GlpBio

ST 045849

目录号: GC50570纯度: >98.50%
ST 045849是一种O-GlcNAc转移酶(OGT)抑制剂，IC50值为53μM。
ST 045849
Cas No.: 442665-87-4
规格价格库存数量操作
1mg¥738.00现货
1
5mg¥1,845.00现货
1
10mg¥2,860.00现货
1
10mM (in 1mL DMSO)¥2,030.00现货
1
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产品描述 Description

ST 045849 is an inhibitor of O-GlcNAc transferase (OGT), with an IC50 value of 53μM[1]. ST 045849 is currently widely used in the research for screening low toxicity OGT inhibitors[2].

In vitro, ST 045849 treatment significantly inhibited the growth of HKCI-2 cells after 72 hours, with an IC50 value of 50.44nM[3]. Mouse embryonic stem cells were treated with ST 045849 (0.2nM) for 30min exhibited the reduced O-GlcNAcylated Notch1 and Notch1 protein expression in the plasma membrane, accompanied by a reduction in glucose production[4]. ST 045849 treatment (15μM; 6h) can significantly reduce the reactive oxygen species (ROS) levels in NE-4C cells cultured under high glucose concentration (500mg/dl)[5]. ST 045849 treatment (0.4mM) for 2h can significantly inhibit the overall O-GlcNAc glycosylation in adipocytes, and induce an increase in the number of small lipid droplets and the appearance of a small number of extremely large lipid droplets in oleic acid-treated adipocytes[6].

In vivo, ST 045849 treatment (20mg/kg/day) via gavage for 4 days in mouse model of diabetic pregnancy significantly reduced the incidence of neural tube defects in the embryos[5].

References:
[1] Wu X, Wang M, Cao Y, et al. Discovery of a novel OGT inhibitor through high-throughput screening based on homogeneous time-resolved fluorescence (HTRF)[J]. Bioorganic Chemistry, 2023, 139: 106726.
[2] Liu Y, Ren Y, Cao Y, et al. Discovery of a low toxicity O-GlcNAc transferase (OGT) inhibitor by structure-based virtual screening of natural products[J]. Scientific reports, 2017, 7(1): 12334.
[3] Xu W, Zhang X, Wu J, et al. O-GlcNAc transferase promotes fatty liver-associated liver cancer through inducing palmitic acid and activating endoplasmic reticulum stress[J]. Journal of hepatology, 2017, 67(2): 310-320.
[4] Jeon J H, Suh H N, Kim M O, et al. Glucosamine-induced OGT activation mediates glucose production through cleaved Notch1 and FoxO1, which coordinately contributed to the regulation of maintenance of self-renewal in mouse embryonic stem cells[J]. Stem cells and development, 2014, 23(17): 2067-2079.
[5] Kim G, Cao L, Reece E A, et al. Impact of protein O-GlcNAcylation on neural tube malformation in diabetic embryopathy[J]. Scientific Reports, 2017, 7(1): 11107.
[6] Yang Y, Fu M, Li M D, et al. O-GlcNAc transferase inhibits visceral fat lipolysis and promotes diet-induced obesity[J]. Nature communications, 2020, 11(1): 181.

ST 045849是一种O-GlcNAc转移酶(OGT)抑制剂，IC50值为53μM[1]。ST 045849目前被广泛用于筛选低毒性OGT抑制剂的研究中[2]。

在体外，ST 045849处理72小时后能显著抑制HKCI-2细胞的生长，IC50值为50.44nM[3]。小鼠胚胎干细胞经0.2nM 浓度的ST 045849处理30分钟后，质膜中O-GlcNAc修饰的Notch1蛋白和Notch1蛋白表达均降低，同时伴随葡萄糖生成减少[4]。在高糖浓度(500mg/dl)培养条件下，15μM浓度的ST 045849处理6小时可显著降低NE-4C细胞中的活性氧水平[5]。0.4mM浓度的ST 045849处理2小时能显著抑制脂肪细胞整体O-GlcNAc糖基化水平，并在油酸处理的脂肪细胞中诱导小脂滴数量增加及少量超大脂滴的出现[6]。

