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16

抑制剂 & 化合物

6

天然产物

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Cat. No. Product Name Target Signaling Pathways
T69625 Benitrobenrazide

Hexokinase 2 inhibitor 1

Hexokinase Metabolism
Benitrobenrazide (Hexokinase 2 inhibitor 1) 是一种新型可口服的己糖激酶 2 (HK2) 抑制剂,具有抗癌抗肿瘤活性,通过靶向糖酵解来阻断癌细胞生长。Benitrobenrazide 抑制 SW1990 和 SW480 异种移植模型中的肿瘤生长,可用于研究癌症。
T5882 3-Bromopyruvic acid

Hexokinase II Inhibitor II, 3-BP,3-溴丙酮酸,Bromopyruvic acid

Apoptosis; Hexokinase; Autophagy Apoptosis; Autophagy; Metabolism
3-Bromopyruvic acid (Hexokinase II Inhibitor II, 3-BP) 是己糖激酶 II 抑制剂,是针对肝癌细胞的一种抗肿瘤剂。
T76111 Hexokinase (ScHEX1)

Hexokinase(ScHEX1) 是一种糖酵解酶己糖激酶,收到 N-乙酰氨基葡萄糖的抑制。N-乙酰氨基葡萄糖对 Hexokinase(ScHEX1) 的抑制导致其与线粒体外膜分离,而导致 NLRP3炎症小体激活。
TQ0055 AMG-3969

Glucokinase Metabolism
AMG-3969 是一种葡萄糖激酶-葡糖激酶调节蛋白相互作用的干扰物,IC50=为4 nM。
T16479 PF-04937319

Others; Glucokinase Metabolism; Others
PF-04937319 是一种葡萄糖激酶激活剂 (EC50 =154.4  μM)。 PF-04937319 保持降糖功效,同时降低许多其他 GKA 观察到的低血糖风险。 PF-04937319可用于治疗2型糖尿病的研究。
T3104 Globalagliatin

LY2608204

Glucokinase Metabolism
Globalagliatin (LY2608204) 是一种葡萄糖激酶 (GK) 活化剂,EC50=42 nM。
T3312 AM-2394

AM2394

Glucokinase Metabolism
AM-2394 是新型的 glucokinase 激活剂 (GKA)。它能够激活葡萄糖激酶 (GK),EC50=60 nM。
T26712 AZD-1656

AZD 1656

Glucokinase Metabolism
AZD-1656 是口服有效的葡萄糖激酶选择性激活剂,EC50为 60 nM。AZD1656在2 型糖尿病中有研究的价值。
T12056 MK-0941 free base

Glucokinase Metabolism
MK-0941 free base 是一种口服具有活力的葡糖激酶抑制剂,在葡萄糖浓度为 2.5 和 10 mM 的条件下,对重组人 glucokinase 的EC50值分别为 240 和 65 nM。它具有较强的降血糖特性,是研究 2 型糖尿病的候选药物。
T15159 Dorzagliatin

HMS5552

Glucokinase Metabolism
Dorzagliatin (HMS5552) 是双重作用的葡萄糖激酶 (glucokinase;GK) 激活剂,可改善 2 型糖尿病的血糖控制,提高胰腺 β 细胞功能。
T0239 Lonidamine

AF1890,氯尼达明,DICA,Diclondazolic Acid

Apoptosis; Hexokinase; Mitochondrial Metabolism Apoptosis; Metabolism
Lonidamine (Diclondazolic Acid) 是一种抗肿瘤药物,是己糖激酶、线粒体丙酮酸载体和质膜单羧酸转运蛋白抑制剂,同时也抑制线粒体复合物 II。
T15654 Ketohexokinase inhibitor 1

PF-06835919

Others Others
Ketohexokinase inhibitor 1 是一种酮己糖激酶抑制剂(对 KHK-C 和 KHK-A 的 IC50:分别为 8.4 nM 和 66 nM)。
T72092 2-Deoxy-D-glucose 6-phosphate disodium

