Search Result
Results for "
CREB phosphorylation
" in MedChemExpress (MCE) Product Catalog:
4
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
-
- HY-B1203
-
|
9α-Fludrocortisone; 9α-Fluorcortisol
|
Mineralocorticoid Receptor
Glucocorticoid Receptor
Apoptosis
|
Neurological Disease
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
Fludrocortisone (9α-Fludrocortisone) is an orally active mineralocorticoid and glucocorticoid receptor agonist. Fludrocortisone suppresses pro-inflammatory cytokine expression, reduces CCL2, IL-6, IL-8 levels, upregulates mineralocorticoid receptor (MR) expression, induces PI3K/Akt, GSK-3β, CREB, ERK1/2, mTOR phosphorylation, blocks Tau hyperphosphorylation, prevents apoptosis, promotes survival and proliferation, enhances renal sodium and water transport, increases plasma volume and blood pressure, reduces plasma potassium and renin activity, stimulates erythropoietin expression, modulates uterine receptivity genes, and reverses PP242-induced MUC1 upregulation. Fludrocortisone can be used for the research of congenital adrenal hyperplasia, postural hypotension, and adrenal insufficiency .
|
-
-
- HY-133529
-
PA-8
2 Publications Verification
|
PACAP Receptor
|
Neurological Disease
Inflammation/Immunology
|
|
PA-8 is a potent, selective and orally active PACAP type I (PAC1) receptor antagonist. PA-8 inhibits the phosphorylation of CREB induced by PACAP in PAC1-, but not VPAC1- or VPAC2-receptor. PA-8 also inhibits PACAP-induced cAMP elevation with an IC50 of 2 nM .
|
-
-
- HY-101084
-
NSC 228155
Maximum Cited Publications
20 Publications Verification
|
EGFR
Histone Acetyltransferase
Epigenetic Reader Domain
|
Cancer
|
|
NSC 228155 is an activator of EGFR, binds to the extracellular region of EGFR and enhance tyrosine phosphorylation of EGFR . NSC 228155 is also a potent inhibitor of KIX-KID interaction, inhibits kinase-inducible domain (KID) from CREB and KID-interacting domain (KIX) from CBP, with an IC50 of 0.36 μM .
|
-
-
- HY-B0188A
-
|
Org GB 94
|
Histamine Receptor
Opioid Receptor
ERK
p38 MAPK
|
Neurological Disease
Metabolic Disease
|
|
Mianserin hydrochloride (Org GB 94) is an orally active H1 receptor antagonist. Mianserin hydrochloride can activate κ-opioid receptor and octopamine receptor. Mianserin hydrochloride increases ERK1/2 and CREB phosphorylation, and antagonizes full κ-opioid agonist and Dynorphin A (HY-P1333)-induced MAPK phosphorylation. Mianserin hydrochloride modulates social and exploratory behaviour, raises electroconvulsive thresholds. Mianserin hydrochloride can be used for the research of neurological disease, such as depression and epilepsy .
|
-
-
- HY-P1291
-
|
|
PKA
Epigenetic Reader Domain
Flavivirus
|
Infection
Neurological Disease
|
|
PKI 14-22 amide, myristoylated is a selective, cAMP-dependent, competitive PKA inhibitor with Ki=~36 nM. The myristoylation modification of PKI 14-22 amide, myristoylated makes it more permeable to cell membranes and blood-brain barriers than the precursor molecule. PKI 14-22 amide, myristoylated can block the phosphorylation of cAMP-dependent downstream targets (such as CREB). PKI 14-22 amide, myristoylated can prevent the development of morphine analgesic tolerance in mice, and also inhibits protein translation and negative-strand RNA synthesis of Zika virus. PKI 14-22 amide, myristoylated can be used in research fields such as opioid tolerance mechanisms and antiviral drugs .
|
-
-
- HY-147557
-
PA-915
1 Publications Verification
PAC1R antagonist 1
|
PACAP Receptor
|
Neurological Disease
|
|
PA-915 (PAC1R antagonist 1) is a potent and orally active antagonist of PAC1 receptor. PA-915 inhibits pituitary adenylate cyclase-activating polypeptide (PACAP)-induced CREB phosphorylation. PA-915 can inhibit PACAP- and nerve injury-induced allodynia. PA-915 can be used for the research of neuropathic pain .
