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27

抑制剂 & 化合物

4

天然产物

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Cat. No. Product Name Target Signaling Pathways
T8452 Dantrolene

Others Others
Dantrolene 是一种肌肉松弛剂,是人红细胞谷胱甘肽还原酶的非竞争性抑制剂,其Ki 和IC50值分别为 111.6 μM 和 52.3 μM。它是兰尼碱受体拮抗剂及Ca2+信号稳定剂。它可用于研究恶性高热、亨廷顿病、肌肉痉挛和其他神经阻滞剂恶性综合征。
T28073 MLS1547

MLS000051547,MLS 1547,MLS-1547

Dopamine Receptor GPCR/G Protein; Neuroscience
MLS1547 (MLS000051547) 是一种高效的 G 蛋白偏向多巴胺 D2 受体激动剂,Ki 为 1.2 μM。 MLS1547 在钙动员试验中刺激 D2R G 蛋白介导的信号传导,EC50 为 0.37 μM。
T27499 GSK-A1

HCV Protease; PI4K Microbiology/Virology; PI3K/Akt/mTOR signaling; Proteases/Proteasome
GSK-A1 是 III 型磷脂酰肌醇 4-激酶 PI4KA 选择性抑制剂,pIC50为 8.5-9.8,抑制 PtdIns(4,5)P2 再合成,IC50约为 3 nM。GSK-A1有效降低 PtdIns(4)P 的水平,而对 PtdIns(4,5)P2 没影响。GSK-A1在抗丙型肝炎病毒方面有研究的潜力。
T6245 BAPTA-AM

BAPTA/AM

Potassium Channel Membrane transporter/Ion channel
BAPTA-AM 是一种钙离子螯合剂,具有细胞渗透性和选择性,可以阻断 hERG、hKv1.3 和 hKv1.5 通道 (IC50=1.3/1.45/1.23 μM)。BAPTA-AM对 Ca2+的亲和力是 Mg2+的 105 倍,可以用于钙在细胞信号传导中的作用。
T14871 Carboxyamidotriazole Orotate

L-651582 Orotate,CAI Orotate

Calcium Channel Membrane transporter/Ion channel; Metabolism
Carboxyamidotriazole Orotate (L-651582 Orotate) 是一种可口服的信号转导抑制剂,是Carboxyamidotriazole (CAI) 的乳清酸盐形式。它是一种非电压性钙通道和钙通道介导的信号通路的细胞抑制剂,具有抗癌、抗炎活性和抗血管生成作用。
T124384 Jasmonic acid

(-)-Jasmonic acid

Jasmonic acid (JA) 是一种植物激素,也是植物生长调节剂,参与植物迫防御和生长发育。Jasmonic acid 在信号传导过程中起着很重要的作用,诱导 MAP 激酶级联通路和钙通道发挥作用。
T2170 SKF-96365 hydrochloride

1-[2-(4-甲氧基)-2-[3-(4-甲氧基苯基)丙氧基]乙基]咪唑,SKF96365

Apoptosis; Potassium Channel; Calcium Channel; TRP/TRPV Channel; Autophagy Apoptosis; Autophagy; Membrane transporter/Ion channel; Metabolism
SKF-96365 hydrochloride (SKF96365) 是store-operated Ca2+entry 抑制剂,也是TRP channel 阻滞剂。它显著抑制豚鼠离体心脏 hERG、hKCNQ1/hKCNE1、hKir2.1 和 hKv4.3 电流,延长QTc 间期。它通过诱导结直肠癌细胞的细胞周期阻滞和凋亡起抗肿瘤作用。
TP1565L1 Foxy-5 Ammonium Salt

Foxy-5 Ammonium Salt(881188-51-8 Free base)

Wnt/beta-catenin Cytoskeletal Signaling; Stem Cells
Foxy-5 Ammonium Salt是 WNT5A 激动剂,是 WNT5A 的一个模拟肽,是 Wnt 家族的非经典成员。Foxy-5 Ammonium Salt可在不影响 β-catenin 激活的情况下触发胞浆游离钙信号传导,并可抑制上皮癌细胞的迁移和侵袭。Foxy-5 Ammonium Salt在原位小鼠模型中能有效降低 WNT5A 低表达的前列腺癌细胞的转移扩散。
T14872 Carboxyamidotriazole

CAI,L-651582

Calcium Channel Membrane transporter/Ion channel; Metabolism
Carboxyamidotriazole is a cytostatic inhibitor of non-voltage-operated calcium channels and calcium channel-mediated signaling pathways. It shows anti-inflammatory, anti-tumor, and antiangiogenic effects.
T83950 ARN 11391

