TP2116
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KRas/son of sevenless 1 (SOS1) interaction inhibitor. Binds within nucleotide binding pocket of KRas (Kd values are 106 - 176 nM for wild type KRas and various KRas mutants). Inhibits nucleotide binding to KRas in a concentration dependent manner. Display |
T76060
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NLS-StAx-h TFA 是选择性的、细胞可渗透的Wnt 信号传导的固定肽抑制剂,IC50为 1.4 μM。NLS-StAx-h TFA 可有效抑制 β-catenin-转录因子的相互作用,具有对癌细胞的抗增殖活性。 |
T37565
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C6 D-threo Ceramide is a bioactive sphingolipid and cell-permeable analog of naturally occurring ceramides., C6 D-threo Ceramide is cytotoxic to U937 cells in vitro (IC50 = 18 μM). It is metabolically inactive and, unlike C6 L-erythro ceramide , C6 D-threo ceramide cannot be converted to C6 glucosylceramide by ceramide glucosyltransferase. C6 D-threo Ceramide promotes survival of isolated rat spinal neurons when used at concentrations up to 2.5 μM but induces cell death at concentrations greater than 5 μM. It enhances IL-4 production induced by phorbol 12-myristate 13-acetate in EL4 T cells when used at a concentration of 10 μM. |
T35927
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C2 L-threo Ceramide is a bioactive sphingolipid and cell-permeable analog of naturally occurring ceramides. It stimulates cholesterol efflux in CHO cells expressing the human ABCA1 receptor when used at a concentration of 10 μM, however, this efflux is 50% less than that stimulated by C2 ceramide . C2 L-threo Ceramide inhibits IL-4 production by 17% in EL4 T cells stimulated with phorbol 12-myristate 13-acetate when used at a concentration of 10 μM. It also induces cell cycle arrest in the G0/G1 phase and a 7-fold increase in sphingosine accumulation as well as inhibits growth of HL-60 leukemia cells. |
T21681
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Phospholipase
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AACOCF3 (Arachidonyl trifluoromethyl ketone) is a cell-permeable trifluoromethyl ketone analog of arachidonic acid. It is a potent and selective slow binding inhibitor of the 85-kDa cytosolic phospholipase A2 (cPLA2). By blocking the production of arachidonate and 12-hydroxyeicosatetraenoic acid in calcium ionophore-challenged platelets, AACOCF3 hinders their synthesis. Moreover, AACOCF3 inhibits glucose-induced insulin secretion from isolated rat islets. Given its diverse applications, AACOCF3 holds promise for cardiovascular disease research. |
T82388
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Caspase
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Fluorescein-6-carbonyl-Asp(OMe)-Glu(OMe)-Val-DL-Asp(OMe)-fluoromethylketone 是一种细胞渗透性且无毒的抑制剂,它能与活化的caspase-3在凋亡细胞内不可逆结合。该抑制剂的荧光强度可通过流式细胞仪、微孔板读数器或荧光显微镜检测。 |
T83469
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10m/ZS44是一种能够穿透血脑屏障的Glioblastoma (GBM) 抑制剂,在小鼠异种移植模型中有效抑制了GBM肿瘤生长,并通过激活SIRT1/p53介导的细胞凋亡途径来抑制U251细胞增殖。 |
T63799
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GID4 Ligand 1 是细胞渗透性的、高度选择性的 GID4 结合剂,其 IC50 值为 5.4 μM,Kd 值为 5.6 μM。GID4 Ligand 1 在细胞中能够结合 GID4,其 EC50 值为 558 nM。GID4 Ligand 1 能够用于 PROTACs 的合成。 |
T37188
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BTC AM is a cell-permeable acetoxy-methyl ester of BTC . As BTC AM enters cells, it is hydrolyzed by intracellular esterases to produce BTC. BTC is a low affinity calcium indicator (Kd = 7-26 μM) that displays excitation/emission spectra of 401/529 nm, respectively. It exhibits a shift in the excitation maximum from approximately 480 to 401 nm upon calcium binding, enabling determination of ratiometric calcium measurements. BTC is suitable for detecting elevated calcium levels associated with activation of smooth muscle, neurons, and intracellular calcium stores. |
T76249L
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RNAENFDRF (βIIPKC624-632) TFA 与细胞渗透性肽 TAT47-57 结合,可用于形成抑制性肽 SAMβA。SAMβA 是一种 Mfn1-βIIPKC 结合选择性拮抗剂。SAMβA 是 mitofusin 1-βIIPKC 关联的选择性抑制剂,可改善大鼠心力衰竭。 |