| 中文名称: | Bisindolylmaleimide I | ||||
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| 英文名称: | Bisindolylmaleimide I | ||||
| 别名: | Bisindolylmaleimide I 3-(1-(3-(Dimethylamino)propyl)-1H-indol-3-yl)-4-(1H-indol-3-yl)-1H-pyrrole-2,5-dione | ||||
| CAS No: | 133052-90-1 | 分子式: | C25H24N4O2 | 分子量: | 412.48 |
| CAS No: | 133052-90-1 | ||||
| 分子式: | C25H24N4O2 | ||||
| 分子量: | 412.48 | ||||
基本信息
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产品编号：B10806 |
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产品名称：Bisindolylmaleimide I |
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CAS: |
133052-90-1 |
储存条件 |
粉末 |
-20℃ |
四年 |
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分子式： |
溶于液体 |
-80℃(避光) |
六个月 |
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分子量： |
412.48 |
-20℃(避光) |
一个月 |
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化学名： |
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Solubility (25°C) |
体外 |
DMSO |
82mg/mL (198.79mM) |
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Ethanol |
1mg/mL (2.42mM) |
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Water |
Insoluble |
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体内（现配现用） |
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＜1mg/ml表示微溶或不溶。 |
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普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。 |
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请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 |
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制备储备液
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浓度
溶液体积 质量 |
1mg |
5mg |
10mg |
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1mM |
2.4244mL |
12.1218mL |
24.2436mL |
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5mM |
0.4849mL |
2.4244mL |
4.8487mL |
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10mM |
0.2424mL |
1.2122mL |
2.4244mL |
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50mM |
0.0485mL |
0.2424mL |
0.4849mL |
生物活性
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产品描述 |
一种高度选择，可渗透细胞，可逆的 PKC抑制剂，Ki 值为14nM。 |
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靶点/IC50 |
PKCβ2 |
PKCβ1 |
PKCα |
PKCγ |
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16nM |
17nM |
20nM |
20nM |
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体外研究 |
Bisindolylmaleimide I is a competitive inhibitor with respect to ATP (Ki=14nM) and displays high selectivity for PKC as compared to five different protein kinases.GF 109203X efficiently prevents PKC-mediated phosphorylations of an Mr=47,000 protein in platelets and of an Mr=80,000 protein in Swiss 3T3 cells. GF 109203X inhibits collagen- and a-thrombininduced platelet aggregation as well as collagen-triggered ATP secretion.However,ADP-dependent reversible aggregation is not modified.In Swiss 3T3 fibroblasts, GF 109203X reverses the inhibition of epidermal growth factor binding induced by phorbol 12,13-dibutyrate and prevents [3H] thymidine incorporation into DNA, only when this is elicited by growth promoting agents which activate PKC. |
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体内研究 |
Pial arteriole diameter changes are monitored using a closed cranial window in vivo microscopy technique.The pial arteriole dilatory response associated with SNS is decreased by 45%,when comparing DM vs either ND or TR rats.Also,pial arteriolar dilations to topical KCl and NS1619 are largely attenuated in DM rats,but not in ND or TR animals.These responses are completely restored by the acute application of Bisindolylmaleimide I to the brain surface.The PKC inhibitor has no effect on vascular responses in normoglycemic and TR animals.In conclusion,DM-associated chronic impairment of neurovascular coupling may be readily reversed by a PKC-α/β/γ inhibitor or prevented via pancreatic islet transplantation. Specific PCK isoforms (α/β/γ) are believed to be mechanistically linked to the neurovascular uncoupling seen with hyperglycemia. |
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推荐实验方法(仅供参考)
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激酶实验： |
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Assay of PKC is arrayed by measuring 32Pi transferred from [γ-32Pi] ATP to lysine-rich histone type Ill-s.The reaction mixture (80μL) contains 50mM Tris-HCI,pH 7.4.100μM CaCl2,10mM MgCI2,37.5μg/mL histone type Ill-s,l0μM [γ-32Pi] ATP (1250cpm/pmol),31μM bovine brain phosphatidylserine and 0.5μM 1,2 sn-dioleylglycerol.15μL of purified PKC (final concentration in assay 0.38μg/mL) is added to the incubation mixture.After 10minutes,the reaction is stopped by addition of at 30μL of casein 30mg/mL and 0.9mL of 12% trichlomacetic acid. |
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细胞实验: |
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细胞系 |
SNU-407结肠癌细胞 |
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浓度 |
1μM |
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处理时间 |
48小时 |
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方法 |
细胞增殖是通过3-（4,5 -二甲基吡啶-2-基）-2,5-二苯基四唑溴化物（MTT）测定的。细胞接种在96孔板中，并让其生长过夜。细胞血清饥饿18-24小时，然后用1mM的乙酰胆碱在100μL的无血清RPMI 1640培养液处理48小时。在加入卡巴胆碱30分钟前加入抑制剂。10微升MTT溶液（5毫克/毫升）加到各孔中，并将板在37℃温育3小时。除去培养基后，所形成的甲臜晶体的溶解在100μL的DMSO中。在570nm处的吸光度用酶标仪测定，背景吸光度在690nm处被减去。各测定法一式三份进行。 |
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动物实验: |
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Three sets of Lewis rats is used for this study:1) euglycemic 4–6 month old non-diabetic controls (ND group,n=11);2) streptozotocin (STZ)-treated diabetic rats (6 month old,4 months post-STZ) (DM group,n=6);and 3) STZ-treated diabetic animals, subjected to pancreatic islet transplantation soon after the establishment of the diabetic model,studied 100–110 days after the transplant (TR group,n=7). |
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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：
质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)
摩尔浓度计算公式
用本工具协助配置特定浓度的溶液，使用的计算公式为：
开始浓度 x 开始体积 = 最终浓度 x 最终体积
稀释公式
稀释公式一般简略地表示为：C1V1 = C2V2 ( 输入 输出 )
