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CAY10404 is a potent and selective cyclooxygenase-2 (COX-2) inhibitor with an IC50 of 1 nM and a selectivity index (SI; COX-1 IC50/COX-2 IC50) of >500000. CAY10404 is a potent PKB/Akt and MAPK signaling pathways inhibitor and induces apoptosis in non-small cell lung cancer (NSCLC) cells. CAY10404, a diarylisoxazole, has good analgesic, anti-inflammatory, and anti-cancer activities .
MIPS521 is a positive allosteric modulator of adenosine A1 receptor (A1AR). MIPS521 also has a lower A1R allosteric affinity (pKB=4.95; KB=11 μM). MIPS521 exhibits pain-relieving effects in vivo through modulation of the increased levels of endogenous adenosine .
API-1, a potent Akt/PKB inhibitor, binds to the PH domain and inhibits Akt membrane translocation. API-1 efficiently reduces the phosphorylation levels of Akt with an IC50 of ∼0.8 μM. API-1 is selective for PKB and does not inhibit the activation of PKC, and PKA. API-1 also induces apoptosis by synergizing with TNF-related apoptosis-inducing ligand (TRAIL) .
Akt1&PKA-IN-2 ((R)-29) is an inhibitor of PKB/AKT with cyclin-dependent kinase 2 (CDK2) selectivity. Akt1&PKA-IN-2 inhibits AKT1, PKAa and CDK2 a with IC50 values of 0.007 µM, 0.01 µM and 0.69 µM, respectively .
AKT-IN-9 is a potent inhibitor of AKT. Protein kinase B (PKB, also known as AKT) is central to PI3K/AKT/mTOR signaling in cells, and its function is important for cell growth, survival, differentiation and metabolism. AKT-IN-9 has the potential for the research of breast and prostate cancer (extracted from patent WO2021185238A1, compound 1) .
AKT-IN-10 is a potent inhibitor of AKT. Protein kinase B (PKB, also known as AKT) is central to PI3K/AKT/mTOR signaling in cells, and its function is important for cell growth, survival, differentiation and metabolism. AKT-IN-10 has the potential for the research of breast and prostate cancer (extracted from patent WO2021185238A1, compound 4) .
MRS2279 is a selective and high affinity P2Y1 receptor antagonist, with a Ki of 2.5 nM and an IC50 of 51.6 nM. MRS2279 competitively inhibits ADP-promoted platelet aggregation with an apparent affnity (pKB=8.05) .
BGC 20-1531 (PGN 1531) hydrochloride is a potent and selective prostanoid EP4 receptor antagonist, with a pKb of 7.6. BGC 20-1531 hydrochloride has the potential for the research of migraine headache .
Cyclopentolate (DL-Cyclopentolate) hydrochloride is an Atropine-like muscarinic receptors antagonist with a pKB value of 7.8 (on the circular ciliary muscle). Cyclopentolate hydrochloride is an anti-muscarinic agent commonly used in the ophthalmologic practice .
Cyclopentolate (DL-Cyclopentolate) is an Atropine-like muscarinic receptors antagonist with a pKB value of 7.8 (on the circular ciliary muscle). Cyclopentolate is an anti-muscarinic agent commonly used in the ophthalmologic practice .
ZD6021 is an orally active Neurokinin 1 Receptor antagonist, with Ki values of 0.12 nM for NK1 and 0.62 nM for NK2. At a concentration of 100 nM, ZD6021 has a pKB value of 8.9 for human pulmonary artery NK1 receptors, and a pKB value of 7.3 for human bronchial NK2 receptors. ZD6021 effectively reduces ASMSP-induced plasma protein extravasation in guinea pigs, with an ED50 of 0.5 mg/kg, and also decreases NK2 mediated bronchoconstriction, with an ED50 of 13 mg/kg .
SB-334867 (SB 334867A) is an excellent,selective and blood–brain barrier permeable orexin-1 (OX1) receptor antagonist, shows selectivity over OX2(pKb=7.4), 100-fold over 5-HT2B, 5-HT2C with pKi values of 5.4 and 5.3, respectively . SB-334867 reduces ethanol consumption and inhibits the acquisition of morphine-induced sensitization to locomotor activity in vivo .
GR 94800 TFA is a potent and selective NK2 receptor peptide antagonist, with pKB values of 9.6, 6.4 and 6.0 for NK2, NK1 and NK3 receptors, respectively .
