ;
1. C6327-2 (powder)
2. C6327-2s (10 mM in DMSO)
2. C6327-2s (10 mM in DMSO)
* Packing size: 2 mg
Product Name: Spautin-1
Spautin-1 is a specific and potent autophagy inhibitor (IC50=0.74µM). It promotes the degradation of Vps34 PI3 kinase
complexes by inhibiting two ubiquitin specific peptidases, USP10 and USP13, that target the Beclin1 subunit of Vps34
complexes. Since USP10 mediates the deubiquitination of p53, regulating deubiquitination activity of USP10 and USP13
by Beclin1 provides a mechanism for Beclin1 to control the levels of p53. By this mechanism, Spautin-1 increased cancer
cell death in the setting of nutrient deprivation when autophagy would normally act as a survival mechanism in these
metabolically stressed cells.
Reference
- Junli Liu, et al. Beclin1 Controls the Levels of p53 by Regulating the Deubiquitination Activity of USP10 and USP13. Cell (2011), 147(1), 223-234.
- Joseph D. Mancias, et al. Targeting Autophagy Addiction in Cancer. Oncotarget (2011). In press.
Ordering information ;
1. C3430-2s (10 mM in DMSO)
2. C3430-2 (powder)
* Packing size: 2 mg
Product Name: SU5402
SU5402 is a fibroblast growth factor receptor (FGFR)-specific tyrosine kinase inhibitor with IC50 of 0.03µM. Studies show
that it inhibits embryonic left-right determination and exhibits potent anticancer activity in vitro and in vivo. Combination
treatment of SU5402 (2µM) with CHIR99021 (3µM) and PD0325901 (0.4µM) is highly effective for maintaining
pluripotency of ESCs.
Reference
- Sun L., et al. Design, synthesis, and evaluations of substituted 3-[(3- or 4-carboxyethylpyrrol-2-yl)methylidenyl]indolin-2-ones as inhibitors of VEGF, FGF, and PDGF receptor tyrosine kinases. J Med Chem. 1999;42(25):5120-30
- Tanaka Y., et al. FGF-induced vesicular release of Sonic hedgehog and retinoic acid in leftward nodal flow is critical for left-right determination. Nature. 2005;435(7039):172-7
- Qi-Long Ying, et al. The ground state of embryonic stem cell self-renewal. Nature 2008; 453, 519–523
Ordering information ;
1. C7854-1s (10 mM in DMSO)
2. C7854-1 (powder)
* Packing size: 1 mg
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