T83963
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Z-DEVD-FMK Caspase-3 Inhibitor 是一种可渗透细胞膜的、不可逆的 caspase-3/CPP32 抑制剂,能够抑制肿瘤细胞的凋亡。在动物体内,它在大鼠发作后的海马区具有神经保护作用,且显著减少创伤后的细胞凋亡,并在诱发的大鼠创伤性脑损伤之前和之后改善神经学恢复情况。 |
T72460
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Dimethyl L-glutamate (Dimethyl glutamate), 一种可透膜的谷氨酸类似物,可刺激葡萄糖诱导的胰岛素 (insulin) 释放。Dimethyl L-glutamate 抑制KATP 通道的活性。Dimethyl L-glutamate 抑制E. gracilis 生长并导致细胞异常分裂。Dimethyl L-glutamate 可用于糖尿病、葡萄糖转运、磷酸化和进一步代谢的研究。 |
T35474
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Degrader of MTH1 fusion proteins for use within the aTAG system. Comprises a ligand selective for MTH1, a linker and the cereblon-binding ligand Thalidomide . Induces highly potent and selective degradation of fusion proteins after a 4 h incubation (DC50 = 0.27 nM; Dmax = 92.1%). Cell-permeable. Suitable for in vitro and in vivo applications. Mouse DMPK properties are provided in the supplementary file (see below). (MTH1 can be expressed as a fusion with a target protein of interest using genome engineering techniques via CRISPR-mediated locus-specific knock-in - see protocol for more information.)
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T35475
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Degrader of MTH1 fusion proteins for use within the aTAG system. Comprises a ligand selective for MTH1, a linker and the cereblon-binding ligand Thalidomide . Induces highly potent and selective degradation of fusion proteins after a 4 h incubation (DC50 = 0.34 nM; Dmax = 93.14%). Cell-permeable. Suitable for in vitro and in vivo applications. Mouse DMPK properties are provided in the supplementary file (see below). (MTH1 can be expressed as a fusion with a target protein of interest using genome engineering techniques via CRISPR-mediated locus-specific knock-in - see protocol for more information.)
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T36871
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In addition to its role in the Krebs cycle, α-ketoglutarate (2-oxoglutarate) has roles as a substrate or modulator of enzymes. 5-Octyl-α-ketoglutarate, also known as α-ketoglutarate octyl ester, is a stable, cell-permeable molecule that generates free α-ketoglutarate upon hydrolysis of the ester bond by cytoplasmic esterases. It is used in experiments to increase levels of intracellular α-ketoglutarate. 5-Octyl-α-ketoglutarate has been shown to modulate a variety of enzymes and signaling pathways, particularly in the context of glycolysis, hypoxia, and cancer. |
T36322
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C8 D-threo Ceramide is a bioactive sphingolipid and cell-permeable analog of naturally occurring ceramides. It is cytotoxic to U937 cells (IC50 = 17 μM) and induces nuclear DNA fragmentation 5- to 6-fold more potently than C8 ceramide . C8 D-threo Ceramide is a substrate for E. coli diacylglycerol kinase. It activates ceramide-activated protein kinase (CAPK) in U937 cells. C8 D-threo Ceramide also enhances V. cholerae cytolysin pore formation in liposome lipid membranes, as measured by calcein release, with a 50% release dose (RD50) value of ~5 μg/ml. |
T73445
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TIM-063 是一种选择性和细胞可渗透的CaMKK 抑制剂,ATP 竞争性抑制剂,可以直接靶向 CaMKK 的催化结构域,作用于 CaMKKα 和CaMKKβ 的Ki 值分别是 0.35 μM 和 0.2 μM,IC50值分别是 0.63 μM 和 0.96 μM。 |
T75937
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Pep2m, myristoylated TFA (Myr-Pep2m TFA)为具备细胞渗透性的肽。该化合物通过破坏PKMζ与其下游靶点NSF/GluR2的相互作用而发挥作用,其中PKMζ为具有自主活性的PKC同工酶。 |
T36677
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Rp-8-bromo-Cyclic AMPS (Rp-8-bromo-cAMPS) is a cell-permeable cAMP analog that combines an exocyclic sulfur substitution in the equatorial position of the cyclophosphate ring with a bromine substitution in the adenine base of cAMP. It acts as an antagonist of cAMP-dependent protein kinases (PKAs) and is resistant to hydrolysis by cyclic nucleotide phosphodiesterases. Rp-8-bromo-cAMPS more effectively antagonizes cAMP-dependent activation of purified PKA type I from rabbit muscle than PKA type II from bovine heart. |
T83293
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5-CFDA-AM作为一种细胞渗透性的酯酶底物,用于测定酶活性和细胞膜完整性,该化合物为电子中性,其渗透细胞的能力超过CFDA且所需浓度更低。在细胞内部,5-CFDA-AM经酯酶水解生成羧基荧光素,后者带有额外负电荷,因此能更有效地在细胞内保留。 |