|
-
-
- HY-B0188
-
|
Mianserine
|
Histamine Receptor
Opioid Receptor
ERK
p38 MAPK
|
Neurological Disease
|
|
Mianserin (Mianserine) is an orally active H1 receptor antagonist. Mianserin can activate κ-opioid receptor and octopamine receptor. Mianserin increases ERK1/2 and CREB phosphorylation, and antagonizes full κ-opioid agonist and Dynorphin A (HY-P1333)-induced MAPK phosphorylation. Mianserin modulates social and exploratory behaviour, raises electroconvulsive thresholds. Mianserin can be used for the research of neurological disease, such as depression and epilepsy .
|
-
-
- HY-103322
-
|
|
PKA
Potassium Channel
|
Metabolic Disease
Cancer
|
|
6-Bnz-cAMP sodium, a derivative of cyclic adenosine monophosphate (cAMP), is a selective PKA activator with inhibitory activity against the bTREK-1 K + channel. 6-Bnz-cAMP sodium does not activate the Epac signaling pathway. It inhibits the bTREK-1 K + channel via a voltage-independent, ATP-dependent mechanism that is independent of the PKA/Epac/calmodulin kinase/MAP kinase pathway. 6-Bnz-cAMP sodium activates CREB phosphorylation to regulate osteoblast-specific gene expression, induces osteoblast differentiation, promotes extracellular matrix mineralization, supports osteoblast proliferation, and shows no cytotoxicity toward osteoblasts. It can be used in studies related to bone tissue repair and regeneration .
|
-
-
- HY-103100
-
|
|
5-HT Receptor
Epigenetic Reader Domain
Akt
Ribosomal S6 Kinase (RSK)
FOXO
|
Neurological Disease
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
SB-699551 is a selective and brain penetrant 5-HT5A receptor antagonist with a pKi of 8.2 nM. SB-699551 shows high selectivity over most other 5-HT receptor subtypes, dopamine receptors, and α1B adrenoceptor. SB-699551 disrupts Gαi/o-coupled and PI3K/AKT/mTOR signaling pathways, alters CREB, ATF1, AKT, PRAS40, S6K, and FOXO1 phosphorylation in breast tumor cells. SB-699551 can be used for the research of anxiety, breast cancer, and Alzheimer's disease .
|
-
-
- HY-B1428
-
-
-
- HY-P1291A
-
|
|
PKA
Epigenetic Reader Domain
Flavivirus
|
Infection
Neurological Disease
|
|
PKI 14-22 amide, myristoylated TFA is a selective, cAMP-dependent, competitive PKA inhibitor with Ki=~36 nM. The myristoylation modification of PKI 14-22 amide, myristoylated TFA makes it more permeable to cell membranes and blood-brain barriers than the precursor molecule. PKI 14-22 amide, myristoylated TFA can block the phosphorylation of cAMP-dependent downstream targets (such as CREB). PKI 14-22 amide, myristoylated TFA can prevent the development of analgesic tolerance in mice, and also inhibits protein translation and negative-strand RNA synthesis of Zika virus. PKI 14-22 amide, myristoylated TFA can be used in research fields such as opioid tolerance mechanisms and antiviral drugs .
|
-
-
- HY-P6292
-
|
|
PACAP Receptor
PKA
ERK
PI3K
Akt
GSK-3
|
Neurological Disease
Cancer
|
|
KS-133 is a bicyclic peptide with VIPR2 antagonistic activity that can cross the blood-brain barrier. KS-133 selectively blocks VIPR2-mediated Gq/Ca, Gs/cAMP, cAMP/PKA/ERK and PI3K/AKT/GSK3β signaling pathways. KS-133 inhibits VIPR2 agonist-induced CREB phosphorylation in the prefrontal cortex of mice. KS-133 shifts the polarization direction of macrophages toward M1. KS-133 attenuates cancer cell proliferation and reduces the cell cycle distribution level at the S-M phase. KS-133 exerts antitumor effects in a mouse model of colorectal cancer. KS-133 reverses cognitive decline in mouse models of psychiatric disorders. KS-133 can be used for research related to schizophrenia, colorectal cancer and breast cancer .
|
-
-
- HY-116586
-
|
|
Sigma Receptor
mAChR
ERK
Amyloid-β
Tau Protein
|
Neurological Disease
|
|
AF710B is an orally effective allosteric agonist for the M1 muscarinic receptor and σ1 receptor. AF710B activates the downstream phosphorylated ERK1/2 and phosphorylated CREB signaling pathways. AF710B simultaneously improves cognitive function and alleviates the core pathological features of Alzheimer's disease, including Aβ deposition, excessive Tau phosphorylation and neuroinflammation. AF710B is applicable to the research of Alzheimer's disease .
