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上海源葉生物科技有限公司

主營產(chǎn)品: S30260異硫氰酸胍,30259鹽酸胍,嗜熱菌蛋白酶

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聯(lián)人:
何小姐
話:
86-021-61559134
機:
15921386130
真:
86-021-55068248
址:
上海市松江區(qū)長塔路465號6幢
編:
200433
網(wǎng)址:
www.shyuanye.com
鋪:
http://www.zjmenchuan.com/st191837/
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S50725
S50725
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更新時間:2024-07-01 21:59:59瀏覽次數(shù):138

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【簡單介紹】
產(chǎn)品描述:ICG-001isapotentandselectiveWntsignalingmodulator
  • 產(chǎn)品描述:

    ICG-001 is a potent and selective Wnt signaling modulator. ICG-001 modulates Wnt signaling and increased the expression of genes beneficial for cardiac regeneration in epicardial cells. ICG-001 binds cAMP-responsive element binding (CREB)-binding protein (CBP) to disrupt its interaction with β-catenin and inhibit CBP function as a coactivator of Wnt/β-catenin-mediated transcription. ICG-001 induces cytotoxicity of multiple myeloma cells in Wnt-independent manner. Note: Chemical structures of ICG-001 and PRI-724 look very close, but they are not the same molecule. Many vendors confused them.

  • 靶點: IC50: 3 μM (CBP)
  • 體外研究: ICG-001 increases caspase activity in colon carcinoma cell lines (SW480 or HCT116) but not in normal colonic epithelial cells (CCD-841Co). The increased caspase activity is manifested in selective cytotoxicity in colorectal cancer cells. cDNA microarray analysis demonstrated that ICG-001 had a very selective effect on gene transcription. Interestingly, two of the most highly up-regulated mRNAs in cancer cells (survivin and S100A4) are down-regulated by ICG-001. Down-regulation of survivin is notable, because survivin has been shown to inhibit caspase activation. It was also demonstrated that ICG-001 reduces endogenous survivin levels in a TCF/β-catenin fashion in vitro (Fig. 4 A and B). Reference: Proc Natl Acad Sci U S A. 2004 Aug 24;101(34):12682-7. https://www.ncbi.nlm.nih.gov/pmc/articles/pmid/15314234/
  • 體內(nèi)研究: A water-soluble analog of ICG-001 was evaluated in vivo in two mouse models of cancer. The Min mouse, which has a germ-line mutation in one allele of the APC tumor suppressor gene, is a well characterized model for human familial adenomatous polyposis. Administration of the analog for 9 weeks reduced the formation of colon and small intestinal polyps by 42% as effectively as the nonsteroidal antiinflammatory agent Sulindac (Table 1), which has consistently demonstrated efficacy in this model (33). No overt toxicity was detected throughout the course of treatment. In the SW620 nude mouse xenograft model of tumor regression, 150 mg/kg, i.v. of the analog demonstrated a dramatic reduction in tumor volume over the 19-day course of treatment (Fig. 5C Left), with no mortality or weight loss (Fig. 5C Right). Reference: Proc Natl Acad Sci U S A. 2004 Aug 24;101(34):12682-7. https://www.ncbi.nlm.nih.gov/pmc/articles/pmid/15314234/
  • 參考文獻:
    1: Rao P, Pang M, Qiao X, Yu H, Wang H, Yang Y, Ren X, Hu M, Chen T, Cao Q, Wang Y, Khushi M, Zhang G, Wang YM, Heok P'ng C, Nankivell B, Lee VW, Alexander SI, Zheng G, Harris DC. Promotion of β-catenin/Foxo1 signaling ameliorates renal interstitial fibrosis. Lab Invest. 2019 Jun 26. doi: 10.1038/s41374-019-0276-z. [Epub ahead of print] PubMed PMID: 31243340.
    2: Bocchicchio S, Tesone M, Irusta G. Convergence of Wnt and Notch signaling controls ovarian cancer cell survival. J Cell Physiol. 2019 May 13. doi: 10.1002/jcp.28775. [Epub ahead of print] PubMed PMID: 31087357.
    3: Taiyab A, Holms J, West-Mays JA. β-Catenin/Smad3 Interaction Regulates Transforming Growth Factor-β-Induced Epithelial to Mesenchymal Transition in the Lens. Int J Mol Sci. 2019 Apr 27;20(9). pii: E2078. doi: 10.3390/ijms20092078. PubMed PMID: 31035577; PubMed Central PMCID: PMC6540099.
    4: Cui Y, Wu X, Lin C, Zhang X, Ye L, Ren L, Chen M, Yang M, Li Y, Li M, Li J, Guan J, Song L. AKIP1 promotes early recurrence of hepatocellular carcinoma through activating the Wnt/β-catenin/CBP signaling pathway. Oncogene. 2019 Jul;38(27):5516-5529. doi: 10.1038/s41388-019-0807-5. Epub 2019 Apr 1. PubMed PMID: 30936461.
    5: Chen Y, Wen H, Zhou C, Su Q, Lin Y, Xie Y, Huang Y, Qiu Q, Lin J, Huang X, Tan W, Min C, Wang C. TNF-α derived from M2 tumor-associated macrophages promotes epithelial-mesenchymal transition and cancer stemness through the Wnt/β-catenin pathway in SMMC-7721 hepatocellular carcinoma cells. Exp Cell Res. 2019 May 1;378
  • 溶解度: DMSO  50mg/ml
    母液保存:分裝凍存,避免反復凍融;-20℃,1個月;-80℃,6個月(稀釋后溶液溫度低保存可能會析出,盡量現(xiàn)用現(xiàn)配)
    細胞實驗:先用DMSO溶解:再用培養(yǎng)基進行稀釋,稀釋過程建議分段進行,避免濃度變化過快導致化合物析出。若稀釋過程中出現(xiàn)化合物析出的情況,  可采用超聲的方法使其復溶。在稀釋時要確保工作液中  DMSO  的終濃度盡量在0.1%以下,不要超過0.5%,并設置相應濃度的DMSO對照組。
    動物實驗:先用DMSO溶解:再用水或者生理鹽水等去稀釋,稀釋過程建議分段進行,避免濃度變化過快導致化合物析出。若稀釋過程中出現(xiàn)化合物析出的情況,  可采用超聲的方法使其復溶。可以通過添加助溶劑來幫助溶解,比如植物油、Tween80、甘油、羧甲基纖維素鈉和PEG400等。具體方式請參考文獻。懸濁液可用于口服和腹腔注射,不會影響產(chǎn)品活性。
  • 保存條件: -20℃
  • 配置溶液濃度參考:
    1mg 5mg 10mg
    1 mM 1.823 ml 9.114 ml 18.227 ml
    5 mM 0.365 ml 1.823 ml 3.645 ml
    10 mM 0.182 ml 0.911 ml 1.823 ml
    50 mM 0.036 ml 0.182 ml 0.365 ml
  • 注意:部分產(chǎn)品我司僅能提供部分信息,我司不保證所提供信息的性,僅供客戶參考交流研究之用。
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