2-Deoxy-D-glucose 6-phosphate disodium,一种2-Deoxy-D-glucose的衍生物,是通过己糖激酶在哺乳动物细胞中作用于2-DG而生成。该化合物是葡萄糖代谢的竞争性抑制剂,主要通过抑制己糖激酶从而阻碍糖酵解过程。
T83889 C-02

C-02是一种由巨噬细胞抑制剂Lonidamine和Cereblon配体Thalidomide组成的蛋白酶体靶向嵌合体(PROTAC)。在20 µM浓度下使用时,可诱导786-O和PANC-1细胞中的Hexokinase 2降解。C-02对786-O、4T1、PANC-1、HGC-27和MCF-7癌细胞具有细胞毒性(IC50分别为34.07、5.08、31.53、6.11和21.65 µM)。同时,20 µM浓度下减少4T1细胞的细胞外酸化率(ECAR)和氧气消耗率(OCR),表明其抑制糖酵解和引起线粒体损伤。在体内,C-02(50 mg/kg)能减少4T1小鼠乳腺癌模型的肿瘤体积,并诱导肿瘤内细胞因子积累和细胞焦亡。
T35683 2-deoxy-D-Glucose-13C6

2-deoxy-D-Glucose-13C6

2-deoxy-D-Glucose-13C6is intended for use as an internal standard for the quantification of 2-deoxy-D-glucose by GC- or LC-MS. 2-deoxy-D-Glucose is a glucose antimetabolite and an inhibitor of glycolysis.1,2It inhibits hexokinase, the enzyme that converts glucose to glucose-6-phosphate, as well as phosphoglucose isomerase, the enzyme that converts glucose-6-phosphate to fructose-6-phosphate.32-deoxy-D-Glucose (16 mM) induces apoptosis in SK-BR-3 cells, as well as inhibits the growth of 143B oste...
T65387 Paromomycin, sulfate (1:1)

Paromomycin (Sulfate Salt) is an aminoglycoside that is active against Gram-negative and many Gram-positive bacteria as well as some protozoa and cestodes. Paromomycin in combination with sodium stibogluconate has proven to be effective in African and Indian VL (visceral leishmaniasis) and improves survival in African VL[3]. PS (Paromomycin Sulfate) is effective for elimination of B. coli without hematological side effects[4]. The activity of phosphoglucose isomerase was slightly inhibited by 10...

化合物

Benitrobenrazide
Cat.No: T69625
Synonym: Hexokinase 2 inhibitor 1
Target: Hexokinase
3-Bromopyruvic acid
Cat.No: T5882
Synonym: Hexokinase II Inhibitor II, 3-BP,3-溴丙酮酸,Bromopyruvic acid
Target: Apoptosis, Hexokinase, Autophagy
Hexokinase (ScHEX1)
Cat.No: T76111
Synonym:
Target:
AMG-3969
Cat.No: TQ0055
Synonym:
Target: Glucokinase
PF-04937319
Cat.No: T16479
Synonym:
Target: Others, Glucokinase
Globalagliatin
Cat.No: T3104
Synonym: LY2608204
Target: Glucokinase
AM-2394
Cat.No: T3312
Synonym: AM2394
Target: Glucokinase
AZD-1656
Cat.No: T26712
Synonym: AZD 1656
Target: Glucokinase
MK-0941 free base
Cat.No: T12056
Synonym:
Target: Glucokinase
Dorzagliatin
Cat.No: T15159
Synonym: HMS5552
Target: Glucokinase
Lonidamine
Cat.No: T0239
Synonym: AF1890,氯尼达明,DICA,Diclondazolic Acid
Target: Apoptosis, Hexokinase, Mitochondrial Metabolism
Ketohexokinase inhibitor 1
Cat.No: T15654
Synonym: PF-06835919
Target: Others
2-Deoxy-D-glucose 6-phosphate disodium
Cat.No: T72092
Synonym:
Target:
C-02
Cat.No: T83889
Synonym:
Target:
2-deoxy-D-Glucose-13C6
Cat.No: T35683
Synonym: 2-deoxy-D-Glucose-13C6
Target:
Paromomycin, sulfate (1:1)
Cat.No: T65387
Synonym:
Target:
Cat. No. Product Name Target Signaling Pathways
T19500 Palmitelaidic Acid

trans-Palmitoleic acid,9-trans-Hexadecenoic acid,软脂酸

Glucokinase; AMPK; PPAR Chromatin/Epigenetic; DNA Damage/DNA Repair; Metabolism; PI3K/Akt/mTOR signaling
trans-Palmitelaidic Acid (trans-Palmitoleic acid) 是palmitoleic acid 的反式异构体。Palmitoleic acid 是血清和组织中最丰富的脂肪酸之一。
T6742 2-Deoxy-D-glucose

