18
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Cat. No. | Product Name | Target | Signaling Pathways |
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T15485 |
HJC0197
|
cAMP; Ras | GPCR/G Protein; MAPK |
HJC0197 是Epac1(cAMP 1 直接激活的交换蛋白) 和Epac2 拮抗剂,其对Epac2 的IC50值为5.9 μM。它在等浓度 cAMP 存在下能够降低 Epac1 介导的 Rap1-GDP 交换活性。它能够选择性阻断 cAMP 诱导的 Epac 活化。 | |||
T40279 |
GLP-1R modulator L7-028
GLP-1R modulator L7-028 |
cAMP; Glucagon Receptor | GPCR/G Protein |
GLP-1R modulator L7-028 是一种变构调节剂,增强了对 GLP-1 的亲和力和 cAMP 信号转导。 | |||
T11662L |
INT-777
S-EMCA |
GPCR19 | GPCR/G Protein |
INT-777(S-EMCA)是有效的 TGR5 激动剂,EC50 为 0.82 μM。 INT-777(S-EMCA)在大鼠蛛网膜下腔出血后通过 TGR3/cAMP/PKA 信号通路抑制 NLRP5-ASC 炎症小体介导的神经炎症。 | |||
T50023 |
ethyl 1-(4-aminophenyl)-5-(trifluoromethyl)-1H-pyrazole-4-carboxylate
|
Others | Others |
ethyl 1-(4-aminophenyl)-5-(trifluoromethyl)-1H-pyrazole-4-carboxylate 又称 EAPT,是一种有效的选择性 PDE4抑制剂,调节细胞内环腺苷酸(cAMP)水平。它已被用于多种科研应用,包括 cAMP 介导的信号转导通路的研究,并有潜力作为治疗炎症和免疫相关疾病的药物。 | |||
T1024 |
Roflumilast
罗氟司特,B9302-107,BYK 20869,APTA 2217,BY 217 |
PDE; RSV | Metabolism; Microbiology/Virology |
Roflumilast (APTA 2217) 是一种口服的长效 4 型磷酸二酯酶抑制剂 (PDE4),具有抗炎和潜在的抗肿瘤活性,作用于PDE4A1,PDEA4,PDEB1和PDEB2,IC50分别为 0.7,0.9,0.7 和 0.2 nM。 | |||
T22529 |
6-Bnz-cAMP sodium salt
|
Others | Others |
6-Bnz-cAMP is a PKA-selective activator. It regulates the PKA dependent signaling pathways. The proliferative signaling pathway which activated by the 6-Bnz-cAMP involves activation of the epidermal growth factor receptor and ERK1/2. Extending the duratio | |||
T68650 | AH 23848 | ||
AH 23848 is a Thromboxane antagonist which accelerates inducible nitric oxide synthase degradation through attenuation of cAMP signaling in glomerular mesangial cells. | |||
T30808 |
CG500354
CG-500354,CG 500354 |
||
CG500354 plays a tumor suppressive role through the cAMP/CREB signaling pathway and is a novel inducer of neural differentiation and growth arrest in primary HUMAN GBM derived cells. | |||
TP1283 |
VIP(6-28)(human, rat, porcine, bovine)
|
||
VIP(6-28)(human, rat, porcine, bovine) is a potent antagonist that effectively counteracts the effects of exogenous vasoactive intestinal peptide (VIP) on cyclic adenosine monophosphate (cAMP) signaling. | |||
T28891 |
SW106
|
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SW106 is a selective antagonist of PTHR1-mediated cAMP signaling, not functioning as an inverse agonist on either PTHR1-T410P or PTHR1-H223R, which have activating mutations at the cytoplasmic ends of TMD helices-2 and -6, respectively. | |||
T37477 |
L-858,051 (hydrochloride)
|
||
L-858,051 is a water-soluble analog of forskolin , a cell-permeant activator of adenylate cyclase. L-858,051 activates adenylate cyclase (EC50 = 3 μM), inhibits glucose transport, and blocks cytochalasin B binding in rat adipocyte membranes. L-858,051 is used to activate adenylate cyclase and initiate signaling through elevated cAMP synthesis in a variety of cell types in culture. | |||
T73690 |
Abaloparatide
|
||
Abaloparatide (BA 058) 是一种甲状旁腺激素受体 1 (PTHR1) 类似物。Abaloparatide 也是一种选择性 PTHR1激活剂。Abaloparatide 增强 Gs/cAMP 信号和β-arrestin 募集。Abaloparatide 可增强小鼠的骨形成和皮质结构。Abaloparatide 具有用于骨质疏松症研究的潜力。 | |||
T36072 |
Skyrin
Endothianin,Rhodophyscin |
||
Skyrin is a fungal metabolite characterized by a bisanthraquinone structure. It interferes with glucagon signaling through adenylate cyclase without binding to the glucagon receptor. At 10 μM, skyrin reduces both glucagon-stimulated cAMP production and glycogenolysis. It does not interfere with epinephrine or glucagon-like peptide 1 effects on these parameters.[1] Reference:[1]. Parker, J.C., McPherson, R.K., Andrews, K.M., et al. Effects of skyrin, a receptor-selective glucagon antagonist, in r... | |||
T82989 |
AP-C6
|
||
AP-C6 是一种有效的 cGMP 依赖性蛋白激酶 II (cGKII) 抑制剂,其 pIC50 值为 6.5。该化合物能够在体外浓度依赖性地抑制人 cGKII 的活性,并能够通过抑制 PDE 来增强 cAMP 信号传导。 | |||
T37896 |
AZ 1729
|
||
