MCE 的所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务。

PGMI-004A

CAS No. : 1313738-90-7

MCE 站：PGMI-004A

产品活性：PGMI-004A 是一种有效的磷酸甘油酸变位酶 1 (PGAM1) 抑制剂，IC₅₀ 为 13.1 μM。

研究领域：Metabolic Enzyme/Protease

作用靶点：Phosphatase

In Vitro: PGMI-004A inhibits PGAM1 with an IC₅₀ of approximately 13.1 μM ａnd the K_d value of the PGMI-004A-PGAM1 interaction is determined to be 7.2±0.7 μM from fluorescence-based binding assay. PGMI-004A may allosterically modulate the enzyme activity of PGAM1. The K_i value is determined to be 3.91±2.50 μM using Dixon plot analysis. The K_d value for protein-ligand interaction is calculated to be 9.4±2.0 μM. Inhibition of PGAM1 activity by PGMI-004A (20 μM) treatment results in decreased 2-PG ａnd increased 3-PG levels in H1299 cells, which could be rescued by treatment with methyl-2-PG. Treatment with PGMI-004A (20 μM) results in significantly reduced lactate production that is rescued by methyl-2-PG treatment, but has no significant effect on intracellular ATP levels. PGMI-004A (20 μM) treatment results in decreased oxidative PPP flux ａnd NADPH/NADP+ratio, as well as reduced biosynthesis of lipids ａnd RNA, ａnd cell proliferation in H1299 cells. PGMI-004A treatment results in decreased cell proliferation of diverse human cancer ａnd leukemia cells, but not control human dermal fibroblasts (HDF), human foreskin fibroblasts (HFF), human HaCaT keratinocyte cells ａnd human melanocyte PIG1 cells, suggesting minimal non-specific toxicity of PGMI-004A in normal, proliferating human cells.

In Vivo: The xenograft experiment is performed by injecting H1299 cells to nude mice. Six days post-injection, mice are divided into two groups (n=8/group) ａnd treated with either PGMI-004A (100mg/kg/day) or vehicle for 21 days. PGMI-004A treatment results in significantly decreased tumor growth ａnd tumor size in treated mice compared with mice receiving vehicle control. Moreover, treatment with PGMI-004A effectively inhibits PGAM1 enzyme activity in tumors in vivo in resected tumors from xenograft nude mice.

相关产品：Natural Product Like Compound Library  |  Bioactive Compound Library Plus  |  Metabolism/Protease Compound Library  |  Anti-Cancer Compound Library  |  Glycolysis Compound Library  |  Anti-Blood Cancer Compound Library  |  Phosphatase Inhibitor Library  |  Cyclosporin A  |  Tacrolimus  |  Ebselen  |  Salubrinal  |  Suramin sodium salt  |  Calyculin A  |  β-Glycerophosphate disodium salt pentahydrate  |  Sodium orthovanadate  |  TPI-1  |  MSI-1436 lactate  |  GSK 2830371  |  NSC 663284  |  Okadaic acid  |  Sodium metatungstate  |  D-erythro-Sphingosine  |  Sodium stibogluconate  |  Voclosporin  |  BCI  |  SF1670  |  Pentamidine isethionate  |  MB05032  |  3α-Aminocholestane  |  ARL67156 trisodium salt  |  PTP1B-IN-2  |  BVT948  |  GNF362  |  L-690330  |  (-)-p-Bromotetramisole oxalate

品牌介绍:
•   MCE (MedChemExpress) 拥有数百种全球独家化合物，我们致力于为全球科研客户提供*新*全的高品质小分子活性化合物；
•   10,000 多种高选择性抑制剂、激动剂涉及各热门信号通路及疾病领域；
•   设有专业的实验中心和严格的质控、验证体系；
•   提供 LC/MS、NMR、HPLC、手性分析、元素分析等各项质检报告，确保产品的高纯度、高品质；
•   产品的生物活性多经各国客户实验验证；
•   Nature, Cell, Science 等多种期刊及制药收录了MCE客户的科研成果；
•   专业团队跟踪*新的制药及生命科学研究进展，为您提供全球*新的活性化合物；
•   与世界各大制药公司及知名科研机构建立了长期的合作。