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VER-155008
CAS No. 1134156-31-2
VER-155008 ( VER-155008 | VER 155008 | VER155008 )
产品货号. M10467 CAS No. 1134156-31-2
一种有效的 Hsp70 家族 (Hsc70/Hsp7/Grp78) 抑制剂，对 Grp78 的 Kd 为 80 nM。
纯度: >98% (HPLC)
COA
Datasheet
HNMR
HPLC
MSDS
Handing Instructions
| 规格 | 价格/人民币 | 库存 | 数量 |
| 2MG | ￥259 | 有现货 |
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| 5MG | ￥449 | 有现货 |
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| 10MG | ￥591 | 有现货 |
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| 25MG | ￥1107 | 有现货 |
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| 50MG | ￥2009 | 有现货 |
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| 100MG | ￥3357 | 有现货 |
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| 200MG | ￥4257 | 有现货 |
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| 500MG | 获取报价 | 有现货 |
|
| 1G | 获取报价 | 有现货 |
|
| 1 mL x 10 mM in DMSO | ￥552 | 有现货 |
|
生物学信息
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产品名称VER-155008
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注意事项本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断
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产品简述一种有效的 Hsp70 家族 (Hsc70/Hsp7/Grp78) 抑制剂，对 Grp78 的 Kd 为 80 nM。
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产品描述A potent Hsp70 family (Hsc70/Hsp7/Grp78) inhibitor with Kd of 80 nM for Grp78; shows cellular activity in HCT116 cells (GI50= 5uM), has similar potencies in both Grp78 and Hsp70; inhibits the proliferation of human breast and colon cancer cell lines with GI50s of 5.3-14.4 uM, and induces Hsp90 client protein degradation in both HCT116 and BT474 cells; induced caspase-3/7 dependent apoptosis in BT474 cells.
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体外实验VER-155008 is an inhibitor of Hsc70 and Hsp70, with IC50s of 0.5 μM, 2.6 μM, and 2.6 μM for Hsp70, Hsc70 and Grp7, respectively, a with a Kd of 0.3 μM for Hsp70, but shows no activities against Hsp90, with an IC50 of >200 μM. VER-155008 inhibits the proliferation of a variety of human colon and breast tumor cell lines, such as BT474, MB-468, HCT116 and HT29 cells, with GI50s of 10.4 μM, 14.4 μM, 5.3 μM, and 12.8 μM, respectively. VER-155008 (5-40 μM) induces client protein degradation in HCT116 and BT474 carcinoma cells. VER-155008 also induces apoptosis in human tumor cell lines. VER-155008 (0.05-5 μM) reverses Aβ-induced axonal degeneration in cultured neurons. VER-155008 (10 μM or 25 μM) inhibits Hsp70 and suppresses the proliferation of LNCaP95 cells. VER-155008 also reduces full-length androgen receptor (AR-FL) and androgen receptor splice variant 7 (AR-V7) protein expression.
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体内实验VER-155008 (25 mg/kg, i.v.) exhibits plasma clearance in naive female BALB/c mice. VER-155008 (40 mg/kg, i.v.) also shows rapid plasma clearance, and reduces the tumor levels in the HCT116 tumor bearing nude BALB/c mice. VER-155008 (10 μmol/kg/day, i.p.) rescues memory deficits, and reduces axonal swelling associated with amyloid plaques in 5XFAD mice. VER-155008 (89.9 μmol/kg/day, i.p.) penetrates into the brain after administration in 5XFAD mice. VER-155008 also decreases amyloid plaques and PHF-tau associated with amyloid plaques in 5XFAD mice.
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同义词VER-155008 | VER 155008 | VER155008
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通路Cytoskeleton/Cell Adhesion Molecules
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靶点HSP
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受体GRP78|HSC70|HSP70
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研究领域Cancer
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适应症——
化学信息
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CAS Number1134156-31-2
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分子量556.4006
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分子式C25H23Cl2N7O4
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纯度>98% (HPLC)
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溶解度DMSO: ≥ 37 mg/mL
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SMILESO[C@@H]([C@H]([C@H](N1C(NCC2=CC=C(Cl)C(Cl)=C2)=NC3=C(N=CN=C31)N)O4)O)[C@H]4COCC5=CC=C(C#N)C=C5
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化学全称Adenosine, 5'-O-[(4-cyanophenyl)methyl]-8-[[(3,4-dichlorophenyl)methyl]amino]-
运输与储存
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储存条件(-20℃)
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运输条件With Ice Pack
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稳定性≥ 2 years
参考文献
1. Macias AT, et al. J Med Chem. 2011 Jun 23;54(12):4034-41.
2. Massey AJ, et al. Cancer Chemother Pharmacol. 2010 Aug;66(3):535-45.
3. Kim SH, et al. Biochem Biophys Res Commun. 2014 Nov 7;454(1):36-41.
产品手册
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