ahr modulator-1

AhR modulator-1 is a selective and orally active aryl hydrocarbon receptor (AhR) modulator. It inhibits metastasis, in part, by inhibiting prostatic VEGF production prior to tumor formation. It also possesses anti-estrogenic properties in rat uterus.

ALDH2 modulator 1 is a potent, orally active modulator of acetaldehyde dehydrogenase-2 (ALDH2), which reduces blood alcohol levels in mice.

AMPA receptor modulator-1 can be activated by glutamate, thereby modulating ion channels.

Fluorogen binding modulator-1 (Fluorogen binding modulator-1) is a nonfluorescent inhibitors of Fluorogen–Fluorogen Activating Protein Binding Pairn.

CB2R FAAH modulator-1, a cannabinoid type 2 receptor (CB2R) agonist, is also a fatty acid amide hydrolase (FAAH) inhibitor (IC50=4 μM) that reduces the production of pro-inflammatory and anti-inflammatory cytokines and is commonly used in inflammation studies. The Kis for CB2R and CB1R are 14.8 nM and 241.3 nM, respectively.

Smurf-1 modulator CMP Example 20 (Smurf-1-IN-20) is a potent Smurf-1 modulator.

Calcium channel-modulator-1, a calcium channel-modulator (IC50: 0.8 μM), specializes in blocking aortic constriction.

CB2 modulator 1 is a potent CB2 modulator. It can be used for the research for immune disorders, osteoporosis, inflammation, renal ischemia.

gamma-secretase modulator 1 is a modulator of γ secretase and can be used in studies about the treatment of Alzheimer's disease.

S1PR1 modulator 1 is a selective inhibitor of S1PR1, with a pIC50 of 7.6.

5-HT1A modulator 1 exhibits high affinities for the 5-HT1A, α1-adrenergic receptor, and D2 receptor (IC50s = 2 nM, 10 nM, and 40 nM).

Kv3 modulator 1 is a voltage-gated potassium channel Kv3 modulator that can be used to study neurologic-level diseases.

Estrogen receptor modulator 1 causes regression of Tamoxifen-resistant, hormone-independent xenograft tumors. Estrogen receptor modulator 1 is an orally active and selective estrogen receptor modulator (SERM) (pIC50: 0.46).

mGluR3 modulator-1 (1-ethyl-3-(morpholin-4-yl)-5,6,7,8-tetrahydroisoquinoline-4-carbonitrile) is a positive allosteric modulator of mGluR3 and can be used in studies about the treatment of Parkinson's disease.

Nur77 modulator 1 is an effective Nur77 binder (KD = 3.58 μM) that up-regulates Nur77 expression, mediates its sub-cellular localization, induces Nur77-dependent ER stress and autophagy, and leads to cell apoptosis, demonstrating anti-hepatoma activity.

Mutant p53 modulator-1 is a mutant p53 modulator that hinders the progression of cancers containing p53 mutations.

KRAS G12D modulator-1 (compound 6), a potent modulator of KRAS G12D, exhibits IC50 values of 1-10 μM against NEA-G12D, PPI-G12D, and p ERK-AGS, and is utilized in cancer research [1].

Immuno modulator-1 (compound 22) effectively suppresses the secretion of TNFα and IL-2 in human peripheral blood mononuclear cells (hPBMC), with IC50 values of 4.7 nM and 26 nM, respectively, and exhibits a 20% inhibitory effect on the hERG potassium channel at a concentration of 3 μM [1].

β-Catenin modulator-1 (IIa-650) is a valuable agent in cancer research for modulating β-Catenin [1].

CRBN modulator-1 (WUN29654) is a Thalidomide analog and CRBN modulator,has an IC50 of 3.5 μM and a Ki of 0.98 μM.

Glucocorticoid receptor modulator 1 is a potent, orally active, non-steroidal selective glucocorticoid receptor modulator, exhibiting IC50 values of 9 nM and 130 nM against NF-κB and AP-1, respectively. It effectively reduces the expression of inflammatory factors such as IL-6, IL-1β, and TNF-α, and alleviates dermatitis in mice.

Ras modulator-1 is a chemical compound that modulates the activity of Ras.

RNA Splicing Modulator 1 (Compound 233) is a modulator of RNA splicing, exhibiting an AC50 value of less than 100 nM [1].

Nrf2-ARE hMAO-B QR2 modulator 1, a new resveratrol-based multitarget-directed ligand (MTDL), exhibits a well-balanced MTDL profile: it activates the NRF2-ARE pathway (CD = 9.83 μM), selectively inhibits both hMAO-B and QR2 (IC50s = 8.05 and 0.57 μM), and effectively promotes hippocampal neurogenesis. It exerts neuroprotective and antioxidant actions in both acute and chronic Alzheimer models using hippocampal tissues.

