creb

PI3K/Akt/CREB Activator 1 is a potent, orally active compound that acts as an activator for the PI3K/Akt/CREB pathway. It enhances neuronal proliferation, induces differentiation of Neuro-2a cells into neuron-like morphology, and accelerates axon-dendrite polarization in primary hippocampal neurons by upregulating brain-derived neurotrophic factor. This compound is utilized in vascular dementia (VaD) research.

CREB-IN-1 TFA is a potent and orally active CREB inhibitor with an IC50 of 0.18 μM, exhibiting inhibitory effects on the growth of breast cancer cells.

666-15 (CREB inhibitor) is a potent and selective CREB inhibitor (IC50: 81 nM).

CREBtide acetate is a synthetic substrate for PKA (Km=3.9 μM), which is based on the phosphorylation sequence in d-CREB (cAMP response element binding protein).

Crebinostat is a potent histone deacetylase (HDAC) inhibitor, targeting HDAC1, HDAC2, HDAC3, and HDAC6 with IC50s of 0.7 nM, 1.0 nM, 2.0 nM, and 9.3 nM, respectively. It increases the density of synapsin-1 punctae along dendrites in neurons in vitro, modulates chromatin-mediated neuroplasticity, and enhances memory in mice. Additionally, Crebinostat induces histone H3 and H4 acetylation and enhances the expression of Egr1, a cAMP-responsive element binding protein (CREB) target gene.

Curcumin (Natural Yellow 3) is a phenolic natural product, an inhibitor of histone acetyltransferase p300/CREB (IC50=25 μM) with specificity. Curcumin has a wide range of pharmacological activities such as antitumor, anti-inflammatory and antioxidant.

Naphthol AS-E (nAS-E) is an the KIX-KID interaction and CREB-mediated gene transcription inhibitor.

1. Crebanine iv 5mg/kg can eonvert BaCl_2-induced arrhythmia into sinus rhythm in rats, and can significantly increase the tolerant dose of aconitine to produce ventrieular fibrillation(VF) and cardiac arrest (CA) in rata. 2. Crebanine can also decrease t

ICG001 antagonizes Wnt β-catenin TCF-mediated transcription and specifically binds to element-binding protein (CREB)-binding protein (CBP) with IC50 of 3 μM, but is not the related transcriptional coactivator p300.

Phanginin A, a potent and orally active activator of salt-induced kinase 1 (SIK1), effectively inhibits gluconeogenesis, increases the expression of p-SIK1, and decreases the expression of p-CREB. By reducing blood glucose levels and enhancing glucose tolerance and dyslipidemia, Phanginin A holds potential for type 2 diabetes research.

L-692429 (MK-0751) is a potent nonpeptidyl growth hormone secretagogue (GHS) agonist and benzolactam derivative, known for reversing glucocorticoid-induced inhibition of GH secretion. L-692429 exhibits high affinity for the G protein-coupled receptor and is useful in studying acromegaly and obesity.

CREBtide is a synthetic substrate for PKA (Km=3.9 µM), which is based on the phosphorylation sequence in d-CREB (cAMP response element binding protein).

Tylocrebrine is anticancer agent.

Crebanine N-oxide is a useful organic compound for research related to life sciences. The catalog number is T126510 and the CAS number is 102719-85-7.

Dehydrocrebanine has strong activity against promyelocytic leukemia cells (HL-60) with an IC50 of 2.14 ug/mL. It also shows potent antimalarial activity with an IC50 value of 70 ng/ml.

Ep300 CREBBP-IN-8 (Example 37), a potent and orally active inhibitor of Ep300 and CREBBP, shows IC50 values of 0.014 μM and 0.018 μM, respectively, and is utilized in cancer research [1].

Ep300 CREBBP-IN-3 (Example 61), a potent inhibitor of Ep300 and CREBBP with IC50 values of 0.056 μM and 0.095 μM, respectively, is applicable in cancer research [1].