AC-265347 is a calcium-sensing receptor (CaSR) agonist and positive allosteric modulator (ago-PAM) with the functional affinity (pKB) of 5.1. AC-265347 can be used for the research of hyperparathyroidism and related diseases .
SB-334867 free base (SB334867A free base) is an excellent, selective and blood–brain barrier permeable orexin-1 (OX1) receptor antagonist, shows selectivity over OX2(pKb=7.4), 100-fold over 5-HT2B, 5-HT2C with pKi values of 5.4 and 5.3, respectively . SB-334867 reduces ethanol consumption and inhibits the acquisition of morphine-induced sensitization to locomotor activity in vivo .
BGC-20-1531 (PGN 1531) free base is a potent and selective prostanoid EP4 receptor antagonist, with a pKB of 7.6. BGC-20-1531 free base has the potential for the research of migraine headache .
Hematein is a oxidation product of hematoxylin acted as a dye . Hematein is an allosteric casein kinase II inhibitor with an IC50 of 0.74 μM. Hematein inhibits Akt/PKB Ser129 phosphorylation, the Wnt/TCF pathway and increases apoptosis in lung cancer cells .
GR 83074 is a potent and selective NK-2 (Neurokinin Receptor) antagonist with a pKB of 8.23. GR 83074 is inactive as an NK-3 antagonist and exhibits a 340-fold NK-2/NK-1 selectivity .
MRS2279 diammonium is a selective and high affinity P2Y1 receptor antagonist, with a Ki value of 2.5 nM and an IC50 value of 51.6 nM. MRS2279 diammonium competitively inhibits ADP-promoted platelet aggregation with an pKb value of 8.05 .
Cyclopentolate (hydrochloride) (Standard) is the analytical standard of Cyclopentolate (hydrochloride). This product is intended for research and analytical applications. Cyclopentolate (DL-Cyclopentolate) hydrochloride is an Atropine-like muscarinic receptors antagonist with a pKB value of 7.8 (on the circular ciliary muscle). Cyclopentolate hydrochloride is an anti-muscarinic agent commonly used in the ophthalmologic practice .
(αR,8aS)-GSK1614343 (compound 18a, d2) is a cyclized ghrelin antagonist with an pIC50 value of 8.4. (αR,8aS)-GSK1614343 shows a competitive antagonism of hGHSR1a with a mean pKb value of 8.06 .
BMS-986187 is an δ-opioid receptor-selective positive allosteric modulator (PAM) with an EC50 of 0.03 μM and a pKB of 6.02 (∼1 μM). BMS-986187 has no observable PAM activity at the μ-receptor (EC50=3 μM) .
T7 peptide is an endothelial cell-specific inhibitor. T7 peptide interacts with αVβ3 integrin to inhibit the FAK, PI3-kinase, PKB/Akt, and mTOR signaling pathways in endothelial cells, ultimately suppressing protein synthesis and inducing apoptosis .
PIK-75 hydrochloride is a reversible DNA-PK and p110α-selective inhibitor, which inhibits DNA-PK, p110α and p110γ with IC50s of 2, 5.8 and 76 nM, respectively. PIK-75 hydrochloride inhibits p110α >200-fold more potently than p110β (IC50=1.3 μM) . PIK-75 hydrochloride induces apoptosis .
PIK-75 is a reversible DNA-PK and p110α-selective inhibitor, which inhibits DNA-PK, p110α and p110γ with IC50s of 2, 5.8 and 76 nM, respectively. PIK-75 inhibits p110α >200-fold more potently than p110β (IC50=1.3 μM) . PIK-75 induces apoptosis .
ROS 234 is a potent H3 antagonist, with a pKB of 9.46 for Guinea-pig ileum H3-receptor, a pKi of 8.90 for Rat cerebral cortex H3-receptor, and a ED50 of 19.12 mg/kg (ip) in ex vivo of Rat cerebral cortex. ROS 234 diaplays poor central access .
ROS 234 dioxalate is a potent H3 antagonist, with a pKB of 9.46 for Guinea-pig ileum H3-receptor, a pKi of 8.90 for Rat cerebral cortex H3-receptor, and a ED50 of 19.12 mg/kg (ip) in ex vivo of Rat cerebral cortex. ROS 234 dioxalate diaplays poor central access .
Tetrahydroxyquinone (Tetrahydroxy-1,4-benzoquinone), a primitive anticataract agent, is a redox active benzoquinone. Tetrahydroxyquinone can take part in a redox cycle with semiquinone radicals, leading to the formation of reactive oxygen species (ROS) .