|
-
-
- HY-121197
-
|
Ophiocordin; Azepinostatin
|
MARCKS
PKA
PKC
|
Others
|
|
Balanol (Ophiocordin; Azepinostatin) is a potent and ATP competitive PKC/PKA inhibitor against human PKC isozymes α, β-I, β-II, γ, δ, ε, η (IC50s=4-9 nM) and ζ (IC50=150 nM). Balanol also blocks the phosphorylation of cyclic AMP response element-binding protein (CREB) and myristoylated alanine-rich C kinase substrate (MARCKS). Balanol can be isolated from the fungus Verticillium balanoides .
|
-
-
- HY-150073
-
|
|
PKA
|
Cancer
|
|
DS01080522 is a Protein Kinase cAMP-Activated Catalytic Subunit Alpha (PRKACA) inhibitor. DS01080522 inhibits PRKACA kinase activity and CREB phosphorylation with IC50s of 0.8 nM and 66 nM, respectively. DS01080522 can be used for the research of cancer .
|
-
-
- HY-B0188AR
-
|
Org GB 94 (Standard)
|
Reference Standards
Histamine Receptor
Opioid Receptor
ERK
p38 MAPK
|
Neurological Disease
Metabolic Disease
|
|
Mianserin hydrochloride (Org GB 94) (Standard) is the analytical standard of Mianserin hydrochloride. This product is intended for research and analytical applications. Mianserin hydrochloride is an orally active H1 receptor antagonist. Mianserin hydrochloride can activate κ-opioid receptor and octopamine receptor. Mianserin hydrochloride increases ERK1/2 and CREB phosphorylation, and antagonizes full κ-opioid agonist and Dynorphin A (HY-P1333)-induced MAPK phosphorylation. Mianserin hydrochloride modulates social and exploratory behaviour, raises electroconvulsive thresholds. Mianserin hydrochloride can be used for the research of neurological disease, such as depression and epilepsy .
|
-
-
- HY-B0188S
-
|
Mianserine-d3
|
Histamine Receptor
Isotope-Labeled Compounds
Opioid Receptor
ERK
p38 MAPK
|
Neurological Disease
|
|
Mianserin-d3 is the deuterium labeled Mianserin (HY-B0188). Mianserin (Mianserine) is an orally active H1 receptor antagonist. Mianserin can activate κ-opioid receptor and octopamine receptor. Mianserin increases ERK1/2 and CREB phosphorylation, and antagonizes full κ-opioid agonist and Dynorphin A (HY-P1333)-induced MAPK phosphorylation. Mianserin modulates social and exploratory behaviour, raises electroconvulsive thresholds. Mianserin can be used for the research of neurological disease, such as depression and epilepsy .
|
-
-
- HY-B0188AS
-
|
Org GB 94-d3
|
Isotope-Labeled Compounds
Histamine Receptor
Opioid Receptor
ERK
p38 MAPK
|
Neurological Disease
Metabolic Disease
|
|
Mianserin-d3 hydrochloride is the deuterium labeled Mianserin. Mianserin (Mianserine) is an orally active H1 receptor antagonist. Mianserin can activate κ-opioid receptor and octopamine receptor. Mianserin increases ERK1/2 and CREB phosphorylation, and antagonizes full κ-opioid agonist and Dynorphin A (HY-P1333)-induced MAPK phosphorylation. Mianserin modulates social and exploratory behaviour, raises electroconvulsive thresholds. Mianserin can be used for the research of neurological disease, such as depression and epilepsy .
|
-
-
- HY-59201A
-
|
|
ERK
5-HT Receptor
Epigenetic Reader Domain
nAChR
|
Neurological Disease
Metabolic Disease
|
|
A-582941 dihydrochloride is a selective, orally active, blood-brain barrier-permeable α7 nAChR agonist, with Ki values of 10.8 nM and 17 nM in rat brain and human frontal cortex, respectively. A-582941 dihydrochloride exhibits agonistic activity at 5-HT3 receptors, with a Ki of 150 nM. A-582941 dihydrochloride triggers phosphorylation of ERK1/2 and CREB, inhibits GSK-3β via Ser-9 phosphorylation, increases acetylcholine release, induces the expression of Arc and c-Fos, activates brain regions associated with working memory and attention, and reduces cell death caused by nerve growth factor (NGF) deprivation. A-582941 dihydrochloride is applicable for the research of Alzheimer's disease and schizophrenia .
