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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
T75372	BODIPY FL Thapsigargin
	BODIPY FL Thapsigargin 作为一种高效绿色荧光染料，主要抑制细胞内肌浆/内质网中的serca型Ca2+泵。其应用焦点在于探究Thapsigargin在活细胞中的结合位置。储存需避光处理。
T16688	Pyr6 N-[4-[3,5-Bis(trifluoromethyl)-1H-pyrazol-1-yl]phenyl]-3-fluoro-4-pyridinecarboxamide	TRP/TRPV Channel	Membrane transporter/Ion channel
	Pyr6 (N-[4-[3,5-Bis(trifluoromethyl)-1H-pyrazol-1-yl]phenyl]-3-fluoro-4-pyridinecarboxamide)是选择性的 TRPC3抑制剂，IC50值为0.49uM。
T69175	Trilobolide
	Trilobolide is a natural counterpart of thapsigargin and an activator of cytokine secretion.
T72004	Azumolene sodium anhydrous
	Azumolene sodium anhydrous is a muscle relaxant that inhibits the release of calcium from skeletal muscle sarcoplasmic reticulum. Azumolene inhibits a component of store-operated calcium entry coupled to the skeletal muscle ryanodine receptor. Azumolene, an equipotent dantrolene analog, inhibits a component of SOCE coupled to activation of RyR1 by caffeine and ryanodine, whereas the SOCE component induced by thapsigargin is not affected.
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。
T35622	FKGK 18
	FKGK 18 is an inhibitor of group VIA (GVIA) calcium-independent phospholipase A2 (iPLA2). It inhibits GVIA iPLA2 by 99.9% at 0.091 mole fraction in a mixed micelle activity assay and is selective for GVIA iPLA2 over GIVA cPLA2 and GV sPLA2 where it shows 80.8 and 36.8% inhibition, respectively. FKGK 18 inhibits iPLA2β activity in cytosolic extracts from INS-1 cells overexpressing iPLA2β (IC50 = ~50 nM) as well as iPLA2γ activity in mouse heart membrane fractions (IC50s = ~1-3 μM). It inhibits gl...

化合物

BODIPY FL Thapsigargin

Synonym: N-[4-[3,5-Bis(trifluoromethyl)-1H-pyrazol-1-yl]phenyl]-3-fluoro-4-pyridinecarboxamide

Target: TRP/TRPV Channel

Azumolene sodium anhydrous

Cat.No: T72004

Synonym:

Target:

Soluble Epoxide Hydrolase PROTAC 1a

Cat.No: T83857

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

Cat. No.	Product Name	Target	Signaling Pathways
TQ0302	Thapsigargin 毒胡萝卜素	Apoptosis; SARS-CoV; Calcium Channel	Apoptosis; Membrane transporter/Ion channel; Metabolism; Microbiology/Virology
	Thapsigargin 属于天然产物，是一种肌/内质网 Ca2+ ATP 酶 (SERCA) 的抑制剂，也是一种内质网应激诱导剂。Thapsigargin 通过阻断细胞将钙泵入肌浆和内质网的能力来提高胞浆钙浓度。