FFA2 allosteric agonist. Inhibits forskolin-induced cAMP increase and stimulates 35SGTPγS binding in biochemical assays (pEC50 values are 6.9 and 7.23, respectively). Binds at allosteric binding site. In functional assays, displays positive allosteric modulation of FFA-induced Gi signaling and negative allosteric modulation of FFA-induced Gq/G11 signaling. Inhibits lipolytic effect of isoproterenol (pEC50 = 5.03) and induces migration of human neutrophils in vitro. Bolognini et al (2016) A novel... | |||
T36781 |
st-Ht31 P
st-Ht31 P |
||
Negative control for st-Ht31 . Gorshkov et al (2017) AKAP-mediated feedback control of cAMP gradients in developing hippocampal neurons. Nat.Chem.Biol. 13 425 PMID:28192412 |Vijayaraghavan et al (1997) Protein kinase A-anchoring inhibitor peptides arrest mammalian sperm motility. J.Biol.Chem. 272 4747 PMID:9030527 |Vincent et al (2017) Signaling: Spatial regulation of axonal cAMP. Nat.Chem.Biol. 13 348 PMID:28328917 | |||
T61617 | Hcyb1 | ||
Hcyb1 is a potent and specific inhibitor of phosphodiesterase 2 (PDE2). It exhibits a high degree of selectivity for inhibiting PDE2A with an IC50 value of 0.57 μM. In addition, Hcyb1 displays over 250-fold selectivity against other recombinant members of the PDE family. Moreover, its pharmacological actions include neuroprotective and antidepressant-like effects, which are believed to be mediated through the cAMP/cGMP-CREB-BDNF signaling pathway [1]. | |||
T65994 |
(6S)-N-Benzyl-6-(4-hydroxybenzyl)-8-(naphthalen-1-ylmethyl)-4,7-dioxohexahydro-2H-pyrazino[1,2-a]pyrimidine-1(6H)-carboxamide
|
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Wnt signaling is required for direct multiple biological processes and also plays key roles in the pathogenesis of various diseases. Cyclic AMP response element-binding protein (CREB) is a transcription factor that is a member of the leucine zipper family of DNA binding proteins. This protein binds as a homodimer to the cAMP-responsive element, an octameric palindrome. The protein is phosphorylated by several protein kinases, and induces transcription of genes in response to hormonal stimulation... |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T3826 |
Polygalasaponin F
异牡荆苷,瓜子金皂苷己 |
NF-κB; TLR; Akt; PI3K | Cytoskeletal Signaling; Immunology/Inflammation; NF-κB; PI3K/Akt/mTOR signaling |
Polygalasaponin F 是从瓜子金中提取的齐墩果烷型三萜皂苷,可通过调节TLR4-PI3K/AKT-NF-kB 信号通路减少神经炎症细胞因子的分泌,能降低炎性细胞因子肿瘤坏死因子 α 的释放。 | |||
T13762 |
Luteolin 7-sulfate
|
Others | Others |
Luteolin 7-sulfate, derived from the marine plant Phyllospadix iwatensis Makino, suppresses TYR gene expression by intervening in a signaling pathway involving the cAMP-responsive element binding protein (CREB) and microphthalmia-associated transcription factor (MITF). This inhibition ultimately leads to a decrease in melanin synthesis. | |||
TN2039 | Panaxydol | cAMP; p38 MAPK; JNK | GPCR/G Protein; MAPK |
Panaxydol has anti-cancer activity, can inhibit the growth and apoptosis of cancer cells, the signaling mechanisms involve a [Ca(2+)](i) increase, JNK and p38 MAPK activation, cAMP, MAP kinase and ROS generation through NADPH oxidase and mitochondria. | |||
TMA0003 | Trans-caffeic acid | cAMP; Tyrosinase | GPCR/G Protein; Proteases/Proteasome |
Trans-caffeic acid stearyl ester is posited to inhibit melanogenesis signaling while suppressing cAMP levels and, subsequently, MC1R, MITF, tyrosinase, TRP-2 and TRP-1 down-regulation, resulting in the suppression of tyrosinase activity, DOPA oxidase activity and melanin synthesis. | |||
TN1694 |
Gliotoxin
|
Apoptosis; NF-κB; Wnt/beta-catenin; COX; PKA; Antibacterial; Antifection | Apoptosis; Cytoskeletal Signaling; Immunology/Inflammation; Microbiology/Virology; Neuroscience; NF-κB; Stem Cells; Tyrosine Kinase/Adaptors |
Gliotoxin 是一种次生代谢产物,由A. fumigatus 分泌,可以抑制巨噬细胞的吞噬作用和其他免疫细胞的免疫功能。它通过阻止 IκB 降解来抑制诱导型NF-κB 活性,从而诱导宿主细胞凋亡。它可以激活PKA 并增加细胞内 cAMP 浓度,调节肌动蛋白细胞骨架重排以促进A. fumigatus 内化到肺上皮细胞。 |