目录号 | 产品详情 | 靶点 | |
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T13134 | Monoamine Transporter | ||
(+)-Tetrabenazine ((3R,11bR)-Tetrabenazine) 是一种可逆的囊泡单胺转运蛋白2 (VMAT-2)抑制剂,对 VMAT2转运的抑制作用是VMAT1的10倍。 | |||
T18922 | Others | ||
BCECF is a fluorescent probe commonly used to measure pH. It is a dual-excitation ratiometric pH indicator with a pKa of ~6.98. Measurements of pH are made by determining the ratio of emission intensity, detected at 535 nm when excited at 490 nm versus th | |||
T70431 | |||
TX-1123是一种针对Src、eEF2-K、PKA和EGFR-K/PKC的有效蛋白酪氨酸激酶(PTK)抑制剂,同时也是一种环氧合酶(COX)抑制剂,对COX2和COX1的IC50值分别为1.16μM和15.7μM。它具有低线粒体毒性,可用于癌症研究。 | |||
T78066 | Calcium Channel | ||
BBT是一种增强剂,用于改善受损的葡萄糖刺激胰岛素分泌(GSIS)。该化合物展现出抗高血糖的活性,并能在2型糖尿病模型中,对β细胞起到保护作用,抵御细胞因子或链脲佐菌素(STZ)引起的细胞死亡。BBT的作用机制涉及通过cAMP/PKA及持久(L型)电压依赖性Ca2+通道/CaMK2通路。 | |||
T61382 | |||
Fasudil dihydrochloride, also known as HA-1077 and AT877, is a nonspecific inhibitor of RhoA/ROCK. It exhibits inhibitory effects on protein kinases, including ROCK1 with a Ki value of 0.33 μM, as well as ROCK2, PKA, PKC, and PKG with IC 50 values of 0.158 μM, 4.58 μM, 12.30 μM, and 1.650 μM, respectively. Additionally, Fasudil dihydrochloride demonstrates potent Ca 2+ channel blocking activity and acts as a vasodilator [1] [2] [3]. | |||
T69895 | |||
Lonaprisan is an orally bioavailable pentafluoroethyl derivative of a mifepristone-related steroid with antiprogestagenic activity. Lonaprisan is a pure, highly receptor-selective progesterone receptor (PR) antagonist; binding of this agent to PRs inhibits PR activation and the associated proliferative effects. Unlike many other antiprogestins such as mifepristone, this agent does not appear to convert to an agonist in the presence of protein kinase A (PKA) activators and shows high antiprogestagenic activity on both progesterone receptor (PR) isoforms PR-A and PR-B. | |||
TD0048 | |||
The cell-permeant pH indicator, carboxy SNARF-1, acetoxymethyl ester, acetate (CAS #126208-13-7) has a pKa of ~7.5 after de-esterification, thus is useful for measuring pH changes between pH 7 and pH 8. Carboxy-SNARF-1 exhibits a significant pH-dependent | |||
T32329 | |||
Juzirine is a member of the class of benzylisoquinolines. Benzylisoquinolines are organic compounds containing an isoquinoline to which a benzyl group is attached. Juzirine, practically insoluble (in water), is a very weakly acidic compound (based on its | |||
T39733 | Akt | ||
Hu7691 free base 是一种具有口服活性、高效性和选择性的 Akt 抑制剂,对多种神经母细胞瘤细胞系的抗增殖和神经发生作用。Hu7691 free base 抑制 Akt1、Akt2 和 Akt3 ,诱导神经母细胞瘤细胞分化。 | |||
T36672 | |||
The extracellular signal-regulated kinase (ERK) signal transduction pathway regulates a diverse array of cellular processes. These processes include cell survival, proliferation, motility, and differentiation and are constitutively activated in cancers involving lung, colon, pancreas, kidney, and ovary. CAY10561 is a potent, ATP-competitive inhibitor of ERK2 (Ki = 2 nM). This compound is highly selective for ERK2 compared to other kinases such as PKA (Ki = 0.39 μM) and JNK3 (Ki = 4 μM). CAY10561 inhibits proliferation of COLO 205 cells with an IC50 value of 0.54 μM. |
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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