- GSK-3 Inhibitor IX (BIO)
- SB 216763
- CHIR-99021 (CT99021)
- AZD2858
- LY2090314
| CHIR-98014GSK-3β inhibitor,selective and ATP-competitive |
Sample solution is provided at 25 µL, 10mM.
Nature.2017 Jan 19;541(7637):417-420.
Nature.2018 Nov;563(7731):407-411.Nature.2018 Jun 13.Nature.2018 Jun 27.Nature.2018 Mar 29;555(7698):673-677.Nature.2017 Sep 7;549(7670):96-100.Nature.2016 Apr 21;532(7599):398-401.
Science.2016 Aug 5;353(6299)594-8Nat Nanotechnol.2017 Dec;12(12):1190-1198.Nature Biotechnology.2017 Jun;35(6):569-576Nat Med.2018 Sep 17.Cell.2018 Dec 21. pii: S0092-8674(18)31561-7.Cell.Available online 25 October 2018.Cell.2018 Sep 27. pii: S0092-8674(18)31183-8.Cell.2018 Jun 28;174(1):172-186.e21.Cell.2018 Feb 22;172(5):1007-1021.e17.Cell.2017 Nov 30;171(6):1284-1300.e21.Cell.2017 Aug 17. pii: S0092-8674(17)30869-3.Cell.2017 Jul 13;170(2):312-323Nat Med.2018 Jan 29.Nat Med.2017 Nov;23(11):1342-1351.Cell.2017 Apr 6;169(2):286-300.Cell.2015 Aug 27;162(5):987-1002.Cell.2015 Feb 12;160(4):729-44.Nature Medicine.2017 Apr;23(4):493-500.Cancer Cell.2018 May 14;33(5):905-921.e5.Cancer Cell.2018 Apr 9;33(4):752-769.e8.Cancer Cell.2018 Mar 12;33(3):401-416.e8.Cancer Cell.2017 Aug 14;32(2):253-267.e5.Nat Methods.2018 Jul;15(7):523-526.Cell Stem Cell.2018 May 3;22(5):769-778.e4.Cell Stem Cell.2017 Nov 20. pii: S1934-5909(17)30375-2.Quality Control & MSDS
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- Purity = 99.13%
- COA (Certificate Of Analysis)
- HPLC
- NMR (Nuclear Magnetic Resonance)
- MSDS (Material Safety Data Sheet)
- Datasheet
Chemical structure
| Description | CHIR-98014 is a potent inhibitor of GSK-3α and GSK-3β with IC50 values of 0.65 nM and 0.58 nM, respectively. | |||||
| Targets | GSK-3β | GSK-3α | p70 S6K | |||
| IC50 | 0.58 nM | 0.65 nM | >1 μM | |||
| Cell experiment: | |
Cell lines | Insulin receptor– expressing CHO-IR cells and primary rat hepatocytes |
Preparation method | The solubility of this compound in DMSO is <10 mm.="" general="" tips="" for="" obtaining="" a="" higher="" concentration:="" please="" warm="" the="" tube="" at="" 37="" °c="" for="" 10="" minutes="" and/or="" shake="" it="" in="" the="" ultrasonic="" bath="" for="" a="" while.stock="" solution="" can="" be="" stored="" below="" -20°c="" for="" several=""> |
Reaction Conditions | 24h; EC50=106 nM (CHO-IR cells); EC50=107 nM (rat hepatocytes). |
Applications | CHIR 98014 resulted in a stimulation of the GS activity ratio above basal. The concentrations of CHIR 98014 causing half-maximal GS stimulation (EC50) were 106 nM for CHO-IR cells and 107 nM for rat hepatocytes. |
| Animal experiment: | |
Animal models | Female db/db mice. |
Dosage form | 30 mg/kg; oral taken |
Applications | Markedly diabetic and insulin-resistant db/db mice treated with 30 mg/kg CHIR 98014 exhibited a significant reduction in fasting hyperglycemia within 4 h of treatment and showed improved glucose disposal during an IPGTT. |
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] Ring D B, Johnson K W, Henriksen E J, et al. Selective glycogen synthase kinase 3 inhibitors potentiate insulin activation of glucose transport and utilization in vitro and in vivo[J]. Diabetes, 2003, 52(3): 588-595. | |
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| Cas No. | 252935-94-7 | SDF | Download SDF |
| Chemical Name | 6-N-[2-[[4-(2,4-dichlorophenyl)-5-imidazol-1-ylpyrimidin-2-yl]amino]ethyl]-3-nitropyridine-2,6-diamine | ||
| Canonical SMILES | C1=CC(=C(C=C1Cl)Cl)C2=NC(=NC=C2N3C=CN=C3)NCCNC4=NC(=C(C=C4)[N+](=O)[O-])N | ||
| Formula | C20H17Cl2N9O2 | M.Wt | 486.31 |
| Solubility | ≥8.1mg/mL in DMSO with gentle warming | 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. | ||
CHIR-98014 is a potent inhibitor of GSK-3α and GSK-3β with IC50 values of 0.65 nM and 0.58 nM, respectively [1]
GSK-3 (Glycogen synthase kinase 3) is a serine/threonine protein kinase and plays a pivotal role in a number of central intracellular signaling pathways, including cellular proliferation, migration, inflammation and immune responses, glucose regulation, and apoptosis. Recently, it has been reported that GSK-3 abnormally expressed in a variety of diseases, including Type II diabetes, Alzheimer"s Disease, inflammation, cancer, and bipolar disorder [2, 3].