Ep300 CREBBP-IN-2 (Example 73) is a potent, orally bioavailable inhibitor of Ep300 and CREBBP, with IC50 values of 0.052 μM and 0.148 μM, respectively, and is used in cancer research [1].

Oxocrebanine, an aporphine alkaloid present in Fissistigma poilanei (Annonaceae) [1], is identified as a constituent of this botanical species.

CREBBP-IN-9, a CREBBP inhibitor, acts on the bromodomain of the protein.

Ep300 CREBBP-IN-4 (Example 56), a potent inhibitor of both Ep300 and CREBBP, shows IC50 values of 0.024 μM and 0.064 μM, respectively, and is employed in cancer research [1].

KG-501 (Naphthol AS-E phosphate) is a cAMP response element-binding protein (CREB) inhibitor(IC50 : 6.89 μM).

ICG-001 antagonizes Wnt/β-catenin/TCF-mediated transcription and specifically binds to element-binding protein (CBP) with IC50 of 3 μM, but is not the related transcriptional coactivator p300.

Anacardic Acid (6-pentadecylsalicylic Acid) is an effective inhibitor of p300 and p300 CBP-associated factor histone acetyltranferases. It also has antimicrobial activity, antibacterial activity, and inhibits prostaglandin synthase, lipoxygenase, and tyrosinase.

EML 425 is a potent and selective inhibitor of CREB binding protein (CBP)/p300 (IC50s: 2.9 and 1.1 μM, respectively).

3,5,6,7,8,3',4'-Heptemthoxyflavone exhibits neuroprotective, chemopreventive, anti-allergic, anti-inflammatory, immunomodulatory, anti-aging, and photoprotective effects; it inhibits collagenase activity, induces type I procollagen synthesis in HDFn cells, and combats nitric oxide (NO) carcinogenesis.

653-47 hydrochloride is a potentiator, significantly potentiates the cAMP-response element binding protein (CREB) inhibitory activity of 666-15. It is also a very weak CREB inhibitor with IC50 of 26.3 μM.

PF-CBP1 HCl is a highly selective inhibitor of the bromodomain of CREB-binding protein(CREBBP). It inhibits CREBBP (IC50: 125 nM) and p300 bromodomains (IC50: 363 nM).

MS7972 is CREBBP inhibitor that blocks human p53 and CREB binding protein association. MS7972 can almost completely block this BRD interaction at 50 μM

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.

MS2126 is a Human p53 and CREB Binding Protein interaction inhibitor.

5-OH-HxMF is an inducer of neurite growth in PC12 cells through the camp / PKA / CREB pathway.

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.

DC-CPin7, a powerful inhibitor of the bromodomain of CREB-binding protein (CBP), exhibits an IC50 value of 2.5 μM [1].

DC-CPin711, a potent and selective inhibitor of the bromodomain of CREB-binding protein (CBP) with an IC50 of 0.0626 μM, effectively halts the cell cycle at the G1 phase and promotes apoptosis [1].

Phoenixin-20 (TFA) (PNX-20 (TFA)) is a bioactive peptide that stimulates hypothalamo-pituitary-gonadal hormones, regulates mammalian reproductive processes, enhances neuronal mitochondrial biogenesis via the CREB-PGC-1α pathway, and exhibits anxiolytic properties [1] [2] [3].

PF-CBP1 hydrochloride (PF-CBP1 HCl) is a highly selective inhibitor of the bromodomain of CREB-binding protein(CREBBP).It inhibits CREBBP and p300 bromodomains with IC50 of 125 and 363 nM respectively.

4′-Demethylnobiletin, a bioactive metabolite, activates the PKA/ERK/CREB signaling pathway, enhances CRE-mediated transcription in hippocampal neurons, and reverses memory impairment linked to NMDA receptor antagonism through ERK signaling stimulation [1].

653-47 acts as a potentiator significantly enhancing the inhibitory activity of 666-15 on the cAMP-response element binding protein (CREB), while it also exhibits mild CREB inhibitory properties itself, with an IC50 value of 26.3 μM [1].

