brd4 inhibitor-10

BRD4 Inhibitor-10 is an inhibitor of BRD4-BD1 (IC50: 8 nM).

Prolyl-4-hydroxylase Inhibitor 11, a novel proline 4-hydroxylase inhibitor, shows protective effects against oxidative stress and Cu(II) toxicity in Chlorella vulgaris.

p53-Mdm2 inhibitor 4 inhibits the p53-MDM2 protein-protein interaction.

4-(2-fluorophenyl)-2,3-dihydro-1,3-thiazol-2-one is a thiazol-2-one analog that has been found to possess anti-inflammatory, antibacterial, antifungal, and antitumor activities.

Dynorphin A (1-10) acetate is an endogenous opioid neuropeptide, binds to extracellular loop 2 of the κ-opioid receptor. Dynorphin A (1-10) also blocks NMDA-activated current with an IC50 of 42.0 μM.

p38α inhibitor 4 is a selective MAPK p38α inhibitor, which is used to study diabetes, pain and chronic inflammation.

MINA53 inhibitor (Compound 10) is an inhibitor of MINA53.

BRD4 Inhibitor-27 is a potent BRD4 inhibitor that inhibits BRD4 BD1 and BRD4 BD2 with IC50s of 9.6 and 11.3 μM, respectively.BRD4 Inhibitor-27 has anticancer activity and can be used for breast cancer research.

Highy selective and potent NK2 receptor agonist (IC50 = 6.1 nM). Induces contraction of the rat fundus and bladder (EC50 values are 117 and 10 nM respectively).

4,4-dimethyl-2,3,4,5-tetrahydro-1H-1,5-benzodiazepin-2-one is a benzodiazepine derivative. It is an orthosteric modulator of the GABAA receptor and selectively binds to the benzodiazepine site of the GABAA receptor. It has anxiolytic, anticonvulsant and sedative activity.

Adrenocorticotropic Hormone (ACTH) (4-10) TFA (Acth (4-10)) is an agonist of potent melanocortin(MC4R) receptor .

Pim-1 kinase inhibitor 4 is a potent Pim-1 kinase inhibitor with an IC50 value of 17.01 nM.Pim-1 kinase inhibitor 4 also possesses antioxidant activity and potential anticancer activity, and inhibits DPPH.Pim-1 kinase inhibitor 4 promotes apoptosis and inhibits the growth of PC-3 cells with an IC50 value of 16 nM. Pim-1 kinase inhibitor 4 promotes apoptosis and inhibits PC-3 cell growth with an IC50 of 16 nM. Pim-1 kinase inhibitor 4 can be used in prostate cancer research.

Neurokinin A(4-10) TFA(97559-35-8 free base) is a tachykinin NK2 receptor agonist[1].

GSK-3 inhibitor 4 is an orally active and brain-permeable triple inhibitor of GSK-3, CDK2 and CDK5 with inhibitory effects on GSK-3β, GSK-3α, CDK2 and CDK5, with IC50 values of 0.56 nM, 0.45 nM, 0.47 μM, 0.68 μM, respectively.GSK-3 inhibitor 4 can effectively reduce Tau protein levels. GSK-3 inhibitor 4 can effectively reduce the level of Tau protein.GSK-3 inhibitor 4 can be used in the study of Alzheimer's disease.

Chitin synthase inhibitor 4 is a chitin synthase (CHS) inhibitor with antimicrobial activity.Chitin synthase inhibitor 4 is a CHS-based compound and a candidate fungicide.

IL-4 inhibitor is an inhibitor of IL-4.1It binds to IL-4 with a Kdvalue of 1.8 μM and inhibits IL-4 activity in a cell-based reporter assay (EC50= 1.81 μM). It is selective for IL-4 over IL-13 (EC50= 18.2 μM). IL-4 inhibitor inhibits IL-4-induced STAT6 phosphorylation in THP-1 monocytes (EC50= 3.1 μM), indicating inhibition of the IL-4-JAK1-STAT6 signaling pathway.

