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NU-2058
CAS No. 161058-83-9
NU-2058( O6-cyclohexylmethyl guanine | NU2058 | NU 2058 )
Catalog No. M12326 CAS No. 161058-83-9
An ATP-competitive inhibitor of CDK1 and CDK2 with Ki of 5 uM and 12 uM respectively; inhibits human tumor cells with a mean GI50 of 13±7 uM.
Purity : >98% (HPLC)
COA
Datasheet
HNMR
HPLC
MSDS
Handing Instructions
| Size | Price / USD | Stock | Quantity |
| 1 mL x 10 mM in DMSO | 37 | In Stock |
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| 10MG | 33 | In Stock |
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| 25MG | 67 | In Stock |
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| 50MG | 100 | In Stock |
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| 100MG | 152 | In Stock |
|
| 200MG | 226 | In Stock |
|
| 500MG | 369 | In Stock |
|
| 1G | Get Quote | In Stock |
|
Biological Information
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Product NameNU-2058
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NoteResearch use only, not for human use.
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Brief DescriptionAn ATP-competitive inhibitor of CDK1 and CDK2 with Ki of 5 uM and 12 uM respectively; inhibits human tumor cells with a mean GI50 of 13±7 uM.
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DescriptionAn ATP-competitive inhibitor of CDK1 and CDK2 with Ki of 5 uM and 12 uM respectively; inhibits human tumor cells with a mean GI50 of 13±7 uM; reduces CDK2-mediated phosphorylation of pRb, E2F transcriptional activity and proliferatio in both anti-estrogen-sensitive and resistant cells; also inhibits DNA topoisomerase II ATPase activity (IC50=300 uM).
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In VitroNU2058 (O6-(Cyclohexylmethyl)guanine) is a competitive inhibitor of CDK2 with respect to ATP (Ki value CDK2, 12 μM) that binds in the ATP binding pocket in a different orientation from other purine-based inhibitors, including olomoucine and roscovotine. NU2058 is the lead compound in a structure-based drug discovery program to develop more potent and selective CDK inhibitors.
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In Vivo——
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SynonymsO6-cyclohexylmethyl guanine | NU2058 | NU 2058
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PathwayAngiogenesis
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TargetCDK
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RecptorCDK1|CDK2|TopoII
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Research AreaCancer
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Indication——
Chemical Information
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CAS Number161058-83-9
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Formula Weight247.2963
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Molecular FormulaC12H17N5O
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Purity>98% (HPLC)
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SolubilityDMSO: ≥ 32 mg/mL
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SMILESNC1=NC(OCC2CCCCC2)=C3N=CNC3=N1
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Chemical Name9H-Purin-2-amine, 6-(cyclohexylmethoxy)-
Shipping & Storage Information
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Storage(-20℃)
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ShippingWith Ice Pack
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Stability≥ 2 years
Reference
1. Arris CE, et al. J Med Chem. 2000 Jul 27;43(15):2797-804.
2. Johnson N, et al. Br J Cancer. 2010 Jan 19;102(2):342-50.
3. Harrison LR, et al. Biochem Pharmacol. 2009 May 15;77(10):1586-92.
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