ML349

• 常用名: ML349
• 英文名: ML 349
• CAS号: 890819-86-0
• 分子量: 454.56
• 密度: N/A
• 沸点: N/A
• 分子式: C₂₃H₂₂N₂O₄S₂
• 熔点: N/A
• 闪点: N/A

ML349用途

ML349 是一个有效且特异的酰基蛋白硫酯酶 2 (APT-2) 抑制剂,其 Ki 值为 120 nM。ML349 也是 LYPLA2 的抑制剂,其 IC50 值为 144 nM。

ML349名称

• 中文名: ML349
• 英文名: ML349

ML349生物活性

• 描述: ML349 是一个有效且特异的酰基蛋白硫酯酶 2 (APT-2) 抑制剂,其 Ki 值为 120 nM。ML349 也是 LYPLA2 的抑制剂,其 IC50 值为 144 nM。
• 相关类别:
  信号通路 >> 代谢酶/蛋白酶 >> 磷脂
  研究领域 >> 癌症
• 靶点实验:

  Ki: 120 nM (APT-2)[1] IC50: 144 nM (LYPLA2)[2]

• 体外研究: ML349是酰基蛋白硫酯酶1和2(APT-1和APT-2)的抑制剂,Kis分别> 10000和120±20 nM [1]。 ML349也是LYPLA1和LYPLA2的抑制剂,IC50> 3000和144 nM,分别为[2]。 ML348和ML349不会降低细胞活力,但它们会导致NRAS突变细胞中AKT的轻微激活[3]。
• 细胞实验: 将细胞接种于96孔板中，密度为每孔4000至8000个细胞，并在37℃，5％CO 2下孵育24小时。然后用增加的药物（包括ML349）浓度及其组合处理细胞。根据制造商的方案[3]，通过细胞活力测定来测量细胞活力。
• 参考文献:

  [1]. Won SJ, et al. Molecular Mechanism for Isoform-Selective Inhibition of Acyl Protein Thioesterases 1 and 2 (APT1 and APT2). ACS Chem Biol. 2016 Dec 16;11(12):3374-3382.

  [2]. Adibekian A, et al. Characterization of a Selective, Reversible Inhibitor of Lysophospholipase 2 (LYPLA2).

  [3]. Vujic I, et al. Acyl protein thioesterase 1 and 2 (APT-1, APT-2) inhibitors palmostatin B, ML348 and ML349 have different effects on NRAS mutant melanoma cells. Oncotarget. 2016 Feb 9;7(6):7297-306.

ML349物理化学性质

• 分子式: C₂₃H₂₂N₂O₄S₂
• 分子量: 454.56
• InChIKey: YVIJPELUPZUEJX-UHFFFAOYSA-N
• SMILES: COc1ccc(N2CCN(C(=O)c3cc4c(s3)-c3ccccc3S(=O)(=O)C4)CC2)cc1
• 储存条件: 2-8℃

ML349靶点实验

查看更多实验

实验名称：Primary cell-based high-throughput screening assay for identification of compounds th... 来源：Johns Hopkins Ion Channel Center 靶标：regulator of G-protein signaling 4 isoform 2 [Homo sapiens] External Id：JHICC_RGS_Act_HTS

实验名称：Luminescence-based cell-based primary high throughput screening assay to identify ago... 来源：The Scripps Research Institute Molecular Screening Center 靶标：mu-type opioid receptor isoform MOR-1 [Homo sapiens] External Id：OPRM1-OPRD1_AG_LUMI_1536_1X%ACT PRUN

实验名称：Primary qHTS assay for small molecule inhibitors of Inositol hexaphosphate kinase 1 (... 来源：NCGC External Id：IP6K1-p1

实验名称：QFRET-based biochemical primary high throughput screening assay to identify exosite i... 来源：The Scripps Research Institute Molecular Screening Center 靶标：disintegrin and metalloproteinase domain-containing protein 17 preproprotein [Homo sapiens] External Id：ADAM17_INH_QFRET_1536_1X%INH PRUN

实验名称：Fluorescence-based cell-based primary high throughput screening assay to identify ago... 来源：The Scripps Research Institute Molecular Screening Center 靶标：muscarinic acetylcholine receptor M1 [Homo sapiens] External Id：CHRM1_AG_FLUO8_1536_1X%ACT PRUN

实验名称：uHTS identification of small molecule activators of the adaptive arm of the Unfolded ... 来源：Burnham Center for Chemical Genomics 靶标：N/A External Id：BCCG-A405-UPR-XBP1-PrimaryAgonist-Assay

实验名称：Cytochrome P450 family 3 subfamily A member 4 (CYP3A4) small molecule antagonists: lu... 来源：NCGC External Id：CYP3A4437

实验名称：Cytochrome P450 family 2 subfamily D member 6 (CYP2D6) small molecule antagonists: lu... 来源：NCGC External Id：CYP2D6395

实验名称：Cytochrome P450 family 2 subfamily C member 9 (CYP2C9) small molecule antagonists: lu... 来源：NCGC External Id：CYP2C9536

实验名称：High throughput fluorescence intensity-based biochemical assay to screen for small mo... 来源：University of Pittsburgh Molecular Library Screening Center 靶标：furin (paired basic amino acid cleaving enzyme), isoform CRA_a [Homo sapiens] External Id：MH080376 Biochemical HTS for Inhibitors of the Proprotein Convertase Furin.

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