MKC9989
目录号 : GC32910
MKC9989是一种HAA抑制剂，且能抑制IRE1α其IC50值在0.23μM至44μM的范围之间。
Cas No.:1338934-20-5
Sample solution is provided at 25 µL, 10mM.
MKC9989 is a Hydroxy aryl aldehydes (HAA) inhibitor and also inhibits IRE1α with an IC50 of 0.23 to 44 μM.
At 10 μM concentration, MKC9989 completely inhibits both basal and thapsigargin induced splicing of XBP1 mRNA. These effects are observed even in cells pre-treated with thapsigargin, indicating that MKC9989 can fully reverse the onset of XPB1 splicing after the UPR is initiated. In parallel analysis, MKC9989, significantly stabilizes the RIDD target CD59 mRNA when co-administered with thapsigargin relative to thapsigargin treatment alone and modestly increases levels of CD59 mRNA in non-stressed cells, the latter likely reflects the inhibition of baseline RIDD activity. In contrast to effects on XBP1 splicing, MKC9989 moderately stabilizes CD59 levels when administered 2 hour post treatment with thapsigargin. Finally, the potency of MKC9989 against the splicing of XBP1 mRNA (EC50=0.33 μM) is comparable to its potency against RNA cleavage in vitro[1].
[1]. Sanches M, et al. Structure and mechanism of action of the hydroxy-aryl-aldehyde class of IRE1 endoribonuclease inhibitors. Nat Commun. 2014 Aug 28;5:4202.
Cell experiment: | Human RPMI 8226 plasmacytoma cells are grown in monolayer culture using medium (DMEM) supplemented with 10% fetal calf serum (FCS) at 37°C and 5% CO2. MKC9989 is prepared as 10 mM stocks in DMSO, stored at -20°C, and diluted in medium. Thapsigargin (Tg) is resuspended in DMSO and diluted in medium. Cells are grown to 50% confluency, treated with 1 μM Tg and/or 10 μM MKC9989 at the indicated time points. After incubation of cells for the indicated periods, cells are harvested[1]. |
References: [1]. Sanches M, et al. Structure and mechanism of action of the hydroxy-aryl-aldehyde class of IRE1 endoribonuclease inhibitors. Nat Commun. 2014 Aug 28;5:4202. | |
| Cas No. | 1338934-20-5 | SDF | |
| Canonical SMILES | O=CC1=C(O2)C(C(C)=C(CCOCCOC)C2=O)=CC(OC)=C1O | ||
| 分子式 | C17H20O7 | 分子量 | 336.34 |
| 溶解度 | DMSO : ≥ 50 mg/mL (148.66 mM);Water : < 0.1 mg/mL (insoluble) | 储存条件 | Store at -20°C |
| General tips | 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。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.9732 mL | 14.8659 mL | 29.7318 mL |
| 5 mM | 0.5946 mL | 2.9732 mL | 5.9464 mL |
| 10 mM | 0.2973 mL | 1.4866 mL | 2.9732 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet