IOX2(Glycine)
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
IOX2是HIF-1α脯氨酰羟化酶-2(PHD2)的有效选择性抑制剂,在无细胞实验中,IOX2对PHD2/ELGN-1的IC50为21 nM,相较于JMJD2A、JMJD2C、JMJD2E、JMJD3或2OG加氧酶FIH,IOX2对PHD2显示出大于100倍的高选择性 [1]。
PHD包括三种异构体,为PHD1、PHD2和PHD3。PHD是利用氧作为共底物的双加氧酶,提供这些酶的氧感应功能的分子基础。报道表明PHD对逐渐缺氧具有显著敏感性,当细胞暴露于培养基中,逐渐缺氧时, HIF-1α蛋白和DNA结合活性逐步增加[2]。
在RCC4细胞中,50 μM IOX2抑制HIF-1α羟基化[1]。缺氧诱导因子(HIF)系统与动物中低氧/缺氧的信号传导相关。HIF-α异构体的水平以氧依赖性方式受HIF脯氨酰羟化酶(PHD或EGLN酶)活性的控制,其是Fe(II)和2-氧戊二酸(2OG)依赖性氧化酶[1,3]。
参考文献:
Murray J K, Balan C, Allgeier A M, et al. Dipeptidyl-quinolone derivatives inhibit hypoxia inducible factor-1α prolyl hydroxylases-1,-2, and-3 with altered selectivity[J]. Journal of combinatorial chemistry, 2010, 12(5): 676-686.
Berra E, Benizri E, Ginouvès A, et al. HIF prolyl‐hydroxylase 2 is the key oxygen sensor setting low steady‐state levels of HIF‐1α in normoxia[J]. The EMBO journal, 2003, 22(16): 4082-4090.
Chowdhury R, Candela-Lena J I, Chan M C, et al. Selective small molecule probes for the hypoxia inducible factor (HIF) prolyl hydroxylases[J]. ACS chemical biology, 2013, 8(7): 1488-1496.
- 1. Peng H, Purkerson JM, et al. "Acidosis induces antimicrobial peptide expression and resistance to uropathogenic E coli infection in kidney collecting duct cells via HIF-1α." Am J Physiol Renal Physiol. 2019 Dec 16. PMID:31841391
- 2. Peng K, Chen WR, et al. "Dexmedetomidine post-treatment attenuates cardiac ischaemia/reperfusion injury by inhibiting apoptosis through HIF-1α signalling." J Cell Mol Med. 2020;24(1):850–861. PMID:31680420
- 3. LUKE ERBER. "Functional Proteomics Analysis To Discover And Characterize Oxygen-Dependent Cellular Pathways." UNIVERSITY OF MINNESOTA. 2019.
- 4. Zhou T, Erber L, et al. "Proteomic analysis reveals diverse proline hydroxylation-mediated oxygen-sensing cellular pathways in cancer cells." Oncotarget. 2016 Nov 29;7(48):79154-79169. PMID:27764789
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 352.34 |
Cas No. | 931398-72-0 |
Formula | C19H16N2O5 |
Solubility | insoluble in EtOH; insoluble in H2O; ≥17.6 mg/mL in DMSO |
Chemical Name | 2-[(1-benzyl-4-hydroxy-2-oxoquinoline-3-carbonyl)amino]acetic acid |
SDF | Download SDF |
Canonical SMILES | C1=CC=C(C=C1)CN2C3=CC=CC=C3C(=C(C2=O)C(=O)NCC(=O)O)O |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |
激酶实验 [1]: | |
Alpha筛选实验 |
使用50 mM HEPES,0.1 % BSA,pH 7.5溶液稀释试剂,加入0.01 % Tween20,在室温下使其平衡,然后将其加入到实验板中。在室温下,使用低容量384孔板进行催化转换实验。反应体系包含0.5 ~ 25 nM酶,30 ~ 1000 nM生物素化的底物肽,1 ~ 10 μM Fe(II),100 μM抗坏血酸盐以及5 ~ 40 μM 2OG,在室温下进行反应。使用EDTA终止反应 (5 μM)。将AlphaScreen供体(链霉亲和素共轭)受体(蛋白A共轭)珠先与多肽产物抗体孵育,再将其加入上述反应体系 (5 μM) 中。使用箔密封实验板,使其避光,在室温下温育60分钟。在PHERAstar FS酶标仪上,以680 nm激发波长/570 nm发射波长为参数,对样品进行读数。在20 μM反应体系中,珠粒的最终浓度为20 μM/mL。使用Prism 5计算IC50值。 |
细胞实验 [1]: | |
细胞系 |
RCC4细胞 |
制备方法 |
在DMSO中的溶解度大于10 mM。若配制更高浓度的溶液,一般步骤如下:请将试管置于37 °C加热10分钟和/或将其置于超声波浴中震荡一段时间。原液于-20 °C可放置数月。 |
反应条件 |
50 μM |
实验结果 |
在RCC4细胞中,IOX2 (50 μM) 抑制HIF-1α羟基化。 |
References: [1]. Murray JK1, Balan C, Allgeier AM et al. Dipeptidyl-quinolone derivatives inhibit hypoxia inducible factor-1α prolyl hydroxylases-1, -2, and -3 with altered selectivity. J Comb Chem. 2010 Sep 13;12(5):676-86. |
Description | IOX2 is a potent inhibitor of HIF-1α prolyl hydroxylase-2 (PHD2) with IC50 of 21 nM. | |||||
Targets | PHD2 | |||||
IC50 | 21 nM |
质量控制和MSDS
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