CBR-5884
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.
CBR-5884是一种选择性的3-磷酸甘油酸脱氢酶(PHGDH)抑制剂,IC50为7 μM。PHGDH催化丝氨酸生物合成的第一关键步骤,通过局部放大和核因子红细胞-2相关因子2(Nrf2)介导的上调,在肿瘤和癌细胞系中过表达。因此CBR-5884能抑制癌细胞从头合成丝氨酸。
CBR5884选择性抑制具有高倾向丝氨酸合成的乳腺癌和黑色素瘤细胞系的增殖,但对依赖胞外丝氨酸摄取的癌细胞系无影响。CBR-5884是一种非竞争性的和时间依赖性的PHGDH抑制剂,并干扰其低聚状态。CBR-5884对丝氨酸标记有作用的剂量与体外生化一致,作用于PHGDH的IC50为33±12 μm。在该浓度下,CBR-5884对其他两种NAD+依赖性脱氢酶,乳酸脱氢酶(LDH)和MDH1无影响。作用于3-PG和NAD +的Ki值分别为50±20 μm和50±3 μm。通过两个独立的细胞活性测定,浓度高达40 μM的CBR-5884通常是非细胞毒性的。在丝氨酸充满培养基中,CBR-5884治疗乳腺癌细胞系剂量依赖性抑制不依靠胞外丝氨酸生长的四种细胞系的生长,30 μM CBR-5884生长抑制范围是35%到60%。丝氨酸消耗增加了在丝氨酸充满条件下敏感的细胞系中CBR-5884的疗效,这通过30 μM CBR-5884导致增殖下降80-90%得以证明。[ 1 ]
参考文献:
Identification of a small molecule inhibitor of 3-phosphoglycerate dehydrogenase to target serine biosynthesis in cancers. Proc Natl Acad Sci U S A. 2016 Feb 16;113(7):1778-83.
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 336.39 |
Cas No. | 681159-27-3 |
Formula | C14H12N2O4S2 |
Solubility | insoluble in EtOH; insoluble in H2O; ≥16.8 mg/mL in DMSO |
Chemical Name | ethyl 5-(furan-2-carboxamido)-3-methyl-4-thiocyanatothiophene-2-carboxylate |
SDF | Download SDF |
Canonical SMILES | O=C(NC1=C(SC#N)C(C)=C(C(OCC)=O)S1)C2=CC=CO2 |
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。 |
质量控制和MSDS
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