Tuberculosis Inhibitor 10 moderately inhibits the enzyme MSMEG_6649 and potentiates the antimycobacterial activity of PAS [1].

WRN Inhibitor 4 (Example 107), a cyclic vinyl sulfone-based compound, serves as an inhibitor of the Werner Syndrome ATP-dependent helicase enzyme (WRN). This inhibitor is applicable in cancer research [1].

Adrenocorticotropic Hormone (ACTH) (4-10) is an agonist of potent melanocortin(MC4R) receptor .

[bAla8]-Neurokinin A(4-10) is a neurokinin 2 (NK2) receptor agonist.

ChoKα Inhibitor-4 is a bioisosteric agent that effectively inhibits human choline kinase α1 (HChoK α1) with an IC50 of 0.66 μM. It demonstrates both inhibitory and antiproliferative effects on cancer cells, induces apoptosis through the mitochondrial pathway, and diminishes the expression of anti-apoptotic proteins [1].

17-oxo-4(Z),7(Z),10(Z),13(Z),15(E),19(Z)-Docosahexaenoic acid is a metabolite of lipoxygenase-mediated oxidation of DHA that is produced endogenously by aspirin-enhanced COX-2 activity. It has been shown to activate Nrf2-dependent antioxidant gene expression, to act as a PPARγ agonist (EC50 = ~200 nM), and to inhibit pro-inflammatory cytokine and nitric oxide production at biological concentration ranges (5-25 μM).

BRD4-IN-4 is a selective BRD4 inhibitor with an IC50 value of 6.83 μM for BRD4.BRD4-IN-4 selectively inhibits the proliferation of the MV4-11 cell line and arrests the cells in G1 phase.BRD4-IN-4 can be used to study MLL leukemias.

JNK3 Inhibitor-4, a potent 2-aryl-1-pyrimidinyl-1H-imidazole-5-yl acetonitrile derivative, demonstrates a strong inhibitory effect on JNK3 with an IC 50 value of 1.0 nM. It exhibits exceptional selectivity against JNK3 when compared to other protein kinases, including isoforms JNK1 (IC 50 = 143.9 nM) and JNK2 (IC 50 = 298.2 nM). Additionally, JNK3 Inhibitor-4 benefits from neuroprotective properties and is predicted to permeate the blood-brain barrier effectively.

Neurokinin A(4-10)(TFA) is an agonist of tachykinin NK2 receptor .

Angiogenesis Inhibitor 4 is a potent agent for inhibiting angiogenesis, with potential applications in cancer research [1].

IRAK-4 protein kinase inhibitor 2 is a potent interleukin-1 receptor-associated kinase-4 (IRAK-4) inhibitor(IC50 = 4 μM).

Dynorphin A (1-10) (TFA), an endogenous opioid neuropeptide, binds in the transmembrane domain of the κ-receptor.

Wnt pathway inhibitor 4 is a small molecule antimicrobial agent with antibacterial and antiproliferative activity against cancer cells.

Compound 13, a topoisomerase I inhibitor 10, selectively inhibits leishmanial topoisomerase IB and exhibits antileishmanial activity. Specifically, it demonstrates efficacy against L. donovani promastigotes with an IC50 value of 27.91 μM [1].

Sodium Channel Inhibitor 4 is a compound that functions as a sodium channel inhibitor [1].

MARK4 inhibitor 4, with an IC50 value of 1.49 μM, serves as an agent targeting MARK4 for potential use in research related to cancer and tauopathies [1].

Hydroxy-2,6,10-trimethyl-2,6,11-dodeca-4-one is a naturally occurring compound present in the Solanaceae family [1].

RIP2 Kinase Inhibitor 4 is a highly potent and selective RIPK2 PROTAC compound that efficiently degrades RIPK2 (with a pIC50 value of 8) and effectively inhibits the release of TNF-α.