|
-
-
- HY-134261
-
|
8-Bromoadenosine-5'-O-diphosphoribose
|
TRP Channel
CaMK
|
Metabolic Disease
Cancer
|
|
8-Br-ADPR (8-Bromoadenosine-5'-O-diphosphoribose) is a TRPM2 inhibitor and ADPR signaling pathway antagonist. 8-Br-ADPR inhibits glucagon-mediated nuclear calcium signaling and downstream CaMKII/CREB phosphorylation by blocking ADPR-induced TRPM2 activation. 8-Br-ADPR significantly reduces gluconeogenic gene expression and blood glucose levels in diabetic models. 8-Br-ADPR effectively blocks ADPR-mediated calcium signal transduction in NK cells, inhibits immune synapse formation, granzyme B release and cytolytic activity against melanoma cells. 8-Br-ADPR is widely used in studies related to diseases such as diabetes, melanoma and lymphoma .
|
-
-
- HY-134261A
-
|
8-Bromoadenosine-5'-O-diphosphoribose disodium
|
CaMK
TRP Channel
|
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
8-Br-ADPR disodium (8-Bromoadenosine-5'-O-diphosphoribose) is a TRPM2 inhibitor and ADPR signaling pathway antagonist. 8-Br-ADPR disodium inhibits glucagon-mediated nuclear calcium signaling and downstream CaMKII/CREB phosphorylation by blocking ADPR-induced TRPM2 activation. 8-Br-ADPR disodium significantly reduces gluconeogenic gene expression and blood glucose levels in diabetic models. 8-Br-ADPR disodium effectively blocks ADPR-mediated calcium signal transduction in NK cells, inhibits immune synapse formation, granzyme B release and cytolytic activity against melanoma cells. 8-Br-ADPR disodium is widely used in studies related to diseases such as diabetes, melanoma and lymphoma .
|
-
-
- HY-171591
-
|
|
Salt-inducible Kinase (SIK)
Interleukin Related
TNF Receptor
|
Infection
|
|
SIK2-IN-4 (Compound 4) is a highly selective SIK1/2 inhibitor (IC50s 0.143 and 0.076 μM, respectively). SIK2-IN-4 reduces the phosphorylation of transcription coactivator 3 (CRTC3) by targeting SIK1/2, thereby regulating cAMP response element binding protein (CREB)-dependent transcriptional activity. SIK2-IN-4 inhibits the production of pro-inflammatory cytokines such as TNF (IC50: 0.11 µM), IL-12/23 p40 (IC50: 0.25 µM), and IL-23 (IC50: 0.47 µM), while inducing the expression of the anti-inflammatory cytokine IL-10. SIK2-IN-4 can be used to study intestinal inflammation and other chronic inflammatory diseases .
|
-
-
- HY-137624
-
|
|
PKA
|
Others
|
|
Sp-cAMPS-AM is an analog of cAMP. Sp-cAMPS-AM acts as the inducer of PKA activation and CREB phosphorylation, through entrance into the cell and release of its parent polar structure Sp-cAMPS .
|
-
-
- HY-B1428R
-
|
Ethenzamide (Standard)
|
Reference Standards
Tyrosinase
Reactive Oxygen Species (ROS)
PERK
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
2-Ethoxybenzamide (Standard) is the analytical standard of 2-Ethoxybenzamide (HY-B1428). 2-Ethoxybenzamide (Ethenzamide) is a nonsteroidal anti-inflammatory agent that shows analgesic and antipyretic effects. 2-Ethoxybenzamide induces melanin synthesis via cAMP response element-binding protein (CREB) phosphorylation. 2-Ethoxybenzamide can be used in the research of hypopigmentation and inflammation-related diseases .
|
-
-
- HY-P11092
-
|
|
Endogenous Metabolite
|
Neurological Disease
|
|
TLQP-62 (mouse,rat) is a secreted C-terminal peptide that can be derived from protein VGF. TLQP-62 activates the BDNF-TrkB signaling pathway, inducing acute, transient phosphorylation of TrkB receptor and downstream CREB (Ser133) phosphorylation. TLQP-62 demonstrates excellent efficacy in promoting long-term fear memory formationin wild-type mice and reversing memory impairment in VGF heterozygous knock-out mice. TLQP-62 can be used for the study of memory-related neurological disorders (e.g., Alzheimer’s disease, frontotemporal dementia) .