ARN 11391是ITPR1 (Inositol 1,4,5-trisphosphate (IP3) receptor type 1)的增效剂,它直接作用于ITPR1,从而增强细胞内钙离子信号。ARN 11391还能增强表达突变型ITPR1细胞中的钙信号,这与SCA29型脊髓小脑共济失调有关。
T21387 Nafoxidine HCl(1845-11-0 Free base)

PNU-0011100,PNU0011100,CP5600,CP 5600,CP-5600,PNU 0011100,Nafoxidine HCl

Nafoxidine is a partial estrogen antagonist. It inhibits angiogenesis in some tissues by blocking the effects of VEGF and FGF; paradoxically, it may enhance angiogenesis in uterine tissue. Nafoxidine also induces calcium signaling, oxidative stress, and p
T18989 Fluo-3AM

Fluo-3-pentaacetoxymethyl ester

Others Others
Fluo-3AM is a calcium indicator that exhibits an increase in fluorescence upon binding Ca2+. It is used to image the spatial dynamics of Ca2+ signaling in flow cytometry experiments.
T37803 8-bromo-Cyclic ADP-Ribose (sodium salt)

Cyclic ADP-ribose (cADP-ribose) is a calcium mobilizing nucleotide that is biosynthesized from NAD+ by cADP-ribose synthases, including CD38. cADP-Ribose appears to activate calcium channels in intracellular membranes, which in turn activate ryanodine receptors. 8-bromo-cADP-Ribose is a stable, cell-permeable analog that blocks calcium release evoked by cADP-ribose in sea urchin egg homogenates with an IC50 value of 1.7 μM. It is commonly used to investigate intracellular signaling through cADP-...
T82538 DM-Nitrophen tertasodium

DM-Nitrophen tertasodium是一种Ca2+笼,能在近紫外光照射下分解释放Ca2+,适用于研究Ca2+信号。
T76663 pTH-Related Protein (1-40) (human, mouse, rat)

pTH-Related Protein (1-40) (human, mouse, rat) 促进大鼠肠细胞通过PTHR1受体和PKCα/β信号通路的钙吸收作用。该蛋白增加了甲状旁腺激素1受体(PTHR1)表达,提升了四种跨膜钙转运蛋白—TRPV6、CaBP-D9k、NCX1和PMCA1的水平。
TP1296 Foxy-5 TFA(881188-51-8 free base)

Foxy-5 (TFA)

Foxy-5 is a peptide that mimics the WNT5A protein and is expected to reduce the mobility of the cancer cells. Foxy-5 triggers cytosolic free calcium signaling without affecting β-catenin activation and it impairs the migration and invasion of epithelial c
T36838 (R)-Bromoenol lactone

The phospholipases are an extensive family of lipid hydrolases that function in cell signaling, digestion, membrane remodeling, and as venom components. The calcium-independent phospholipases (iPLA2) are a PLA2 subfamily closely associated with the release of arachidonic acid in response to physiologic stimuli. (R)-Bromoenol lactone ((R)-BEL) is an irreversible, chiral, mechanism-based inhibitor of calcium-independent phospholipase γ (iPLA2γ). Unlike (S)-BEL, (R)-BEL does not inhibit iPLA2β exce...
T35827 Epsilon-V1-2

PKCε Inhibitor Peptide,Protein Kinase Cɛ Inhibitor Peptide,ɛV1-2

Protein kinase C (PKC ) is a calcium-independent, phospholipid- and diacylglycerol-dependent serine/threonine kinase involved in diverse signaling pathways, including those involved in neuronal signaling, cytoskeletal function, and inflammation.[1] PKC inhibitor peptide is a synthetic peptide corresponding to an amino acid sequence found in the amino terminal C2 domain of most mammalian forms of PKC .[2] It selectively and reversibly inhibits the translocation of PKC to intracellular membrane...
T11240 Ethacrynic acid D5

Others Others
Ethacrynic acid, a diuretic, functions as an inhibitor of L-type voltage-dependent and store-operated calcium channels, facilitating the relaxation of airway smooth muscle (ASM) cells. It exhibits anti-inflammatory effects, notably reducing retinoid-induced ear edema in mice, and inhibits glutathione S-transferases (GSTs), making it a potent suppressor of the NF-kB signaling pathway. Additionally, ethacrynic acid modulates leukotriene formation. A variant, Ethacrynic acid D5, is distinguished by...
TP1565L Foxy-5 acetate

Foxy-5 acetate(881188-51-8 free base)

Wnt/beta-catenin Cytoskeletal Signaling; Stem Cells
Foxy-5 acetate 是 Wnt 5A 的激动剂,Wnt 5A 是 Wnt 家族的非经典成员。 Foxy-5 acetate 损害上皮癌细胞的迁移和侵袭,触发细胞溶质游离钙信号传导,而不影响 β-连环蛋白活化。
T37182 AX 048

