目录号 | 产品详情 | 靶点 | |
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TP1903 | |||
Competitive inhibitor of cGMP-dependent protein kinase (PKG); analog of a substrate peptide corresponding to a phosphorylation site of histone H2B. Competes with synthetic substrates (Ki = 86 mM) but does not inhibit phosphorylation of intact histones by | |||
T73708 | |||
Sp-cAMPS triethylamine,一种 cAMP 类似物,是一种依赖 cAMP 的PKAI 和PKAII 的有效激活剂。Sp-cAMPS triethylamine 还是一种有效的竞争性磷酸二酯酶 (PDE3A) 抑制剂,Ki 为 47.6 µM。Sp-cAMPS triethylamine 以EC50为 40 μM 来结合PDE10GAF 域。 | |||
T22014 | |||
8-CPT-2Me-cAMP sodium is a sodium salt compound that selectively activates exchange proteins activated by cAMP (Epac). These Epac proteins are cAMP-sensitive guanine nucleotide exchange factors (GEFs) responsible for activating small GTPases Rap1 and Rap2. 8-CPT-2Me-cAMP sodium specifically activates Epac1 with an EC50 value of 2.2 μM, while showing no activation of PKA with an EC50 value greater than 10 μM [1]. Additionally, 8-CPT-2Me-cAMP sodium stimulates the Epac-mediated release of calcium ions (Ca2+) in vitro in pancreatic β-cells [2]. | |||
T60924 | ROCK | ||
Verosudil (AR-12286) 是一种高效的 Rho 激酶 (ROCK) 抑制剂,对 ROCK1 和 ROCK2 的 Ki 分别为 2 和 2 nM。AR-12286 可逆转类固醇诱导的小鼠眼内压,可通过增加眼房水通过小梁网流出来减缓眼压。 | |||
T83683 | |||
st-Ht31是一种由A-kinase锚定蛋白(AKAPs)的两亲螺旋域衍生的、可穿透细胞的硬脂化肽,它能够结合蛋白激酶A (PKA)。在使用50 µM浓度时,能降低PKA在细胞膜上的锚定,但不影响其在使用BHK-21成纤维细胞进行的报告基因分析中的活性。st-Ht31 (1和3 µM)能减少小鼠精子的电容和超活化,同时阻止体外受精。当使用50 µM浓度时,它还能促进表达ATP结合盒转运蛋白1 (ABCA1)的BHK-21细胞和RAW 264.7巨噬细胞中的胆固醇排出。 | |||
T76127 | |||
Urocortin II, mouse 是一种选择性的 2 型促肾上腺皮质激素释放因子 (CRF2) 受体内源性多肽激动剂,对CRFR2和CRFR1的Ki 值分别为 0.66 nM 和 ﹥100 nM。Urocortin II, mouse 通过以 cAMP/PKA 和 Ca2+/CaMKII 依赖性方式激活 CRF2 受体。Urocortin II, mouse 在中枢神经系统的离散区域表达,并激活参与内脏感觉信息处理和调节自主神经外流的中枢神经元。 | |||
T32876 | |||
Loquatoside belongs to the class of organic compounds known as flavonoid-3-o-glycosides. These are phenolic compounds containing a flavonoid moiety which is O-glycosidically linked to carbohydrate moiety at the C3-position. Loquatoside exists as a solid, | |||
T1920 | Akt PKA mTOR Autophagy | ||
Capivasertib (AZD5363) 是一种广谱的 AKT 抑制剂,对 Akt1、Akt2 和 Akt3 均有抑制活性 (IC50=3/7/7 nM),具有口服活性。Capivasertib 具有抗肿瘤活性,可以用于治疗乳腺癌。 | |||
T34180 | |||
Psilostachyin c is a member of the class of compounds known as ambrosanolides and secoambrosanolides. Ambrosanolides and secoambrosanolides are sesquiterpene lactones from the Ambrosia family, with a backbone derivative of azuleno[6,5-b]furan-2-one (ambro | |||
T21705 | |||
8-CPT-Cyclic AMP (8-CPT-cAMP) sodium 是环 AMP 依赖性蛋白激酶的选择性激活剂。 8-CPT-Cyclic AMP sodium 也是有效的环 GMP 特异性磷酸二酯酶(PDE VA)抑制剂,IC50为 0.9 μM。 8-CPT-Cyclic AMP sodium 还抑制 PDE III 和 PDE IV,IC50分别为 24 和 25 μM。8-CPT-Cyclic AMP sodium 对 Epac 具有非常高的亲和力,是一种有效的Epac 活化剂。 |
目录号 | 产品名/同用名 | 种属 | 表达系统 | ||
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TMPK-00677 | PKA/PRKACA Protein, Canine, Recombinant (His) | Canine | E. coli | ||
The cAMP-dependent protein kinase PKA is a well-characterized member of the serine-threonine protein AGC kinase family and is the effector kinase of cAMP signaling. As such, PKA is involved in the control of a wide variety of cellular processes including metabolism, cell growth, gene expression and apoptosis. cAMP-dependent PKA signaling pathways play important roles during infection and virulence of various pathogens. Since fluxes in cAMP are involved in multiple intracellular functions, a variety of different pathological infectious processes can be affected by PKA signaling pathways.