|
-
-
- HY-137381
-
|
N6-Benzoyl-cAMP
|
PKA
Potassium Channel
|
Metabolic Disease
|
|
6-Bnz-cAMP, a derivative of cyclic adenosine monophosphate (cAMP), is a selective PKA activator with inhibitory activity against the bTREK-1 K + channel. 6-Bnz-cAMP does not activate the Epac signaling pathway. 6-Bnz-cAMP inhibits the bTREK-1 K + channel via a voltage-independent, ATP-dependent mechanism that is independent of the PKA/Epac/calmodulin kinase/MAP kinase pathway. 6-Bnz-cAMP activates CREB phosphorylation to regulate osteoblast-specific gene expression, induces osteoblast differentiation, promotes extracellular matrix mineralization, supports osteoblast proliferation, and shows no cytotoxicity toward osteoblasts. 6-Bnz-cAMP can be used in studies related to bone tissue repair and regeneration .
|
-
-
- HY-B1203S
-
|
9α-Fludrocortisone-d5; 9α-Fluorcortisol-d5
|
Isotope-Labeled Compounds
Mineralocorticoid Receptor
Glucocorticoid Receptor
Apoptosis
|
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
Fludrocortisone-d5 (9α-Fludrocortisone-d5) is the deuterium labeled Fludrocortisone (HY-B1203). Fludrocortisone is an orally active mineralocorticoid and glucocorticoid receptor agonist. Fludrocortisone suppresses pro-inflammatory cytokine expression, reduces CCL2, IL-6, IL-8 levels, upregulates mineralocorticoid receptor (MR) expression, induces PI3K/Akt, GSK-3β, CREB, ERK1/2, mTOR phosphorylation, blocks Tau hyperphosphorylation, prevents apoptosis, promotes survival and proliferation, enhances renal sodium and water transport, increases plasma volume and blood pressure, reduces plasma potassium and renin activity, stimulates erythropoietin expression, modulates uterine receptivity genes, and reverses PP242-induced MUC1 upregulation. Fludrocortisone can be used for the research of congenital adrenal hyperplasia, postural hypotension, and adrenal insufficiency.
|
-
-
- HY-B1203R
-
|
9α-Fludrocortisone (Standard); 9α-Fluorcortisol (Standard)
|
Reference Standards
Mineralocorticoid Receptor
Glucocorticoid Receptor
Apoptosis
|
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
Fludrocortisone (Standard) (9α-Fludrocortisone (Standard)) is the analytical standard of Fludrocortisone (HY-B1203). This product is intended for research and analytical applications. Fludrocortisone is an orally active mineralocorticoid and glucocorticoid receptor agonist. Fludrocortisone suppresses pro-inflammatory cytokine expression, reduces CCL2, IL-6, IL-8 levels, upregulates mineralocorticoid receptor (MR) expression, induces PI3K/Akt, GSK-3β, CREB, ERK1/2, mTOR phosphorylation, blocks Tau hyperphosphorylation, prevents apoptosis, promotes survival and proliferation, enhances renal sodium and water transport, increases plasma volume and blood pressure, reduces plasma potassium and renin activity, stimulates erythropoietin expression, modulates uterine receptivity genes, and reverses PP242-induced MUC1 upregulation. Fludrocortisone can be used for the research of congenital adrenal hyperplasia, postural hypotension, and adrenal insufficiency.
|
-
-
- HY-B1203S1
-
|
9α-Fludrocortisone-d2; 9α-Fluorcortisol-d2
|
Isotope-Labeled Compounds
Mineralocorticoid Receptor
Glucocorticoid Receptor
Apoptosis
|
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
Fludrocortisone-d2 (9α-Fludrocortisone-d2) is the deuterium labeled Fludrocortisone (HY-B1203). Fludrocortisone is an orally active mineralocorticoid and glucocorticoid receptor agonist. Fludrocortisone suppresses pro-inflammatory cytokine expression, reduces CCL2, IL-6, IL-8 levels, upregulates mineralocorticoid receptor (MR) expression, induces PI3K/Akt, GSK-3β, CREB, ERK1/2, mTOR phosphorylation, blocks Tau hyperphosphorylation, prevents apoptosis, promotes survival and proliferation, enhances renal sodium and water transport, increases plasma volume and blood pressure, reduces plasma potassium and renin activity, stimulates erythropoietin expression, modulates uterine receptivity genes, and reverses PP242-induced MUC1 upregulation. Fludrocortisone can be used for the research of congenital adrenal hyperplasia, postural hypotension, and adrenal insufficiency.
|
-
-
- HY-183599
-
|
|
Adenosine Receptor
|
Cancer
|
|
MK-1088 is an orally active A2A/A2B adenosine receptor antagonist with human A2A Ki of 0.31 nM, human A2B Ki 5.3 nM. MK-1088 blocks receptor downstream signaling, inhibits CREB phosphorylation and reverses adenosine-mediated immunosuppression. MK-1088 restores TNF−α release and enhances tumor immune surveillance. MK-1088 can be used for the research of cancer[1].