2-Deoxy-D-arabino-hexose,2-deoxyglucose,D-Arabino-2-deoxyhexose,Ba 2758,D-2-脱氧葡萄糖,NSC 15193,2-DG,2-脱氧-D-葡萄糖

Apoptosis; Hexokinase; HSV Apoptosis; Metabolism; Microbiology/Virology
2-Deoxy-D-glucose (2-DG) 是葡萄糖的类似物,是一种糖酵解抑制剂。2-Deoxy-D-glucose 具有抗病毒活性,还具有抑制细胞增殖、诱导细胞凋亡的活性。
T4900 (±)-Methyl Jasmonate

(±)-茉莉酸甲酯,甲基茉莉酮酸酯,(±)-Jasmonic Acid methyl ester,Methyl 2-(3-oxo-2-(pent-2-en-1-yl)cyclopentyl)acetate

Others; Endogenous Metabolite Metabolism; Others
Methyl 2-(3-oxo-2-(pent-2-en-1-yl)cyclopentyl)acetate ((±)-Jasmonic Acid methyl ester) 是内源性代谢产物的一种。
T5113 L-GLUCOSE

L-葡萄糖,L-(-)-Glucose

Others Others
L-Glucose (L-(-)-Glucose) 是一种 D-glucose 的对映体,可促进食物的摄取。
T4726 D-Glucose 6-phosphate sodium

G6P sodium salt,D-Glucose 6-phosphate sodium salt,D-葡萄糖-6-磷酸钠盐,Sodium Glucose-6-Phosphate

Others; Endogenous Metabolite Metabolism; Others
D-Glucose 6-phosphate sodium (G6P sodium salt) 是内源性代谢产物的一种。
T5069 D-Glucose 6-phosphate potassium salt

Others Others
在细胞中,当葡萄糖被己糖激酶或葡萄糖激酶磷酸化或在糖原分解过程中通过磷酸葡萄糖变位酶转化葡萄糖 1-磷酸时,会产生D-glucose 6-phosphate (G6P)。 G6P 位于糖酵解和戊糖磷酸途径的起点。当血糖水平高时,它也可以作为糖原储存。

天然产物

Palmitelaidic Acid
Cat.No: T19500
Synonym: trans-Palmitoleic acid,9-trans-Hexadecenoic acid,软脂酸
Target: Glucokinase, AMPK, PPAR
2-Deoxy-D-glucose
Cat.No: T6742
Synonym: 2-Deoxy-D-arabino-hexose,2-deoxyglucose,D-Arabino-2-deoxyhexose,Ba 2758,D-2-脱氧葡萄糖,NSC 15193,2-DG,2-脱氧-D-葡萄糖
Target: Apoptosis, Hexokinase, HSV
(±)-Methyl Jasmonate
Cat.No: T4900
Synonym: (±)-茉莉酸甲酯,甲基茉莉酮酸酯,(±)-Jasmonic Acid methyl ester,Methyl 2-(3-oxo-2-(pent-2-en-1-yl)cyclopentyl)acetate
Target: Others, Endogenous Metabolite
L-GLUCOSE
Cat.No: T5113
Synonym: L-葡萄糖,L-(-)-Glucose
Target: Others
D-Glucose 6-phosphate sodium
Cat.No: T4726
Synonym: G6P sodium salt,D-Glucose 6-phosphate sodium salt,D-葡萄糖-6-磷酸钠盐,Sodium Glucose-6-Phosphate
Target: Others, Endogenous Metabolite
D-Glucose 6-phosphate potassium salt
Cat.No: T5069
Synonym:
Target: Others
TargetMol Loading
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