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TMPJ-01309 | PKI-Beta Protein, Human, Recombinant (His) | Human | E. coli | ||
cAMP-Dependent Protein Kinase Inhibitor β (PKI-β) is a member of the PKI family. As a member of the cAMP-dependent protein kinase inhibitor family,It has been shown that PKI-β is an extremely potent competitive inhibitor of cAMP-dependent protein kinase activity; this protein interacts with the catalytic subunit of the enzyme after the cAMP-induced dissociation of its regulatory chains. It may play a role in the protein kinase A (PKA) pathway by interacting with the catalytic subunit of PKA, and overexpression of this gene may play a role in prostate cancer.
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TMPJ-00528 | PPP1R1A Protein, Human, Recombinant (His) | Human | E. coli | ||
Protein Phosphatase 1 Regulatory Subunit 1A (PPP1R1A) is an inhibitor of protein-phosphatase 1. PPP1R1A is a cellular regulator of eIF2 alpha phosphorylation. In hormonal control of glycogen metabolism, IPP-1 protein plays important function. Hormones can elevate intracellular cAMP level and elevate IPP-1 activity. PPP1R1A activation caused cAMP increase , cAMP control over proteins that are not directly phosphorylated by PKA following a rise in intracellular calcium. IPP-1 is inactivated by calcineurin (PP2B). Multiple domains in IPP-1 target cellular PP1 complexes.
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TMPH-00028 | Adeno-associated virus 2 (isolate Srivastava/1982) Rep78 Protein (His & MBP) | AAV-2 | E. coli | ||
Plays an essential role in the initiation of viral DNA synthesis. Binds specifically to an inverted terminal repeat element (ITR) on the 3' and 5' ends of the viral DNA, where it cleaves a site specifically to generate a priming site for initiation of the synthesis of a complementary strand. Plays also a role as transcriptional regulator, DNA helicase and as key factors in site-specific integration of the viral genome. Regulates host PKA activity by interacting with host PRKX as a mechanism of interfering with helper virus propagation and promoting its own replication. Inhibits the host cell cycle G1/S, S and G2/M transitions. These arrests may provide essential cellular factors for viral DNA replication.
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TMPY-01117 | MRAP Protein, Human, Recombinant (hFc) | Human | HEK293 Cells | ||
MRAP (Melanocortin 2 Receptor Accessory Protein) is a Protein Coding gene. This gene encodes a melanocortin receptor-interacting protein. It belongs to the MRAP family. MRAP, which contains a single transmembrane domain, has a unique structure, an antiparallel homodimer. MRAP is a single transmembrane domain accessory protein and a critical component of the hypothamo pituitary-adrenal axis. MRAP is highly expressed in the adrenal gland and is essential for adrenocorticotropin hormone (ACTH) receptor expression and function. In adrenal cells, MRAP is essential for adrenocorticotropic hormone (ACTH)-induced activation of the cAMP/protein kinase A (PKA) pathway by melanocortin 2 receptor (MC2R), leading to glucocorticoid production and secretion. Diseases associated with MRAP include Glucocorticoid Deficiency 2 and Glucocorticoid Deficiency 1.
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TMPJ-00886 | ATF1 Protein, Human, Recombinant (His) | Human | E. coli | ||
Cyclic AMP-dependent transcription factor ATF-1(ATF1) which contains 1 bZIP (basic-leucine zipper) domain and 1 KID (kinase-inducible) domain, belongs to the bZIP family. It influences cellular physiologic processes by regulating the expression of downstream target genes, which are related to growth, survival, and other cellular activities. ATF1 binds the cAMP response element (CRE) (consensus: 5'-GTGACGT[AC][AG]-3'), a sequence present in many viral and cellular promoters. It also binds to the Tax-responsive element (TRE) of HTLV-I. ATF1 mediates PKA-induced stimulation of CRE-reporter genes, represses the expression of FTH1 and other antioxidant detoxification genes, triggers cell proliferation and transformation. ATF1 is phosphorylated at serine 63 in its kinase-inducible domain by serine/threonine kinases, cAMP-dependent protein kinase A, calmodulin-dependent protein kinase I/II, mitogen- and stress-activated protein kinase and CDK3. Its phosphorylation enhances its transactivation and transcriptional activities, and enhances cell transformation.
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