Small Molecules, best seller/ PD0325901,etc.
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Small Molecules, best seller/ PD0325901, Kartogenin, Necrostatin
Product Name: PD0325901
PD0325901 is the selective inhibitor of mitogen activated protein kinase kinase (MEK or MAPKK) with IC50 about 1nM against activated MEK1 and MEK2. Its potency, solubility and effectiveness are all much better than CI-1040. Anticancer activity of PD0325901 has been demonstrated for a broad spectrum of human tumor xenografts. When using with GSK-3beta inhibitor CHIR99021, PD0325901 could prevent cell differentiation and sustain ES cell self-renewal.
Details
- Chemical Formula : C16H14F3IN2O4
- CAS #: 391210-10-9
- Molecular Weight: 482.19
- Purity: >98%
- Formulation: Off white solid
- Storage: Store solid powder at 4oC desiccated; Store DMSO solution at -20oC.
Reference
- Barrett, S.D., et al. The discovery of the benzhydroxamate MEK inhibitors CI-1040 and PD 0325901. Bioorg. Med. Chem. Lett. (2008), 18: 6501-6504.
- Judith S. Sebolt-Leopold et al. The biological profile of PD 0325901: A second generation analog of CI-1040 with improved pharmaceutical potential . Proc Amer Assoc Cancer Res, Volume 45, 2004.
- Tongxiang Lin, et al. A chemial platform for improved induction of human iPSCs. Nature Methods 6, 805 - 808 (2009)
Ordering information ;
1. C7303-2s (10 mM in DMSO)
2. C7303-2 (powder)
* Packing size: 2 mg
Product Name: Kartogenin (KGN)
Kartogenin (KGN) is a potent and specific small molecule to promote chondrocyte differentiation and can be used in cartilage cell engineering and cartilage repair after disease or injury. Kartogenin was shown to promote robust chondrocyte differentiation from primary human mesenchymal stem cells/MSCs [EC50 = 100 nM]. In an in vitro model mimicking cytokine-induced damage during osteoarthritis (OA), 1-5 µM of Kartogenin treatment inhibited nitric oxide (NO) and glycosaminoglycans (GAG) release. Direct Intra-articular administration of Kartogenin promoted cartilage repair in collagenase and surgery induced OA models in mice, and alleviated OA-induced joint pain. Mechanism of action studies showed that Kartogenin interacts with filamin A (FLNA) and results in the release of transcription factor CBFβ to the nucleus to regulate chondrogenic gene expression.
Details
- Chemical Formula: C20H15NO3
- CAS #: 4727-31-5
- Molecular Weight: 317.34
- Purity: >99%
- Formulation: Off-white solid
- Storage: Store solid powder at 4oC desiccated; Store DMSO solution at -20oC.
Reference
- Johnson K. et. al. A Stem Cell-Based Approach to Cartilage Repair. Science (2012) April 5. [Epub ahead of print].
Ordering information ;
1. C5278-2s (10 mM in DMSO)
2. C5278-2 (powder)
* Packing size: 2 mg
Product Name: Necrostatin-1
Necrostatin-1 is a specific ATP-competitive allosteric inhibitor (EC50 = 180 nM) of death domain receptor-associated adaptor kinase (RIP1)1. It selectively blocks a specific programed cell death pathway, necroptosis, which leads to necrosis. While affecting this distinct cell death pathway, Necrostatin-1 does not present any perturbation of the Fas/TNFR triggered canonical apoptosis cascade. Necrostatin-1 inhibits the necrosis-induced RIP1 and RIP3 interactions in vitro2 and reduces ischemic brain injury in a mouse model of stroke3.
Detail
- Chemical Formula: C13H13N3OS
- CAS #: 4311-88-0
- Molecular Weight:259.33
- Purity: >98%
- Formulation: Light yellow solid
- Storage: Store solid powder at 4oC desiccated; Store DMSO solution at -20oC.
Reference
- Degterev A., et al. Identification of RIP1 kinase as a specific cellular target of necrostatins. Nat. Chem. Biol. (2008), 4:313-321
- Sun L., et al. Mixed Lineage Kinase Domain-like Protein Mediates Necrosis Signaling Downstream of RIP3 Kinase. Cell (2012), 148:213-227
- Degterev A., et al. Chemical inhibitor of nonapoptotic cell death with therapeutic potential for ischemic brain injury. Nat. Chem. Biol. (2005), 1:112-119
Ordering information ;
1. C6221-5s (10 mM in DMSO)
2. C6221-5 (powder)
* Packing size: 2 mg
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