Tetrahydroxyquinone monohydrate (Tetrahydroxy-1,4-benzoquinone monohydrate), a primitive anticataract agent, is a redox active benzoquinone. Tetrahydroxyquinone monohydrate can take part in a redox cycle with semiquinone radicals, leading to the formation of reactive oxygen species (ROS) .
SB-203186 hydrochloride is a potent, selective and competitive 5-HT4 antagonist. SB-203186 hydrochloride antagonizes the 5-HT4 receptor-mediated relaxations of the carbachol-contracted rat isolated oesophagus against 5-HT with pKB values of 10.9 (rat oesophagus), 9.5 (guinea-pig ileum), and 9.0 (human colon) respectively .
PS210 is a potent and selective PDK1 activator with a Kd of 3 μM and targets the PIF-binding pocket of PDK1. PS210 is inactive against other protein kinases, including PDK1 downstream signaling components such as S6K, PKB/Akt or GSK3. In cells, the prodrug of PS210 (PS423) acts as a substrate-selective inhibitor of PDK1, inhibiting the phosphorylation and activation of S6K .
SB 243213 hydrochloride is an orally active, selective and high-affinity 5-HT2C receptor antagonist with a pKi of 9.37 and a pKb of 9.8 for human 5-HT2C receptor. SB 243213 hydrochloride shows greater than a 100-fold selectivity over a wide range of neurotransmitter receptors, enzymes and ion channels. SB 243213 hydrochloride has improved anxiolytic profile and has the potential for schizophrenia and motor disorders .
GR 113808 is a potent and highly selective 5-HT4 receptor antagonist (pKb= 8.8). GR 113808 shows 300-fold selectivity over 5-HT1A, 5-HT1B, 5-HT2A, 5-HT2C and 5-HT3 receptors .
SB 243213 dihydrochloride is an orally active, selective and high-affinity 5-HT2C receptor antagonist with a pKi of 9.37 and a pKb of 9.8 for human 5-HT2C receptor. SB 243213 dihydrochloride shows greater than a 100-fold selectivity over a wide range of neurotransmitter receptors, enzymes and ion channels. SB 243213 dihydrochloride has improved anxiolytic profile and has the potential for schizophrenia and motor disorders .
SB 243213 is an orally active, selective and high-affinity 5-HT2C receptor antagonist with a pKi of 9.37 and a pKb of 9.8 for human 5-HT2C receptor. SB 243213 shows greater than a 100-fold selectivity over a wide range of neurotransmitter receptors, enzymes and ion channels. SB 243213 has improved anxiolytic profile and has the potential for schizophrenia and motor disorders .
Butein is a cAMP-specific PDE inhibitor with an IC50 of 10.4 μM for PDE4 . Butein is a specific protein tyrosine kinase inhibitor with IC50s of 16 and 65 μM for EGFR and p60 c-src in HepG2 cells . Butein sensitizes HeLa cells to Cisplatin through AKT and ERK/p38 MAPK pathways by targeting FoxO3a . Butein is a SIRT1 activator (STAC).
Butein (Standard) is the analytical standard of Butein. This product is intended for research and analytical applications. Butein is a cAMP-specific PDE inhibitor with an IC50 of 10.4 μM for PDE4 . Butein is a specific protein tyrosine kinase inhibitor with IC50s of 16 and 65 μM for EGFR and p60c-src in HepG2 cells . Butein sensitizes HeLa cells to Cisplatin through AKT and ERK/p38 MAPK pathways by targeting FoxO3a . Butein is a SIRT1 activator (STAC).
Adezmapimod (SB 203580) is a selective and ATP-competitive p38 MAPK inhibitor with IC50s of 50 nM and 500 nM for SAPK2a/p38 and SAPK2b/p38β2, respectively. Adezmapimod inhibits LCK, GSK3β and PKBα with IC50s of 100-500-fold higher than that for SAPK2a/p38. Adezmapimod does not disrupt JNK activity and is an autophagy and mitophagy activator .
Adezmapimod (SB 203580; RWJ 64809) hydrochloride is a selective and ATP-competitive p38 MAPK inhibitor with IC50s of 50 nM and 500 nM for SAPK2a/p38 and SAPK2b/p38β2, respectively. Adezmapimod hydrochloride inhibits LCK, GSK3β and PKBα with IC50s of 100-500-fold higher than that for SAPK2a/p38. Adezmapimod hydrochloride does not disrupt JNK activity and is an autophagy and mitophagy activator .