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-
-
- HY-179606
-
|
|
Transmembrane Glycoprotein
Arrestin
ERK
Epigenetic Reader Domain
|
Neurological Disease
|
|
RWT9996 is a balanced GPR17 antagonist. RWT9996 has an inhibitory effect on G protein activation and β-arrestin-2 recruitment induced by MDL-29951. RWT9996 inhibits the phosphorylation of ERK/CREB and the accumulation of inositol phosphate (b IP1) induced by MDL-29951. RWT9996 can be used for the study of neurological diseases .
|
-
-
- HY-179684
-
|
|
CGRP Receptor
5-HT Receptor
ERK
Epigenetic Reader Domain
|
Neurological Disease
|
|
PCC0105005 is a dual-target CGRP Receptor antagonist (IC50 = 1.01 nM) and a partial agonist of 5-HT1F Receptor (EC50 = 77.91 nM). PCC0105005 shows significant efficacy in the rat model of migraine. PCC0105005 significantly reduces the expression of CGRP and c-Fos proteins, and inhibits the phosphorylation levels of ERK and CREB. PCC0105005 can be used for research on migraine .
|
-
-
- HY-101084R
-
|
|
EGFR
Reference Standards
Histone Acetyltransferase
Epigenetic Reader Domain
|
Cancer
|
|
NSC 228155 (Standard) is the analytical standard of NSC 228155 (HY-101084). This product is intended for research and analytical applications. NSC 228155 is an activator of EGFR, binds to the extracellular region of EGFR and enhance tyrosine phosphorylation of EGFR . NSC 228155 is also a potent inhibitor of KIX-KID interaction, inhibits kinase-inducible domain (KID) from CREB and KID-interacting domain (KIX) from CBP, with an IC50 of 0.36 μM .
|
-
-
- HY-103100R
-
|
|
Reference Standards
5-HT Receptor
Epigenetic Reader Domain
Akt
Ribosomal S6 Kinase (RSK)
FOXO
|
Neurological Disease
Cancer
|
|
SB-699551 (Standard) is the analytical standard of SB-699551 (HY-103100). This product is intended for research and analytical applications. SB-699551 is a potent and selective 5-HT5A antagonist with a Ki value of 5.1 μM. SB-699551 increases the phosphorylation levels of CREB and ATF1, and decreases the phosphorylation levels of AKT, PRAS40, P70S6K, FOXO1, and S6RP. SB-699551 improves drug-induced cognitive deficits. SB-699551 improves social withdrawal and forgetfulness. SB-699551 inhibits breast cancer.
|
-
-
- HY-182580
-
|
|
GPR119
Dipeptidyl Peptidase
|
Metabolic Disease
Inflammation/Immunology
|
|
HBK001 is an orally active and selective dual GPR119 agonist and DPP-IV inhibitor. HBK001 triggers cAMP production, PKA activation, CREB phosphorylation, glucose-stimulated insulin secretion, plasma incretin elevation, β-cell proliferation, and β-cell function gene up-regulation. HBK001 reduces blood glucose, ameliorates hyperglycemia, improves glucose tolerance, and enhances islet morphology. HBK001 can be used for the research of type 2 diabetes mellitus .
|
-
-
- HY-59201
-
|
|
nAChR
5-HT Receptor
ERK
Epigenetic Reader Domain
|
Neurological Disease
|
|
A-582941 is a selective, orally active, blood-brain barrier-permeable α7 nAChR agonist, with Ki values of 10.8 nM and 17 nM in rat brain and human frontal cortex, respectively. A-582941 exhibits agonistic activity at 5-HT3 receptors, with a Ki of 150 nM. A-582941 triggers phosphorylation of ERK1/2 and CREB, inhibits GSK-3β via Ser-9 phosphorylation, increases acetylcholine release, induces the expression of Arc and c-Fos, activates brain regions associated with working memory and attention, and reduces cell death caused by nerve growth factor (NGF) deprivation. A-582941 is applicable for the research of Alzheimer's disease and schizophrenia .