The group IVA phospholipase A2 (PLA2), known as calcium-dependent cytosolic PLA2 (cPLA2), selectively releases arachidonic acid from membrane phospholipids, playing a central role in initiating the synthesis of prostaglandins and leukotrienes. AX 048 is a potent group IVA cPLA2 inhibitor that demonstrates 50% inhibition of the enzyme at a mole fraction (XI(50)) of 0.022. Pretreatment with AX 048 (ED50 = 1.2 mg/kg) dose-dependently reduces thermal hyperalgesia evoked by carrageenan injection of r...
T70039 BIM-46174

BIM-46174 is a New Inhibitor of the Heterotrimeric Gα/Gβγ Protein Complex. BIM-46174 acts as a selective inhibitor of heterotrimeric G-protein complex. BIM-46174 prevents the heterotrimeric G-protein signaling linked to several GPCRs mediating (a) cyclic AMP generation (Gαs), (b) calcium release (Gαq), and (c) cancer cell invasion by Wnt-2 frizzled receptors and high-affinity neurotensin receptors (Gαo/i and Gαq). BIM-46174 inhibits the growth of a large panel of human cancer cell lines, includ...
T75941 Foxy-5 TFA

Foxy-5 TFA 是WNT5A 激动剂,是 WNT5A 的一个模拟肽,是Wnt 家族的非经典成员。Foxy-5 TFA 可在不影响β-catenin 激活的情况下触发胞浆游离钙信号传导,并可抑制上皮癌细胞的迁移和侵袭。Foxy-5 TFA 在原位小鼠模型中能有效降低 WNT5A 低表达的前列腺癌细胞的转移扩散。
T36367 RK-682 (calcium salt)

Protein tyrosine phosphatases (PTPs) remove phosphate from tyrosine residues of cellular proteins. Reversible phosphorylation catalyzed by the coordinated actions of protein tyrosine kinases and phosphatases is key to the regulation of the signaling events that control cell growth and proliferation, differentiation, and survival or apoptosis, as well as adhesion and motility. RK-682, a bioactive compound originally isolated from the fermentation of Streptomyces sp. 88-682, is an inhibitor of the...
T80240 Ala-parafluoroPhe-Arg-Cha-Cit-Tyr-NH2

Ala-parafluoroPhe-Arg-Cha-Cit-Tyr-NH2是一类具有生物活性的肽,作为蛋白酶激活受体1 (PAR-1) 的选择性激动剂,其特异性优于PAR-2。该肽通过HEK293细胞进行的基于细胞的钙信号传导测定确认了其对PAR-1的高特异性,并可用于研究PAR-1在体内的激活。PAR-1除了介导凝血酶的多种细胞作用外,还与PAR-4协作,参与调控凝血酶诱导的被分类为“凝血型”的肝细胞癌。
T37604 ITK inhibitor

Interleukin-2-inducible T cell kinase (ITK) is a non-receptor tyrosine kinase expressed in T cells, NKT cells and mast cells which plays a crucial role in regulating the T cell receptor (TCR), CD28, CD2, chemokine receptor CXCR4, and FcepsilonR-mediated signaling pathways. ITK inhibitors can be used for the treatment of inflammation and immune-mediated disorders. ITK inhibitor (N-[5-[[3-[(4-Acetylpiperazin-1-yl)carbonyl]-4-methyl-6-methoxy-phenyl]thio]thiazol-2-yl]-4-(N-1,2-dimethylpropylaminome...
T38077 TLQP-21 TFA

TLQP-21 TFA, a VGF-derived peptide endowed of endocrine and extraendocrine properties, is a potent G-protein-coupled receptor complement-3a receptor1 (C3aR1) agonist (EC50: mouse TLQP-21=10.3 μM; human TLQP-21=68.8μM). TLQP-21 TFA activates C3aR1 to induce an increase of intracellular Ca2+. TLQP-21 TFA is used for the research in regulation of nociception and other relevant physiologic functions[1][2]. TLQP-21 TFA is a peptide of 21 amino acids. At a dose of 3 μM TLQP-21 induces up to ~69% of th...

