532813 p21 Inhibitor, UC2288 - Calbiochem

532813
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Overview

Replacement Information

Key Specifications Table

Empirical Formula
C₂₀H₁₈ClF₆N₃O₂

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      Glass bottle 10 mg
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      Description
      OverviewA cell-permeable, orally available, phenylcyclohexyl-urea based compound that selectively downregulates the expression of p21 (~10 µM), independent of p53 expression, at either transcription or post-transcriptional level. However, it does not affect the stability of p21. Also, it has no significant effect on the activities of Raf kinases, VEGFR2 kinase, or the phosphorylation state of ERK. Effectively blocks the growth of multiple cancer cell lines (GI50 ~ 10 µM against NCI60 cell lines). Its greater inhibitory effect on cytosolic p21 is indicative of its ability to induce apoptotic cell death in 786-O cells. Synergistically suppresses the growth of HCT116 and ACHN cells in athymic nude mice when combined with imetelstat, a telomerase inhibitor (15 mg/kg of UC2288, p.o., & 30 mg/kg of imetelstat, i.p., 3 times per week).

      Please note that the molecular weight for this compound is batch-specific due to variable water content.
      Catalogue Number532813
      Brand Family Calbiochem®
      Synonyms1-(4-Chloro-3-(trifluoromethyl)phenyl)-3-((1r,4r)-4-(5-(trifluoromethyl)pyridin-2-yloxy)cyclohexyl)urea, trans-1-(4-Chloro-3-trifluoromethyl-phenyl)-3-(4-hydroxy-cyclohexyl)-urea, p21/Cip1/CKI/Waf1 Inhibitor, t-CTTU; UC-2288
      References
      ReferencesGupta, R., et al. 2014. Proc. Natl. Acad. Sci. USA 111, E3062.
      Wettersten, H.I., et al. 2013. Cancer Biol. Ther. 14, 278.
      Product Information
      FormWhite solid
      Hill FormulaC₂₀H₁₈ClF₆N₃O₂
      Chemical formulaC₂₀H₁₈ClF₆N₃O₂
      Quality LevelMQ100
      Applications
      Biological Information
      Purity≥98% by HPLC
      Physicochemical Information
      Cell permeableY
      Dimensions
      Materials Information
      Toxicological Information
      Safety Information according to GHS
      Safety Information
      Product Usage Statements
      Storage and Shipping Information
      Ship Code Ambient Temperature Only
      Toxicity Standard Handling
      Storage +2°C to +8°C
      Protect from Light Protect from light
      Do not freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Transport Information
      Supplemental Information
      Specifications

      Documentation

      p21 Inhibitor, UC2288 - Calbiochem SDS

      Title

      Safety Data Sheet (SDS) 

      p21 Inhibitor, UC2288 - Calbiochem Certificates of Analysis

      TitleLot Number
      532813

      References

      Reference overview
      Gupta, R., et al. 2014. Proc. Natl. Acad. Sci. USA 111, E3062.
      Wettersten, H.I., et al. 2013. Cancer Biol. Ther. 14, 278.

      Technical Info

      Title
      Characterization of Estrogen Receptor α Phosphorylation Sites in Breast Cancer Tissue Using the SNAP i.d® 2.0 System
      White Paper: Further considerations of antibody validation and usage. (EMD)
      Data Sheet

      Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

      Revision15-March-2015 JSW
      Synonyms1-(4-Chloro-3-(trifluoromethyl)phenyl)-3-((1r,4r)-4-(5-(trifluoromethyl)pyridin-2-yloxy)cyclohexyl)urea, trans-1-(4-Chloro-3-trifluoromethyl-phenyl)-3-(4-hydroxy-cyclohexyl)-urea, p21/Cip1/CKI/Waf1 Inhibitor, t-CTTU; UC-2288
      DescriptionA cell-permeable phenylcyclohexyl-urea compound that downregulates cellular p21/Cip1/CKI/Waf1 protein level (by > 95% in HCT116 cells after 24 h UC2288 treatment at 2.5 µM), presumably by means of a yet undetermined transcriptional or post-transcriptional regulation without affecting p21 cellular half-life or inhibiting the kinase activities of C-raf, B-rafV600E, or VEGFR2 (IC50 > 10 µM). Dual telomerase and p21, but not p16 or p27 (gene = CDKN1A, CDKN2A, CDKN1B, respectively), knockdown/inhibition is demonstrated to effectively kill cancer cells both in vitro (% viability inhibition/% Annexin V+ cells induction = 20%/2% or 77%/55%, respectively, following telomerase inhibition by Imetelstat with or without 2.5 µM UC2288 for 24 h in HCT116 colon cancer cultures) and in mice in vivo (% tumor expansion suppression by UC2288 alone/Imetelstat alone/combined treatment = 13%/42%/90%/HCT116 and 4%/23%/92%/ACHN; 30 mg Imetelstat/kg via i.p. and/or 15 mg UC2288/kg via p.o. 3X/wk for 3 wk) by inducing p53- and E2F1-dependent PUMA expression, while p21 overexpression, p53 inactivation by mutation, shRNA-mediated E2F1 or PUMA downregulation abolishes such synergized cell killing. Likewise, reactivating mutant p53 activitiy by CP-31398 (Cat. No. 506166) treatment is reported to resensitize DLD1 (p53 S241F) and A375.S2 (p53 R273H & P309S) to p21 shRNA- & Imetelstat-induced apoptotic cell death and tumor growth inhibition.
      FormWhite solid
      Intert gas (Yes/No) Packaged under inert gas
      Chemical formulaC₂₀H₁₈ClF₆N₃O₂
      Purity≥98% by HPLC
      SolubilityDMSO (50 mg/ml). Use only fresh DMSO for reconstitution.
      Storage +2°C to +8°C
      Protect from light
      Do Not Freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
      Toxicity Standard Handling
      ReferencesGupta, R., et al. 2014. Proc. Natl. Acad. Sci. USA 111, E3062.
      Wettersten, H.I., et al. 2013. Cancer Biol. Ther. 14, 278.