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Merck
CN

SML0601

BPTES

≥95% (HPLC), powder, glutaminase GLS1 (KGA) inhibitor

别名:

双-2-(5-苯基乙酰胺基-1,3,4-噻二唑-2-基)乙基硫醚

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关于此项目

经验公式(希尔记法):
C24H24N6O2S3
化学文摘社编号:
分子量:
524.68
UNSPSC Code:
12352200
PubChem Substance ID:
NACRES:
NA.77
MDL number:
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产品名称

BPTES, ≥95% (HPLC)

SMILES string

O=C(CC1=CC=CC=C1)NC2=NN=C(S2)CCSCCC3=NN=C(NC(CC4=CC=CC=C4)=O)S3

InChI

1S/C24H24N6O2S3/c31-19(15-17-7-3-1-4-8-17)25-23-29-27-21(34-23)11-13-33-14-12-22-28-30-24(35-22)26-20(32)16-18-9-5-2-6-10-18/h1-10H,11-16H2,(H,25,29,31)(H,26,30,32)

InChI key

MDJIPXYRSZHCFS-UHFFFAOYSA-N

assay

≥95% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 10 mg/mL, clear

storage temp.

2-8°C

Quality Level

Application

双-2-(5-苯基乙酰胺基-1,3,4-噻二唑-2-基)乙基硫醚(BPTES)已被用作谷氨酰胺酶抑制剂。

Biochem/physiol Actions

BPTES是谷氨酰胺酶GLS1的选择性抑制剂。
BPTES是谷氨酰胺酶GLS1(KGA)的选择性抑制剂,GLS1存在于肾和脑中,由myc正向调节,在许多肿瘤和肿瘤细胞系中高度表达。谷氨酰胺酶可将谷氨酰胺转化为谷氨酸,谷氨酸是脑中重要的兴奋性神经递质,可进一步氧化成α-酮戊二酸(供给三羧酸(TCA)循环)和谷胱甘肽,谷胱甘肽对控制活性氧(ROS)水平很重要,对癌细胞生长尤为重要。BPTES可减缓胶质瘤细胞的生长。BPTES是一种非竞争性抑制剂,Ki为3 μmM。
牛痘病毒(VACV)需要谷氨酰胺代谢才能实现最佳复制。双-2-(5-苯基乙酰胺基-1,3,4-噻二唑-2-基)乙基硫醚(BPTES)抑制谷氨酰胺分解可能有望治疗痘病毒感染。

pictograms

Exclamation mark

signalword

Warning

Hazard Classifications

Eye Irrit. 2 - Skin Irrit. 2 - STOT SE 3

target_organs

Respiratory system

存储类别

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable


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谷氨酰胺是谷氨酸和GABA生物合成的常用前体。谷氨酰胺可以利用不同的谷氨酰胺载体在神经元和星形胶质细胞进行细胞内外转运。神经递质谷氨酸可以通过磷酸盐活化的谷氨酰胺酶的作用从谷氨酰胺合成。

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