| BI-D1870P90 RSK inhibitor,ATP-competitive and cell-permeable |
Sample solution is provided at 25 µL, 10mM.
Quality Control & MSDS
- View current batch:
- Purity = 98.99%
- COA (Certificate Of Analysis)
- HPLC
- NMR (Nuclear Magnetic Resonance)
- MSDS (Material Safety Data Sheet)
- Datasheet
Chemical structure
Related Biological Data
| Description | BI-D1870 is an ATP-competitive inhibitor of S6 ribosome for RSK1/2/3/4 with IC50 values of 31 nM/24 nM/18 nM/15 nM, respectively. | |||||
| Targets | RSK4 | RSK3 | RSK2 | RSK1 | ||
| IC50 | 15 nM | 18 nM | 24 nM | 31 nM | ||
| Cell experiment [1]: | |
Cell lines | HEK-293 cells |
Preparation method | The solubility of this compound in DMSO is >19.6mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
Reacting condition | 0-10 μM; 15, 30, 60, 120 and 240 min |
Applications | In HEK-293 cells, BI-D1870 greatly inhibited the PMA-induced phosphorylation of GSK3α and GSK3β. BI-D1870 also inhibited PMA-induced phosphorylation of GSK3 isoforms and another RSK substrate, the protein kinase LKB1 with an IC50 of approx. 1 μM. |
| Animal experiment [2]: | |
Animal models | experimental autoimmune encephalomyelitis (EAE) mice |
Dosage form | 0.5 mg/kg; intraperitoneal injection; every other day for 11 days |
Application | In EAE mice immunized with MOG peptide, BI-D1870 protected mice from EAE by reducing the infiltration of TH1 and TH17 cells into the CNS and decreasing mRNA levels of Ccr6 in TH17 cells. |
Other notes | Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
References: [1] Sapkota G, Cummings L, Newell F, et al. BI-D1870 is a specific inhibitor of the p90 RSK (ribosomal S6 kinase) isoforms in vitro and in vivo. Biochem. J, 2007, 401: 29-38. [2]. Takada I1, Yogiashi Y2, Makishima M3. et al. The ribosomal S6 kinase inhibitor BI-D1870 ameliorated experimental autoimmune encephalomyelitis in mice. Immunobiology. 2016 Feb;221(2):188-92. | |
BI-D1870 Dilution Calculator
calculate
BI-D1870 Molarity Calculator
calculate
| Cas No. | 501437-28-1 | SDF | Download SDF |
| Synonyms | N/A | ||
| Chemical Name | 2-(3,5-difluoro-4-hydroxyanilino)-5,7-dimethyl-8-(3-methylbutyl)-7H-pteridin-6-one | ||
| Canonical SMILES | CC1C(=O)N(C2=CN=C(N=C2N1CCC(C)C)NC3=CC(=C(C(=C3)F)O)F)C | ||
| Formula | C19H23F2N5O2 | M.Wt | 391.42 |
| Solubility | ≥19.55mg/mL in DMSO | Storage | Store at -20°C |
| Physical Appearance | A solid | Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. | ||
BI-D1870 is a cell-permeable inhibitor of the p90 RSK isoforms with IC50 values of 31nM, 24nM, 18nM and 15nM for RSK1, RSK2, RSK3 and RSK4 respectively [1].
BI-D1870 is a derivative of dihydropteridinone and found to be a remarkably specific inhibitor of RSK isoforms. It is an ATP-competitive inhibitor. When the concentrations of ATP are 10μM and 100μM, the IC50 values of BI-D1870 against RSK1 and RSK2 are 5nM, 10nM and 10nM, 20nM, respectively. BI-D1870 also inhibits RSK3 and RSK4 with IC50 values of 18nM and 15nM respectively, when ATP is 100μM. The inhibition activity of BI-D1870 against RSK is more than 500-fold greater than some other AGC kinases suggesting BI-D1870 as a specific inhibitor of RSK. In addition, BI-D1870 is reported to induce the phosphorylation of ERK1/ERK2 and the subsequent phosphorylation of CREB in Rat-2 cells [1].
References:[1] Sapkota G, Cummings L, Newell F, et al. BI-D1870 is a specific inhibitor of the p90 RSK (ribosomal S6 kinase) isoforms in vitro and in vivo. Biochem. J, 2007, 401: 29-38.
ebiomall.com
>
>
>
>
>
>
>
>
>
>
>
>
制冰机原理：
制冰机是一种将水通过蒸发器由制冷系统制冷剂冷却后生成冰的制冷机械设备。根据蒸发器和生成过程方式原理不同，生成的冰的形状也不同，人们一般根据冰形状将制冰机分为颗粒冰机、片冰机、板冰机、管冰机、壳冰机等等。
制冰机的分类：
按冰的形状可分：鳞形片冰机，雪花制冰机，条冰机，板冰机，块冰机（可分食用小块冰机和工业用大块冰机），冰粒机，颗粒机，管冰机，子弹头制冰机。
实验室制冰机种类选择：
我们平时在外面就餐时，经常看到商家在饮料中加入冰块，有时候是方块的，有时候是中空的，还有在菜市场买海鲜的时候也会看到下面铺着一层冰，究竟有什么区别吗？我们在开展实验室工作的时候，应如何选择制冰机呢？
实验室制冰机主要是用于在开展生命科学相关实验时，给样品提供冰浴环境，防止样品（如核酸、蛋白）因为温度的变化导致降解或变质，从而保障实验结果的准确性和有效性。绝大部分的时候，我们的样品是放在EP管、离心管、pcr管等容器里面，然后把样品管插在冰浴中，靠接触来实现温度的保持。由于样品和冰无法直接接触，而是要通过管壁来传输，所以管壁和冰浴的接触面积是冰浴效果的保障，为了更好的保障样品，应尽量的扩大管壁和冰浴的接触面积。
针对以上考虑，实验室制冰机一般选择雪花制冰机，该种类型的制冰机生产出来的冰呈雪花状碎冰，由于颗粒很小，可以和管壁进行密切的接触，保障冰浴效果。
对于出冰的具体要求中，还有一点是非常重要的，出来的雪花冰要求有15-25%的含水量，这样可极大的提高冰浴和管壁的接触效果。
文章来源：厦门国仪科学仪器有限公司
2：冰满探头调整太靠近冰格，顺时针调整180度就好了，也有可能冰满探头坏了。需要更换。
3：水位浮球开关坏，更换。