CRT5, a pyrazine benzamide, is a potent and selective PKD inhibitor. It inhibits VEGF-induced phosphorylation of three PKD substrates (IC50s = 1, 2, and 1.5 nM for PKD1, PKD2, and PKD3, respectively), histone deacetylase 5, CREB (cAMP-response-element-binding protein), and HSP27 (heat-shock protein 27) at Ser82. Additionally, CRT5 decreases VEGF-induced endothelial migration, proliferation, and tubulogenesis[1].

Asperosaponin VI (Akebia saponin D) , the most abundant constituent of the rhizome of Dipsacus asper, has been used for the treatment of lower back pain, traumatic hematoma and bone fractures.

Praeruptorin A ((+)-Praeruptorin A) has the potential to inhibit migration/fusion of preosteoclasts in vitro and bone erosion in vivo by targeting calmodulin and inhibiting the Ca(2+)/calmodulin-CaMKIV-CREB-NFATc1 and/or Ca(2+)/calmodulin-calcineurin-NFATc1 signaling axis.

CAY10669 is an inhibitor of the histone acetyltransferase PCAF (p300/CREB-binding protein-associated factor; IC50 = 662 μM), displaying a 2-fold improvement in inhibitory potency over anacardic acid . At 30-60 μM, CAY10669 can dose-dependently inhibit histone H4 acetylation in HepG2 cells in vitro.

Spadin TFA, a natural peptide originating from a propeptide in blood, acts as a powerful TREK-1 channel inhibitor with an IC 50 of 10 nM. It boosts dorsal raphe nucleus 5-HT neurotransmission in mice, activates hippocampal CREB, and promotes neurogenesis. This compound is useful for antidepressant research [1] [2].

Crocin II (Crocetin gentiobiosylglucosyl ester) has anti-inflammatory and anti-apoptotic effects against gastric ischemia-reperfusion injury in rats, the effect of crocin is mainly mediated by reducing the protein expression of iNOS and caspase-3. Crocin II can ameliorate CCl4-induced liver injury via inhibition of inflammatory cytokines, caspase3 and oxidative stress along with modulation of liver metabolizing enzymes favoring elimination of CCl4 toxic metabolite. Crocin II has antihyperlipidemic effect, may be due to the inhibition of pancreatic lipase and crocin, and its metabolite, Crocin II , can improve hyperlipidemia. Crocin has antidepressant effects by increasing CREB, BDNF and VGF levels in hippocampus.

Sekikaic acid is a phenolic lichen metabolite that has been found in H. obscurata and has diverse biological activities. It scavenges superoxide and DPPH radicals in cell-free assays when used at a concentration of 0.5 µM. Sekikaic acid is active against the rg recombinant strain of respiratory syncytial virus (RSV; IC50 = 5.69 µg/ml). It inhibits the protein-protein interaction between mixed lineage leukemia 1 (MLL1) and the GACKIX domain of CREB-binding protein (CBP; IC50 = 34 µM).

XX-650-23 is a small molecule CREB inhibitor that blocks the critical interaction between CREB and its required coactivator, CBP (CREB-binding protein), inducing apoptosis and cell cycle arrest in AML cells, and can be used in the study of acute myelogenous leukaemia (AML).

Bryonolic acid (20-epi-Bryonolic acid), a triterpenoid extracted from Sandoricum indicum, possesses immunomodulatory, anti-inflammatory, antioxidant and anticancer activities and protects PC12 cells from NMDA-induced apoptosis by inhibiting Ca2+ in-flux and modulating gene expression in the Ca2+-CaMKII-CREB signalling pathway.

NASTRp, an inhibitor of CREB-CBP complex, possesses anti-cancer effects along with cell cycle regulation, autophagy suppression, and endoplasmic reticulum stress.

6-O-Isobutyrylbritannilactone, a sesquiterpene natural melanogenesis inhibitor, can be extracted from Inula britannica flowers. It effectively suppresses IBMX-induced melanin production in B16F10 cells and exerts antimelanogenic effects in zebrafish embryo models by modulating ERK, PI3K/AKT, and CREB pathways [1].