AhR Ligand-Linker Conjugates 1, also known as E3 Ligase Ligand-Linker Conjugates 57, is a chemical compound that combines an IAP ligand for the E3 ubiquitin ligase with a SNIPER linker. It is specifically designed to be used in the development of SNIPER[1].

MRGPRX4 modulator-1 (compound 31-2) is a potent antagonist of the mas-related G-protein receptor X4 (MRGPR X4) with an IC50 < 100 nM against MRGPR4, utilized for investigating MRGPR X4-dependent diseases including itch, pain, and autoimmune disorders [1].

CD33 splicing modulator 1 (Compound 1) is a CD33 splicing modulator that targets the CD33 Siglec 3 myeloid cell surface receptor, known for regulating microglial cell activity, and holds potential for studying neurodegenerative diseases such as Alzheimer's disease.

NOT Receptor Modulator 1 (2-(3-(2-(4-chlorophenyl)imidazo[1,2-a]pyridin-6-yl)phenyl)propan-2-ol) is a modulator of nuclear receptor NOT.

RIG-1 modulator 1 is useful for the treatment of viral infections including influenza virus, HBV, HCV and HIV.

GPR120 modulator 1 is useful for modulating GPR120.

Opioid receptor modulator 1 is a modulator of the opioid receptor.

TRPC5 modulator-1 (Compound 9) is a TRPC5 modulator with an IC50 of less than 1 nM, suitable for studying neuropsychiatric disorders.

Utrophin Modulator 1 (UM1) is a highly effective agent that upregulates utrophin protein levels, displaying an EC 50 of 0.11 μM. Its application in the investigation of Duchenne Muscular Dystrophy (DMD) has been well-established [1].

IL-17 Modulator 1 (disodium) is a potent, orally active compound, known for its high efficacy in modulating IL-17. This compound is extensively utilized for researching various diseases such as psoriasis, ankylosing spondylitis, and psoriatic arthritis[1].

CXCR7 modulator 1 is an effective and orally bioavailable peptoid hybrid CXCR7 modulator with Ki of 9 nM.

DPP-4 GPR119 modulator 1 (Compound 22) is an orally active compound that acts as both a dipeptidyl peptidase IV (DPP-IV) inhibitor and GPR119 agonist, demonstrating a glucose-lowering effect in blood and moderate inhibition of the hERG channel with an IC50 value of 4.9 µM. This compound is applicable in diabetes research [1].

Autotaxin modulator 1 is a new modulator of Autotaxin.

GPR40/FFAR1 modulator 1 is a Gq-coupled free fatty acid receptor 1 (GPR40/FFAR1) agonist and allosteric modulator.

CXCR4 modulator-1 (compound ZINC72372983) is a potent CXCR4 modulator (EC50 = 100 nM) with research value in anti-inflammatory, anticancer, and anti-HIV studies.

NR2F6 modulator-1 is a potent modulator of nuclear receptor subfamily 2, group F, member 6 (NR2F6), used to study immune regulation and modulation of tumour stem cell activity.

Orexin Receptor Modulator-1 is a compound utilized in the study of various conditions including substance addiction, panic disorder, anxiety, post-traumatic stress disorder (PTSD), pain, depression, seasonal affective disorder (SAD), eating disorders, and hypertension [1].

THR-β Modulator-1 (Compound 1a) is a potent modulator of the thyroid hormone receptor β, utilized in the study of thyroid hormone receptor-associated disorders [1].

Compound 38-S is an orally active CB1R/AMPK modulator with a K i of 0.81 nM and an IC50 of 3.9 nM for CB1R. This compound activates AMPK and has been shown to decrease food intake and body weight, in addition to enhancing glucose tolerance and insulin sensitivity [1].

α7β1 Integrin Modulator-1 is a potent modulator with research potential for muscular dystrophy [1].

hA2A/hCA XII modulator 1 is a potent antagonist of the hA2A adenosine receptor (hA2AAR), a triazolopyrazine that acts on hA2AAR (Ki: 6.4 nM), hA1AR (Ki: 4.819 μM), and hA3AR (Ki>30 μM). hA2A/hCA XII modulator 1 Also a potent inhibitor of human carbonic anhydrase XII (hCA XII), capable of acting on hCA XII (Ki: 6.2 nM), hCA II (Ki: 46 nM), hCA IX (Ki: 466 nM) and hCA I (Ki: 8.351 μM). hA2A/hCA XII modulator 1 exhibits potential for cancer research.

5-HT6R MAO-B modulator 1 is an antagonist of 5-HT6R (at Gs signaling) and an irreversible inhibitor of MAO-B that exhibits glial protective activity and induces scopolamine-induced memory deficits.

CB1R Allosteric Modulator 1 (compound 11) is a potent allosteric modulator of CB1Rs, negatively affecting the functional activity of orthosteric ligands [NAM] at CB1Rs.