|
-
-
- HY-136700
-
|
|
5-HT Receptor
Akt
|
Neurological Disease
Cancer
|
|
SB-699551 free base is a selective and brain penetrant 5-HT5A receptor antagonist with a pKi of 8.2 nM. SB-699551 free base shows high selectivity over most other 5-HT receptor subtypes, dopamine receptors, and α1B adrenoceptor. SB-699551 free base disrupts Gαi/o-coupled and PI3K/AKT/mTOR signaling pathways, alters CREB, ATF1, AKT, PRAS40, S6K, and FOXO1 phosphorylation in breast tumor cells. SB-699551 free base can be used for the research of anxiety, breast cancer, and Alzheimer's disease .
|
-
| Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P1291
-
|
|
PKA
Epigenetic Reader Domain
Flavivirus
|
Infection
Neurological Disease
|
|
PKI 14-22 amide, myristoylated is a selective, cAMP-dependent, competitive PKA inhibitor with Ki=~36 nM. The myristoylation modification of PKI 14-22 amide, myristoylated makes it more permeable to cell membranes and blood-brain barriers than the precursor molecule. PKI 14-22 amide, myristoylated can block the phosphorylation of cAMP-dependent downstream targets (such as CREB). PKI 14-22 amide, myristoylated can prevent the development of morphine analgesic tolerance in mice, and also inhibits protein translation and negative-strand RNA synthesis of Zika virus. PKI 14-22 amide, myristoylated can be used in research fields such as opioid tolerance mechanisms and antiviral drugs .
|
-
- HY-P1291A
-
|
|
PKA
Epigenetic Reader Domain
Flavivirus
|
Infection
Neurological Disease
|
|
PKI 14-22 amide, myristoylated TFA is a selective, cAMP-dependent, competitive PKA inhibitor with Ki=~36 nM. The myristoylation modification of PKI 14-22 amide, myristoylated TFA makes it more permeable to cell membranes and blood-brain barriers than the precursor molecule. PKI 14-22 amide, myristoylated TFA can block the phosphorylation of cAMP-dependent downstream targets (such as CREB). PKI 14-22 amide, myristoylated TFA can prevent the development of analgesic tolerance in mice, and also inhibits protein translation and negative-strand RNA synthesis of Zika virus. PKI 14-22 amide, myristoylated TFA can be used in research fields such as opioid tolerance mechanisms and antiviral drugs .
|
-
- HY-P6292
-
|
|
PACAP Receptor
PKA
ERK
PI3K
Akt
GSK-3
|
Neurological Disease
Cancer
|
|
KS-133 is a bicyclic peptide with VIPR2 antagonistic activity that can cross the blood-brain barrier. KS-133 selectively blocks VIPR2-mediated Gq/Ca, Gs/cAMP, cAMP/PKA/ERK and PI3K/AKT/GSK3β signaling pathways. KS-133 inhibits VIPR2 agonist-induced CREB phosphorylation in the prefrontal cortex of mice. KS-133 shifts the polarization direction of macrophages toward M1. KS-133 attenuates cancer cell proliferation and reduces the cell cycle distribution level at the S-M phase. KS-133 exerts antitumor effects in a mouse model of colorectal cancer. KS-133 reverses cognitive decline in mouse models of psychiatric disorders. KS-133 can be used for research related to schizophrenia, colorectal cancer and breast cancer .
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- HY-P11092
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Endogenous Metabolite
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Neurological Disease
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TLQP-62 (mouse,rat) is a secreted C-terminal peptide that can be derived from protein VGF. TLQP-62 activates the BDNF-TrkB signaling pathway, inducing acute, transient phosphorylation of TrkB receptor and downstream CREB (Ser133) phosphorylation. TLQP-62 demonstrates excellent efficacy in promoting long-term fear memory formationin wild-type mice and reversing memory impairment in VGF heterozygous knock-out mice. TLQP-62 can be used for the study of memory-related neurological disorders (e.g., Alzheimer’s disease, frontotemporal dementia) .
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Product Name |
Category |
Target |
Chemical Structure |
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- HY-B0188A
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- HY-121197
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Ophiocordin; Azepinostatin
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Structural Classification
Natural Products
Microorganisms
Source Classification
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MARCKS
PKA
PKC
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Balanol (Ophiocordin; Azepinostatin) is a potent and ATP competitive PKC/PKA inhibitor against human PKC isozymes α, β-I, β-II, γ, δ, ε, η (IC50s=4-9 nM) and ζ (IC50=150 nM). Balanol also blocks the phosphorylation of cyclic AMP response element-binding protein (CREB) and myristoylated alanine-rich C kinase substrate (MARCKS). Balanol can be isolated from the fungus Verticillium balanoides .