8-pCPT-2'-O-Me-cAMP-AM is a cyclic AMP analogue, selectively activates Epac-Rap signaling pathway. 8-pCPT-2'-O-Me-cAMP-AM protects renal function by activating Epac from ischemia injury. 8-pCPT-2'-O-Me-cAMP-AM also stimulates insulin secretion by interaction with PKA pathway .
Urantide is a selective and competitive urotensin-II (UT) receptor antagonist peptide (pKB=8.3) that blocks human urotensin-II (hU-II)-induced contractions in rat thoracic aorta ex vivo. Urantide can be used to study the (patho)physiological role of hU-II in the mammalian cardiovascular system .
GR 94800 TFA is a potent and selective NK2 receptor peptide antagonist, with pKB values of 9.6, 6.4 and 6.0 for NK2, NK1 and NK3 receptors, respectively .
GR 83074 is a potent and selective NK-2 (Neurokinin Receptor) antagonist with a pKB of 8.23. GR 83074 is inactive as an NK-3 antagonist and exhibits a 340-fold NK-2/NK-1 selectivity .
T7 peptide is an endothelial cell-specific inhibitor. T7 peptide interacts with αVβ3 integrin to inhibit the FAK, PI3-kinase, PKB/Akt, and mTOR signaling pathways in endothelial cells, ultimately suppressing protein synthesis and inducing apoptosis .
Butein is a cAMP-specific PDE inhibitor with an IC50 of 10.4 μM for PDE4 . Butein is a specific protein tyrosine kinase inhibitor with IC50s of 16 and 65 μM for EGFR and p60 c-src in HepG2 cells . Butein sensitizes HeLa cells to Cisplatin through AKT and ERK/p38 MAPK pathways by targeting FoxO3a . Butein is a SIRT1 activator (STAC).
Butein (Standard) is the analytical standard of Butein. This product is intended for research and analytical applications. Butein is a cAMP-specific PDE inhibitor with an IC50 of 10.4 μM for PDE4 . Butein is a specific protein tyrosine kinase inhibitor with IC50s of 16 and 65 μM for EGFR and p60c-src in HepG2 cells . Butein sensitizes HeLa cells to Cisplatin through AKT and ERK/p38 MAPK pathways by targeting FoxO3a . Butein is a SIRT1 activator (STAC).
The AKT1 protein is part of the AKT kinase family and is critical for metabolism, proliferation, survival, growth, and angiogenesis. It phosphorylates more than 100 substrates, coordinates insulin-induced SLC2A4/GLUT4 translocation, affects glucose uptake, and controls glycogen storage through inhibition of GSK3A/B. AKT1 Protein, Human (sf9, His) is the recombinant human-derived AKT1 protein, expressed by Sf9 insect cells , with C-10*His labeled tag.
The AKT2 protein is a serine/threonine protein kinase in the AKT family that is critical for metabolism, proliferation, survival, growth, and angiogenesis. It phosphorylates more than 100 substrates, coordinates insulin-induced SLC2A4/GLUT4 translocation, affects glucose uptake, and controls glycogen storage. AKT2 Protein, Human (sf9, His-GST) is the recombinant human-derived AKT2 protein, expressed by Sf9 insect cells , with C-His, N-GST labeled tag. The total length of AKT2 Protein, Human (sf9, His-GST) is 481 a.a., with molecular weight of ~83.6 kDa.
The AKT3 protein, like AKT1 and AKT2, is an important member of the AKT kinase family and plays a central role in a variety of cellular processes, including metabolism, proliferation, survival, growth, and angiogenesis. AKT3 has more than 100 reported targets and coordinates complex signaling pathways that control glucose uptake, regulate glycogen storage, and influence neurogenesis. AKT3 Protein, Human (sf9, GST) is the recombinant human-derived AKT3 protein, expressed by Sf9 insect cells , with N-GST labeled tag. The total length of AKT3 Protein, Human (sf9, GST) is 479 a.a., with molecular weight of ~81 kDa.