BRD4 Inhibitor-24 is a BRD4 small molecule inhibitor with antitumor activity.

MAT2A inhibitor 4 is an inhibitor of the catalytic subunit of methionine S-adenosyltransferase-2, which is used in cancer research.

Bromodomain inhibitor-10 (compound 128) is a highly potent inhibitor of bromodomain activity. It exhibits strong binding affinity with K d values of 15.0 nM and 2500 nM for BRD4-1 and BRD4-2, respectively. Furthermore, Bromodomain inhibitor-10 effectively inhibits the production of IL12p40 [1].

BRD4 Inhibitor-28 (Compound 18), an orally active molecule, selectively inhibits the bromodomains of BRD4 (BRD4-BD1 and BRD4-BD2) with IC50 values of 15 and 55 nM, respectively. It also demonstrates inhibition of BRD2-BD1, BRD3-BD1, and BRDT-BD1 with IC50 values of 19, 25, and 68 nM, respectively. Furthermore, this compound exhibits anti-melanoma activity [1].

Cav 3.2 Inhibitor 4 (Compound 21) is a selective and potent inhibitor of the T-type calcium channel (Ca v 3.2), demonstrating peripheral restriction with an IC50 value of 0.6 μM. It is utilized in atrial fibrillation research [1].

Glyoxalase I inhibitor 4 is a potent inhibitor of glyoxalase I (GLO1) (Ki: 10 nM).

1,3-dihydroxy-4-methoxy-10-methylacridin-9-one is a natural product for research related to life sciences. The catalog number is TN2491 and the CAS number is 1189362-86-4.

PI3Kγ inhibitor 4 is a selective, potent, orally active PI3Kγ inhibitor (IC50: 40 nM). PI3Kγ inhibitor 4 is ~7-fold more selective for PI3Kγ than the α subtype, 43-fold more selective than the β subtype and 18-fold more selective than the δ subtype. inflammation.

KRAS G12D Inhibitor 10 is a potent agent targeting the KRAS G12D mutation, a variant in the Ras protein family crucial for cellular growth and development. This compound shows promise for investigating cancers mediated by KRAS G12D.

BRM/BRG1 ATP Inhibitor-4, a potent inhibitor of BRG1/BRM, is utilized in the research of cancers and BAF complex-related disorders.

URAT1 Inhibitor 4, derived from Lesinurad, is a potent, orally active inhibitor of URAT1 with an IC50 value of 7.56 μM, demonstrating greater in vivo urate-lowering efficacy than Lesinurad [1].

ERK1/2 Inhibitor 5, a potent suppressant of the ERK1/2 pathway, is instrumental in the mitogen-activated protein kinase (MAPK) signal transduction pathway, where extracellular signal-regulated kinase (ERK) serves as a critical component of the MAPK family. This compound holds promise for the investigation or mitigation of cancer, inflammation, or various proliferative diseases[1].

Neurokinin A (4-10) TFA is a tachykinin NK 2 receptor agonist [1] .

Ac-[Nle4,D-Phe7]-α-MSH (4-10)-NH2, a melanotropin derivative and melanocyte-stimulating hormone, activates tyrosinase and demonstrates a thermoregulatory effect in rat models [1] [2].

(p-Iodo-Phe7)-ACTH (4-10), a derivative of adrenocorticotrophic hormone (ACTH) produced by the anterior pituitary gland, functions as a melanocortin (MC) receptor antagonist. It effectively inhibits α-melanocyte-stimulating hormone (α-MSH)-induced excessive grooming behavior in rats [1].

FSH receptor-binding inhibitor fragment (bi-10) is a potent antagonist that inhibits the binding of follicle-stimulating hormone (FSH) to its receptor (FSHR), modifying FSH activity at the receptor level. It suppresses ovulation and induces follicular atresia in mice. Furthermore, this compound holds potential for curbing ovarian cancer carcinogenesis by reducing the overexpression of FSHR and estrogen receptor beta (ERβ) in the ovaries [1].