CHIR-98014 is a potent GSK-3α and GSK-3β inhibitor. When tested with insulin receptor-expressing CHO-IR cells or primary rat hepatocytes, CHIR-98014 stimulated the GS activity ratio as high as two- to three fold compared with basal in a dose dependent manner. Similarly, in isolated type 1 skeletal muscle from insulin-sensitive lean Zucker and from insulin-resistant ZDF rats, administration of CHIR-98014 activated GS activity ratio [1]. In mouse ES-D3 cells, CHIR-98014 treatment (48 and 72 hours later) resulted in a significant activation of the Wnt/beta-catenin pathway via inhibiting GSK-3 [4].
In markedly diabetic and insulin-resistant db/db mice model, oral administration of CHIR-98014 (30mg/kg) significantly reduced fasting hyperglycemia within 4 hours and improved glucose disposal during an ipGTT [1].
References: [1].Ring, D.B., et al., Selective glycogen synthase kinase 3 inhibitors potentiate insulin activation of glucose transport and utilization in vitro and in vivo. Diabetes, 2003. 52(3): p. 588-95.[2]. Pan WA, et al. The RNA recognition motif of NIFK is required for rRNA maturation during cell cycle progression. RNA Biol. 2015. 12(3):255-67.[3]. McCubrey JA, et al. GSK-3 as potential target for therapeutic intervention in cancer. Oncotarget. 2014. 5(10):2881-911.[4]. Naujok O, et al. Cytotoxicity and activation of the Wnt/beta-catenin pathway in mouse embryonic stem cells treated with four GSK3 inhibitors. BMC Res Notes. 2014. 7(1):273-281.
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就好像撒一撮芝麻在培养基那么大的地方上，我们不能知道它会怎么落。
原代细胞产品专家齐氏生物提醒，原代细胞培养注意事项，供参考：
1、实验材料要新鲜，从活体分离材料后要低温保存，并尽快进行细胞分离实验。
2、无菌操作。操作时用的培养液，可加平时细胞培养液5倍含量的青链霉素。
3、用酶法分离细胞时，注意酶液的浓度和控制消化时间。
贴块法分离细胞时，注意动作要轻柔，不要伤到细胞组织，组织块边缘尽量平整有利于细胞游离。
4、培养液的选择。不同的细胞有对培养液中营养的要求不同，根据所分离细胞的特性选择。
不知道楼主明白没有,意思是说培养基上的癌细胞可能过密,导致营养缺乏,无法满足生长分裂的需要,所以进入G0期,暂时不生长分裂.
3,MHC基因位于第六号染色体上,MHC存在于人类和哺乳动物的细胞表面.根据MHC所编码的分子结构和功能不同而将其分为1,2,3类?.1,2类分子结构相似,主要功能是向T细胞呈递抗原,是被T细胞识别的重要靶分子.1类存在于除红细胞以外的机体所以细胞膜上,2类分子仅存在于成熟B细胞,一些T细胞和抗原呈递细胞膜上,3类分子不具备上述功能,属于血清蛋白.
现在楼主应该明白了,MHC是不参与抗原抗体特异性结合的,是专门用来呈递抗原的.
细胞株(cell strain) 是通过选择法或克隆形成法从原代培养细胞中获得具有特殊性质或标志物的细胞称为细胞株。一般认为，细胞株是用单细胞分离培养或通过筛选的方法，由单细胞增殖形成的细胞群。细胞株的特殊性质或标志必须在整个培养期间始终存在。
细胞系(cell line) 是原代细胞经首次传代成功后即为细胞系。泛指一般可能传代的细胞。其中能够连续传代的细胞叫做连续细胞系或无限细胞系，不能连续培养的称为有限细胞系。大多数二倍体细胞为有限细胞系。由原先存在于原代培养物中的细胞世系所组成。如果不能继续传代，或传代次数有限， 可称为有限细胞系(finite cell line)， 如可以连续培养， 则称为连续细胞系(continuous cell line)， 培养50代以上并无限培养下去。人类肿瘤细胞，在体外培养半年以上，生长稳定，并连续传代的即可称为连续性株或系。
不知道楼主明白没有,意思是说培养基上的癌细胞可能过密,导致营养缺乏,无法满足生长分裂的需要,所以进入G0期,暂时不生长分裂.
3,MHC基因位于第六号染色体上,MHC存在于人类和哺乳动物的细胞表面.根据MHC所编码的分子结构和功能不同而将其分为1,2,3类?.1,2类分子结构相似,主要功能是向T细胞呈递抗原,是被T细胞识别的重要靶分子.1类存在于除红细胞以外的机体所以细胞膜上,2类分子仅存在于成熟B细胞,一些T细胞和抗原呈递细胞膜上,3类分子不具备上述功能,属于血清蛋白.
现在楼主应该明白了,MHC是不参与抗原抗体特异性结合的,是专门用来呈递抗原的.
哪种要好，有什么要求吗？接种多少代的细胞？
1.培养基最好是培养原代细胞专门的培养基或说是配套的培养基; 2.关键还是生长因子等的浓度; 3.如果需要的话,需要明胶包被.
2.关键还是生长因子等的浓度；
3.如果需要的话,需要明胶包被.