The AKT1 protein is part of the AKT kinase family and is critical for metabolism, proliferation, survival, growth, and angiogenesis. It phosphorylates more than 100 substrates, coordinates insulin-induced SLC2A4/GLUT4 translocation, affects glucose uptake, and controls glycogen storage through inhibition of GSK3A/B. AKT1 Protein, Human (Active, sf9, GST) is the recombinant human-derived AKT1, expressed by Sf9 insect cells , with GST labeled tag. The total length of AKT1 Protein, Human (Active, sf9, GST) is 480 a.a.,
AKT2 Protein, Mouse (His, Myc) is the recombinant mouse-derived AKT2, expressed by E. coli , with N-10*His, C-Myc labeled tag. The total length of AKT2 Protein, Mouse (His, Myc) is 481 a.a.,
The AKT3 protein is part of the AKT kinase family and regulates a variety of cellular processes, including metabolism, proliferation, and survival.Its least-studied isoform, AKT3, is critical for brain development and is critical for the viability of malignant glioma cells.AKT3 Protein, Mouse (sf9) is the recombinant mouse-derived AKT3 protein, expressed by Sf9 insect cells , with tag free.
The AKT3 protein, like AKT1 and AKT2, is an important member of the AKT kinase family and plays a central role in a variety of cellular processes, including metabolism, proliferation, survival, growth, and angiogenesis. AKT3 has more than 100 reported targets and coordinates complex signaling pathways that control glucose uptake, regulate glycogen storage, and influence neurogenesis. AKT3 Protein, Human (Active, sf9, GST) is the recombinant human-derived AKT3, expressed by Sf9 insect cells , with GST labeled tag. The total length of AKT3 Protein, Human (Active, sf9, GST) is 479 a.a.,
The AKT2 protein is a serine/threonine protein kinase in the AKT family that is critical for metabolism, proliferation, survival, growth, and angiogenesis. It phosphorylates more than 100 substrates, coordinates insulin-induced SLC2A4/GLUT4 translocation, affects glucose uptake, and controls glycogen storage. AKT2 Protein, Human (Active, sf9, GST) is the recombinant human-derived AKT2, expressed by Sf9 insect cells , with GST labeled tag. The total length of AKT2 Protein, Human (Active, sf9, GST) is 480 a.a.,
AKT1; PKB; RAC; RAC-alpha serine/threonine-protein kinase; Protein kinase B; PKB; Protein kinase B alpha; PKB alpha; Proto-oncogene c-Akt; RAC-PK-alpha
ICC/IF, WB, IHC-F, IHC-P, ELISA
Human, Mouse, Rat
Phospho-AKT (Thr308) Antibody is a non-conjugated and Rabbit origined polyclonal antibody about 56 kDa, targeting to Phospho-AKT (Thr308). It can be used for ICC/IF,WB,IHC-F,IHC-P,ELISA assays with tag free, in the background of Human, Mouse, Rat.
AKT1; PKB; RAC; RAC-alpha serine/threonine-protein kinase; Protein kinase B; PKB; Protein kinase B alpha; PKB alpha; Proto-oncogene c-Akt; RAC-PK-alpha
WB
Human, Mouse, Rat
Phospho-AKT1 (Ser473) Antibody is a non-conjugated and Rabbit origined monoclonal antibody about 56 kDa, targeting to Phospho-AKT (Ser473). It can be used for WB assays with tag free, in the background of Human, Mouse, Rat.
AKT 1; AKT; AKT1; AKT1_HUMAN ; MGC99656; PKB; PKB-ALPHA; PRKBA; Protein Kinase B Alpha ; Proto-oncogene c-Akt; RAC Alpha;
IHC-P, IHC-F, ICC/IF, IP, FC
Human, Mouse
AKT1 Antibody (YA634) is a non-conjugated and Rabbit origined monoclonal antibody about 56 kDa, targeting to AKT1. It can be used for IHC-P,IP,FC assays with tag free, in the background of Human, Mouse.
AKT 1 antibody; AKT antibody; AKT1 antibody; AKT1_HUMAN antibody; MGC99656 antibody; PKB antibody; PKB-ALPHA antibody; PRKBA antibody; Protein Kinase B Alpha antibody; Protein kinase B antibody; Proto-oncogene c-Akt antibody; RAC Alpha antibody; RAC antibody; RAC-alpha serine/threonine-protein kinase antibody; RAC-PK-alpha antibody;
WB, ICC/IF, IHC-P
Human, Mouse
Phospho-Akt1(Ser473) Antibody is a non-conjugated and Rabbit origined monoclonal antibody about 56 kDa, targeting to Phospho-Akt1(Ser473). It can be used for WB,ICC/IF,IHC-P assays with tag free, in the background of Human, Mouse.
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