在体内，糖尿病妊娠小鼠模型连续4天灌胃给予20mg/kg/day剂量的ST 045849，能显著降低胚胎神经管缺陷的发生率[5]。

实验参考方法 Experimental Reference Method

Cell experiment [1]:

Cell lines

ATDC5 cells

Preparation Method

The chondrocytes (ATDC5 cells) were cultured in Dulbecco’s modified Eagle’s medium (DMEM) containing 10% foetal bovine serum (FBS) and 1% P/S. ATDC5 cells were maintained at 37°C under humidified air with 5% CO2. In order to set up the osteoarthritis cell model, ATDC5 cells were stimulated with 10µg/mL lipopolysaccharide (LPS) for 12h. Meanwhile, ST 045849 was incubated with the cells at a concentration of 10μM for 24 hours. Cell viability of the indicated ATDC5 cells was assessed with the CCK-8 kit. In brief, cells were seeded into 96-well plates at a density of 5000 cells/well and incubated for 48h. After that, each well was added with 10μL CCK-8 cocktail and subjected to further incubation at 37°C for 2h. A microplate reader was used to measure the absorbance value at a wavelength of 450nm.

Reaction Conditions

10μM; 24h

Applications

ST 045849 significantly restored the decreased cell viability of ATDC5 cells induced by LPS.
Animal experiment [2]:

Animal models

C57BL/6J female mice

Preparation Method

Ten-week-old female C57BL/6J mice were injected with streptozotocin in 0.1mM citrate buffer at 65mg/kg body weight intravenously. Blood glucose level was measured by tail clipping using Blood Glucose Monitoring System. The value ≥250mg/dl or 14mM indicated diabetes Mellitus (DM). The normal glucose level (~150mg/dl or ~8mM) was restored by subcutaneous implantation of insulin pellets. A group of sham-operated mice was used as non-diabetic (ND) controls. Female mice were mated with normal male mice in the afternoon. The presence of vaginal plug on the following morning was denoted as embryonic (E) day 0.5. Insulin pellets were removed at E5.5 to make the female animals of the DM group hyperglycemic again before the beginning of neurulation at E8.5. Diabetic pregnant mice were given gavage feeding with an OGT inhibitor ST 045849 (20mg/kg/day), suspended in water (vehicle), at E6.5 for 4 days. At E10.5 (late neurulation), mice were sacrificed and the embryos were collected for examination.

Dosage form

20mg/kg/day for 4 days; p.o.

Applications

ST 045849 treatment significantly reduced the incidence of neural tube defects in the embryos of diabetic pregnant mice.

References:
[1] He C, Wu Q, Zeng Z, et al. OGT-induced O-GlcNAcylation of NEK7 protein aggravates osteoarthritis progression by enhancing NEK7/NLRP3 axis[J]. Autoimmunity, 2024, 57(1): 2319202.
[2] Kim G, Cao L, Reece E A, et al. Impact of protein O-GlcNAcylation on neural tube malformation in diabetic embryopathy[J]. Scientific Reports, 2017, 7(1): 11107.

产品文档 Product Documents

Purity:>98.50%

化学性质Chemical Properties

CAS 号
442665-87-4
SMILES
OC(C1CC(N(/C(S1)=N/C2=CC=C(C=C2)Cl)CCC34CC5CC(C4)CC(C3)C5)=O)=O
分子式
C23H27ClN2O3S
分子量
446.99 g/mol
溶解性
44.7mg/mL in DMSO
保存条件
Store at -20°C
General tips
请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。
为了提高溶解度，请将管子加热至 37°C，然后在超声波浴中震荡一段时间。
Shipping Condition
评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备 RT，或根据请求配备蓝冰。

计算工具摩尔浓度 / 稀释 / 分子量 / 单位换算 / 体内配方 / 溶解度

g/mol