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。
CAS No. : 1113044-49-7
MCE 国际站:FIT-039
产品活性:FIT-039 是一种选择性,ATP 竞争性且具有口服活性的 CDK9 抑制剂,对 CKD9/cyclin T1 的 IC50 为 5.8 μM。FIT-039 不抑制其他 CDK 和其他激酶。FIT-039 抑制 HSV-1 (IC50 为 0.69 μM),HSV-2,人腺病毒和人 CMV 的复制。FIT-039 是一种有前途的抗病毒剂,可用于抑制耐药性 HSV 和其他 DNA 病毒。
研究领域:Cell Cycle/DNA Damage | Anti-infection
作用靶点:CDK | HSV | CMV | DNA/RNA Synthesis
In Vitro: FIT-039 (30 μM; 3 hours; HEK293 cells) treatment decreases phosphorylated CTD in the infected or noninfected cells to a level lower than that shown by Flavopiridol. FIT-039 reduces the expression levels of HSV-1 immediate-early genes (IEGs) and early and late genes.
FIT-039 inhibits replication of the HSV-1 genome in a dose-dependent manner (EC50 and EC80 are 0.69 μM and 4.0 μM, respectively).
FIT-039 potently suppresses 8 kinases (GSK3β, PKN1, haspin, p70s6K, DYRK1B, GSK3α, IRR, and DYRK3) other than CDK9 on the 332-kinase panel. These kinases are involved in the replication of various viruses.
In Vivo: Treatment with the FIT-039 ointment twice a day suppresses skin lesions and rescues mice (male BALB/c mice injected with HSV-1) from lethality in a dose-dependent manner. The healing of lesions is observed with 5% to 10% FIT-039 ointment, leading to the complete regression of zosteriform spread on day 10, which is also observed with the 5% ACV ointment.
FIT-039 does not affect body weight gain in mice administrated with an overdose of this compound (1000 mg/kg/d) for 14 days, and no changes are observed in biological markers in their blood.
相关产品:Bioactive Compound Library Plus | Anti-Infection Compound Library | Cell Cycle/DNA Damage Compound Library | Kinase Inhibitor Library | Antiviral Compound Library | Anti-Aging Compound Library | Orally Active Compound Library | Anti-Breast Cancer Compound Library | Anti-Blood Cancer Compound Library | Human Metabolite Library | Cancer Stem Cells Compound Library | Heterocyclic Compound Library | Membrane Protein-targeted Compound Library | Highly Selective Inhibitors Library | SY-5609 | CLK1/2-IN-1 | IBU-DC Phosphoramidite | MFH290 | 2,4-D sodium salt | Thailanstatin D | SB-218078 | Toyocamycin | (S)-LY3177833 hydrate | Carboplatin-d4 | Dinaciclib | Caracemide | EGFR/HER2/CDK9-IN-2 | CDK8-IN-11 | Farudodstat | SNS-032 | M2N12 | Palbociclib-d8 | Ara-ATP | EGFR/CDK2-IN-1 | BSJ-04-132 | (E/Z)-Zotiraciclib | DNA31 | 2'-OMe-Ac-C Phosphoramidite | CCT-251921 | BS-181 | PMEDAP | Dasabuvir | DNA Gyrase-IN-4 | Uridine triphosphate-13C9,15N2 sodium
热门产品线:重组蛋白 | 化合物库 | 天然产物 | 荧光染料 | PROTAC | 同位素标记物 | 寡核苷酸 | 抗体 | 点击化学
Trending products:Recombinant Proteins | Bioactive Screening Libraries | Natural Products | Fluorescent Dye | PROTAC | Isotope-Labeled Compounds | Oligonucleotides | Antibodies | Click Chemistry
货号: HY-18944
品牌介绍:
• MCE (MedChemExpress) 拥有200 多种全球独家化合物库,我们致力于为全球科研客户提供前沿最全的高品质小分子活性化合物;
• 50,000 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;
• 产品种类涵盖各种重组蛋白,多肽,常用试剂盒 ,更有 PROTAC、ADC 等特色产品,广泛应用于新药研发、生命科学等科研项目;
• 提供虚拟筛选,离子通道筛选,代谢组学分析检测分析,药物筛选等专业技术服务;
• 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 等多种顶级期刊及制药专利收录了MCE客户的科研成果;
• 专业团队跟踪最新的制药及生命科学研究进展,为您提供全球最新的活性化合物;
• 与世界各大制药公司及知名科研机构建立了长期的合作。