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品質等級
化驗
≥98% (HPLC)
形狀
powder
顏色
white to beige
溶解度
DMSO: 10 mg/mL, clear
儲存溫度
2-8°C
SMILES 字串
CC1=CC(NC(N2CCN(CC3=CC=C(C(F)(F)F)C=C3)CC2)=S)=NC(C)=C1
InChI
1S/C20H23F3N4S/c1-14-11-15(2)24-18(12-14)25-19(28)27-9-7-26(8-10-27)13-16-3-5-17(6-4-16)20(21,22)23/h3-6,11-12H,7-10,13H2,1-2H3,(H,24,25,28)
InChI 密鑰
PJNSZIQUFLWRLH-UHFFFAOYSA-N
生化／生理作用
NCT-503是磷酸甘油酸脱氢酶（PHGDH）的抑制剂，可催化葡萄糖衍生的丝氨酸合成的第一步限速步骤。NCT-503可减少葡萄糖衍生的丝氨酸生成，并抑制培养物中PHGDH依赖性癌细胞和异种移植瘤的生长，并导致MDA-MB-468细胞发生G1/S细胞周期阻滞。NCT-503能够减少将葡萄糖和外源丝氨酸的一碳单元掺入核苷酸，这可能有助于其发挥抗癌活性。NCT-503对PHGDH的IC50 值为2.5 μM，对一组其他脱氢酶无效，并且在一组168个G蛋白偶联受体（GPCR）中具有极低的交叉反应性。NCT-503已被发现对3-PG和NAD+均不具有竞争性，并且表现出良好的稳定性（溶于测定缓冲液中48小时后，>98%）和水溶性。
推薦產品
NCT-503 阴性对照品，是NCT-503的结构类似物，可从Sigma购买。要了解更多信息并购买NCT-503阴性对照品， 请单击此处 。
訊號詞
Warning
危險聲明
危險分類
Skin Irrit. 2
儲存類別代碼
11 - Combustible Solids
水污染物質分類（WGK）
WGK 3
閃點（°F）
Not applicable
閃點（°C）
Not applicable
其他客户在看
Nirmalya Sen et al.
Molecular carcinogenesis, 57(10), 1342-1357 (2018-06-07)
Ewing sarcoma (EWS) is a soft tissue and bone tumor that occurs primarily in adolescents and young adults. In most cases of EWS, the chimeric transcription factor, EWS-FLI1 is the primary oncogenic driver. The epigenome of EWS cells reflects EWS-FLI1
Samah Elsaadi et al.
Experimental hematology & oncology, 10(1), 3-3 (2021-01-06)
Multiple myeloma (MM) is a hematological malignancy characterized by the clonal expansion of plasma cells in the bone marrow. To date, this disease is still incurable and novel therapeutic approaches are required. Phosphoglycerate dehydrogenase (PHGDH) is the first and rate-limiting
Yingfeng Xia et al.
Cancer research, 79(15), 3837-3850 (2019-05-16)
MYCN amplification drives the development of neuronal cancers in children and adults. Given the challenge in therapeutically targeting MYCN directly, we searched for MYCN-activated metabolic pathways as potential drug targets. Here we report that neuroblastoma cells with MYCN amplification show
Birte Arlt et al.
Journal of enzyme inhibition and medicinal chemistry, 36(1), 1282-1289 (2021-07-02)
The small-molecule inhibitor of phosphoglycerate dehydrogenase, NCT-503, reduces incorporation of glucose-derived carbons into serine in vitro. Here we describe an off-target effect of NCT-503 in neuroblastoma cell lines expressing divergent phosphoglycerate dehydrogenase (PHGDH) levels and single-cell clones with CRISPR-Cas9-directed PHGDH
Shauni Lien Geeraerts et al.
Molecular cancer therapeutics, 20(1), 50-63 (2020-11-19)
Metabolic rewiring is a hallmark of cancer that supports tumor growth, survival, and chemotherapy resistance. Although normal cells often rely on extracellular serine and glycine supply, a significant subset of cancers becomes addicted to intracellular serine/glycine synthesis, offering an attractive
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