化合物

Dantrolene
Cat.No: T8452
Synonym:
Target: Others
MLS1547
Cat.No: T28073
Synonym: MLS000051547,MLS 1547,MLS-1547
Target: Dopamine Receptor
GSK-A1
Cat.No: T27499
Synonym:
Target: HCV Protease, PI4K
BAPTA-AM
Cat.No: T6245
Synonym: BAPTA/AM
Target: Potassium Channel
Carboxyamidotriazole Orotate
Cat.No: T14871
Synonym: L-651582 Orotate,CAI Orotate
Target: Calcium Channel
Jasmonic acid
Cat.No: T124384
Synonym: (-)-Jasmonic acid
Target:
SKF-96365 hydrochloride
Cat.No: T2170
Synonym: 1-[2-(4-甲氧基)-2-[3-(4-甲氧基苯基)丙氧基]乙基]咪唑,SKF96365
Target: Apoptosis, Potassium Channel, Calcium Channel, TRP/TRPV Channel, Autophagy
Foxy-5 Ammonium Salt
Cat.No: TP1565L1
Synonym: Foxy-5 Ammonium Salt(881188-51-8 Free base)
Target: Wnt/beta-catenin
Carboxyamidotriazole
Cat.No: T14872
Synonym: CAI,L-651582
Target: Calcium Channel
ARN 11391
Cat.No: T83950
Synonym:
Target:
Nafoxidine HCl(1845-11-0 Free base)
Cat.No: T21387
Synonym: PNU-0011100,PNU0011100,CP5600,CP 5600,CP-5600,PNU 0011100,Nafoxidine HCl
Target:
Fluo-3AM
Cat.No: T18989
Synonym: Fluo-3-pentaacetoxymethyl ester
Target: Others
8-bromo-Cyclic ADP-Ribose (sodium salt)
Cat.No: T37803
Synonym:
Target:
DM-Nitrophen tertasodium
Cat.No: T82538
Synonym:
Target:
pTH-Related Protein (1-40) (human, mouse, rat)
Cat.No: T76663
Synonym:
Target:
Foxy-5 TFA(881188-51-8 free base)
Cat.No: TP1296
Synonym: Foxy-5 (TFA)
Target:
(R)-Bromoenol lactone
Cat.No: T36838
Synonym:
Target:
Epsilon-V1-2
Cat.No: T35827
Synonym: PKCε Inhibitor Peptide,Protein Kinase Cɛ Inhibitor Peptide,ɛV1-2
Target:
Ethacrynic acid D5
Cat.No: T11240
Synonym:
Target: Others
Foxy-5 acetate
Cat.No: TP1565L
Synonym: Foxy-5 acetate(881188-51-8 free base)
Target: Wnt/beta-catenin
AX 048
Cat.No: T37182
Synonym:
Target:
BIM-46174
Cat.No: T70039
Synonym:
Target:
Foxy-5 TFA
Cat.No: T75941
Synonym:
Target:
RK-682 (calcium salt)
Cat.No: T36367
Synonym:
Target:
Ala-parafluoroPhe-Arg-Cha-Cit-Tyr-NH2
Cat.No: T80240
Synonym:
Target:
ITK inhibitor
Cat.No: T37604
Synonym:
Target:
TLQP-21 TFA
Cat.No: T38077
Synonym:
Target:
Cat. No. Product Name Target Signaling Pathways
T5120 Rhamnose

6-Deoxyhexopyranose,L-鼠李糖,6-Deoxy-L-mannose,alpha-L-Rhamnose

Calcium Channel; Endogenous Metabolite Membrane transporter/Ion channel; Metabolism
alpha-L-Rhamnose (6-Deoxy-L-mannose) 是存在植物和细菌中的一种单糖。Rhamnose- 免疫原连接物能被用于免疫疗法。Rhamnose 能通过胞外途径穿过上皮细胞,能够作为肠吸收的标志。
T3929 Kaurenoic acid

Kauren-19-Oic Acid,异贝壳杉烯酸,kaurenoate,kaur-16-en-18-oic acid

Others Others
Kaurenoic acid (kaurenoate) 是一种二萜,来源于 Sphagneticola trilobata 中,可以抑制细胞因子的产生和激活 NO–cyclic GMP–PKG–ATP- 敏感型钾通道信号通路,并抑制炎症疼痛。
T11363 Ganoderic acid F

Others Others
Ganoderic acid F 是一种灵芝酸。它具有抗肿瘤和抗转移的活性,与抑制血管生成和涉及细胞增殖和细胞死亡,致癌作用,氧化应激,钙信号传导和内质网应激的蛋白质改变等机制相关。
T79932 Eudebeiolide B

Plebeiolide D

NF-κB NF-κB
Eudebeiolide B,一种自荔枝草分离得的化合物,能通过调控RANKL诱导的NF-κB、c-Fos及钙信号来抑制破骨细胞的生成,适用于研究与破骨细胞相关的疾病。

天然产物

Rhamnose
Cat.No: T5120
Synonym: 6-Deoxyhexopyranose,L-鼠李糖,6-Deoxy-L-mannose,alpha-L-Rhamnose
Target: Calcium Channel, Endogenous Metabolite
Kaurenoic acid
Cat.No: T3929
Synonym: Kauren-19-Oic Acid,异贝壳杉烯酸,kaurenoate,kaur-16-en-18-oic acid
Target: Others
Ganoderic acid F
Cat.No: T11363
Synonym:
Target: Others
Eudebeiolide B
Cat.No: T79932
Synonym: Plebeiolide D
Target: NF-κB
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