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抑制剂 & 化合物

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T1140	Doxycycline hydrochloride Doxylin,盐酸多西环素,Vibramycin,Hyclate	MMP; Antibacterial; Antibiotic	Microbiology/Virology; Proteases/Proteasome
	Doxycycline hydrochloride (Hyclate) 是一种四环素抗生素，是口服有效的广谱金属蛋白酶抑制剂，具有抗菌活性。
T5318	666-15 CREB inhibitor	Epigenetic Reader Domain	Chromatin/Epigenetic
	666-15 (CREB inhibitor) 是一种选择性CREB 抑制剂，IC50为 81 nM，可抑制乳腺癌异种移植模型中的肿瘤生长。
T10200	9-Hydroxyellipticine hydrochloride	Others	Others
	9-Hydroxyellipticine hydrochloride is a inhibitor of Topo II and RyR. It exhibits antitumor, antioxidant and catecholamine-releasing activities. 9-Hydroxyellipticine hydrochloride inihibits Hela S-3 and 293T cells (IC50s: 1.6 μM and 1.2μM).
T83857	Soluble Epoxide Hydrolase PROTAC 1a sEH Proteolysis-targeting Chimera 1a,Soluble Epoxide Hydrolase Proteolysis-targeting Chimera 1a,sEH PROTAC 1a
	Soluble epoxide hydrolase (sEH) PROTAC 1a是一种利用蛋白质降解靶向嵌合体(PROTAC)技术，通过连接区域将cereblon配体1与sEH抑制剂t-TUCB结合。该化合物通过促进sEH的降解，特异性抑制sEH的水解酶活性(IC50 = 0.8 nM)，相较于其磷酸酶活性(IC50 = >10,000 nM)具有较高选择性。sEH PROTAC 1a还特定促进细胞质中而非过氧体中的sEH降解，并通过溶酶体而非蛋白酶体实现其降解。它能够降低thapsigargin诱导的HepG2与293T细胞中磷酸化的inositol-requiring enzyme 1α (IRE1α)水平和X-box结合蛋白1 (XBP1)剪接，表明能减少ER应激。
T78758	IHMT-IDH1-053	Isocitrate Dehydrogenase (IDH)	Metabolism
	IHMT-IDH1-053（compound 16）为高选择性不可逆IDH1R132H突变抑制剂，IC50值仅为4.7 nM。对IDH1wt和IDH2wt/突变体活性低。该化合物在IDH1R132H突变293T细胞中显著抑制2-羟基戊二酸（2-HG）生成，IC50为28 nM。IHMT-IDH1-053通过与IDH1R132H蛋白的Cys269残基形成共价键，结合至NADPH结合袋附近的变构袋。此外，它能够抑制携带IDH1R132突变的HT1080细胞系及原代AML细胞增殖。
T36684	Ipivivint
	Ipivivint, a first-in-class, orally active and potent CDC-like kinase (CLK) inhibitor, inhibits CLK1 (IC50=1.4 μM), CLK2 (IC50=0.002 μM) and CLK3 (IC50=0.022 μM). Ipivivint reduces Wnt pathway signaling gene expression through inhibiting CLK activity and serine and arginine rich splicing factor (SRSF) phosphorylation and disrupting spliceosome activity. Ipivivint can be used for the research of cancer[1]. Ipivivint (SW480 cells; 0.01~10 μM; 1 hour) potently inhibits SRSF5/6 phosphorylation[1].Ip...

化合物

Doxycycline hydrochloride

Cat.No: T1140

Synonym: Doxylin,盐酸多西环素,Vibramycin,Hyclate

Target: MMP, Antibacterial, Antibiotic

666-15

Cat.No: T5318

Synonym: CREB inhibitor

Target: Epigenetic Reader Domain

9-Hydroxyellipticine hydrochloride

Cat.No: T10200

Synonym:

Target: Others

Soluble Epoxide Hydrolase PROTAC 1a

Cat.No: T83857

Synonym: sEH Proteolysis-targeting Chimera 1a,Soluble Epoxide Hydrolase Proteolysis-targeting Chimera 1a,sEH PROTAC 1a

Target: Isocitrate Dehydrogenase (IDH)

Cat. No.	Product Name	Target	Signaling Pathways
T1687	Doxycycline Vibramycin,多西环素,Doxiciclina,Doxytetracycline,Doxycyclinum,强力霉素	MMP; ribosome; Antibacterial; Antibiotic; Parasite	Microbiology/Virology; Proteases/Proteasome
	Doxycycline (Doxiciclina) 属于四环素类抗生素，是一种广谱的金属蛋白酶 (MMP) 抑制剂，具有口服活性。Doxycycline 具有抗菌活性和抗肿瘤活性。
T1687L	Doxycycline (hyclate) Doxycycline hydrochloride hemiethanolate hemihydrate,盐酸强力霉素,WC2031,Doxycycline hyclate	MMP; ribosome; Antibacterial; Antibiotic	Microbiology/Virology; Proteases/Proteasome
	Doxycycline hyclate (WC2031) 属于四环素类抗生素，是一种广谱的金属蛋白酶 (MMP) 抑制剂，具有口服活性。Doxycycline hyclate 具有抗菌活性和抗肿瘤活性。
T3918	Ginsenoside Rb3 人参皂苷 Rb3,Gypenoside IV,人参皂苷Rb3	NF-κB; COX; NO Synthase	Immunology/Inflammation; Neuroscience; NF-κB
	Ginsenoside Rb3 (Gypenoside IV) 是从三七中提取的一种天然产物。它在 293T 细胞系中抑制 TNFα 诱导的NF-κB 转录活性，IC50为 8.2 μM。它还抑制COX-2和iNOSmRNA 的诱导。