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- HY-B0188AR
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Org GB 94 (Standard)
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Alkaloids
Structural Classification
Leguminosae
Other Alkaloids
Crotalaria pallida Ait.
Plants
Source Classification
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Reference Standards
Histamine Receptor
Opioid Receptor
ERK
p38 MAPK
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Mianserin hydrochloride (Org GB 94) (Standard) is the analytical standard of Mianserin hydrochloride. This product is intended for research and analytical applications. Mianserin hydrochloride is an orally active H1 receptor antagonist. Mianserin hydrochloride can activate κ-opioid receptor and octopamine receptor. Mianserin hydrochloride increases ERK1/2 and CREB phosphorylation, and antagonizes full κ-opioid agonist and Dynorphin A (HY-P1333)-induced MAPK phosphorylation. Mianserin hydrochloride modulates social and exploratory behaviour, raises electroconvulsive thresholds. Mianserin hydrochloride can be used for the research of neurological disease, such as depression and epilepsy .
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| Cat. No. |
Product Name |
Chemical Structure |
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- HY-B0188S
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Mianserin-d3 is the deuterium labeled Mianserin (HY-B0188). Mianserin (Mianserine) is an orally active H1 receptor antagonist. Mianserin can activate κ-opioid receptor and octopamine receptor. Mianserin increases ERK1/2 and CREB phosphorylation, and antagonizes full κ-opioid agonist and Dynorphin A (HY-P1333)-induced MAPK phosphorylation. Mianserin modulates social and exploratory behaviour, raises electroconvulsive thresholds. Mianserin can be used for the research of neurological disease, such as depression and epilepsy .
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- HY-B0188AS
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Mianserin-d3 hydrochloride is the deuterium labeled Mianserin. Mianserin (Mianserine) is an orally active H1 receptor antagonist. Mianserin can activate κ-opioid receptor and octopamine receptor. Mianserin increases ERK1/2 and CREB phosphorylation, and antagonizes full κ-opioid agonist and Dynorphin A (HY-P1333)-induced MAPK phosphorylation. Mianserin modulates social and exploratory behaviour, raises electroconvulsive thresholds. Mianserin can be used for the research of neurological disease, such as depression and epilepsy .
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- HY-B1203S
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Fludrocortisone-d5 (9α-Fludrocortisone-d5) is the deuterium labeled Fludrocortisone (HY-B1203). Fludrocortisone is an orally active mineralocorticoid and glucocorticoid receptor agonist. Fludrocortisone suppresses pro-inflammatory cytokine expression, reduces CCL2, IL-6, IL-8 levels, upregulates mineralocorticoid receptor (MR) expression, induces PI3K/Akt, GSK-3β, CREB, ERK1/2, mTOR phosphorylation, blocks Tau hyperphosphorylation, prevents apoptosis, promotes survival and proliferation, enhances renal sodium and water transport, increases plasma volume and blood pressure, reduces plasma potassium and renin activity, stimulates erythropoietin expression, modulates uterine receptivity genes, and reverses PP242-induced MUC1 upregulation. Fludrocortisone can be used for the research of congenital adrenal hyperplasia, postural hypotension, and adrenal insufficiency.
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- HY-B1203S1
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Fludrocortisone-d2 (9α-Fludrocortisone-d2) is the deuterium labeled Fludrocortisone (HY-B1203). Fludrocortisone is an orally active mineralocorticoid and glucocorticoid receptor agonist. Fludrocortisone suppresses pro-inflammatory cytokine expression, reduces CCL2, IL-6, IL-8 levels, upregulates mineralocorticoid receptor (MR) expression, induces PI3K/Akt, GSK-3β, CREB, ERK1/2, mTOR phosphorylation, blocks Tau hyperphosphorylation, prevents apoptosis, promotes survival and proliferation, enhances renal sodium and water transport, increases plasma volume and blood pressure, reduces plasma potassium and renin activity, stimulates erythropoietin expression, modulates uterine receptivity genes, and reverses PP242-induced MUC1 upregulation. Fludrocortisone can be used for the research of congenital adrenal hyperplasia, postural hypotension, and adrenal insufficiency.
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