molecule activator

VVD-130037 is a small molecule activator specifically targeting Kelch-like ECH-associated protein 1 (KEAP1) with potential antitumor activity.VVD-130037 inhibits tumor growth in advanced solid tumors by degrading NRF2.

Butyzamide is an effective and oral Mpl activator. It is a novel non-peptide-based molecule with antagonistic effects on thrombopoietin (TPO) receptors, which promotes proliferation of human Mpl (hMpl) expression and mouse pro B cell line Ba F3. The phosphorylation of JAK2, STAT3, STAT5 and MAPK is induced. Butyzamide has been shown to help increase platelet levels in mouse xenotransplantation trials.

Stemazole is a novel small molecule human stem progenitor cell proliferation activator that promotes the survival of human embryonic stem cells and maintains stemness, and promotes the survival of oligodendrocyte precursor cells in vitro. Stemazole significantly increased cell survival and clone formation in a dose-dependent manner, reduced apoptosis, and promoted recovery of motor dysfunction and myelin repair. Stemazole can be used as a therapeutic agent in demyelinating disorders, promoting OPC survival in vitro and regeneration in vivo.

PF-03382792 is a small molecule 5-HT4 receptor activator for the study of Alzheimer's disease.

Birinapant (TL32711) is a synthetic small molecule that is both a peptidomimetic of second mitochondrial-derived activator of caspases (SMAC) and inhibitor of IAP (Inhibitor of Apoptosis Protein) family proteins, with potential antineoplastic activity.

Kevetrin hydrochloride (4-Isothioureidobutyronitrile hydrochloride) is a small molecule and activator of the tumor suppressor protein p53, with potential antineoplastic activity.

ML198 is a novel activator and non-inhibitory chaperone of glucocerebrosidase. ML198 serves as a starting point to develop a novel approach towards small molecule treatment for patients suffering from Gaucher disease.

Isovalerylcarnitine (3-methylbutyrylcarnitine) is a small molecule compound produced by the catabolism of L-leucine and the accumulation of isovaleric acid. Isovalerylcarnitine is also a selective and effective calpain activator that can promote cell apoptosis. Isovalerylcarnitine is related to isovaleric acidemia and can be used as a marker of isovaleric acidemia.

2-AHA-cAMP is an analog of the natural signaling molecule cAMP and an activator of cAMP-dependent protein kinase. It features a free terminal primary amine group that can be used for coupling to gels or fluorescent dyes.

Atiprimod is an orally bioavailable small molecule belonging to the azaspirane class of cationic amphiphilic agents with anti-inflammatory, antineoplastic, and antiangiogenic properties. Atiprimod inhibits the phosphorylation of signal transducer and activator of transcription 3 (STAT3), blocking the signalling pathways of interleukin-6 and vascular endothelial growth factor (VEGF) and downregulating the anti-apoptotic proteins Bcl-2, Bcl-XL, and Mcl-1, thereby inhibiting cell proliferation, inducing cell cycle arrest, and inducing apoptosis.

Fasoracetam monohydrate is a small synthetic molecule and a metabotropic glutamate receptor activator, which has previously undergone extensive Phase I-III clinical trials in humans for vascular dementia.

STING agonist-11 is a potent activator of the small molecule cyclic urea class of STING (EC50: 18 nM).STING activation is a highly promising immunotherapy.

Norswertianolin, a compound isolated from G. acuta, is a small molecule activator of CSE, which enhances the H-generation 2S activity of CSE and can be used in the study of cardiovascular diseases.

BC-1258 is a unique small molecule F-box LRR-repeat protein 2 (FBXL2) activator.

2'-O-Me-cAMP is an analog of the natural signaling molecule cAMP and serves as a selective activator for the cAMP-activated exchange factor (Epac), characterized by its low membrane permeability.

8-CPT-cAMP-AM is a highly membrane-permeable analog of the signaling molecule cAMP. It serves as an activator for both cAMP and cGMP-dependent protein kinases, as well as Epac (exchange protein activated by cAMP).

STING agonist-10 is a potent activator of the STING small molecule cyclic urea class (EC50: 2600 nM).STING activation is a highly promising immunotherapy.

JH-131e-153, a diacylglycerol (DAG)-lactone, serves as a small molecule activator for the C1 domain of Munc13-1, exhibiting an activation hierarchy of WT>I590≈R592A≈W588A. This compound's C1 domain shares sequence and structure homology with protein kinase C (PKC), with an activation preference of PKCα>Munc13-1>PKCε. JH-131e-153 is implicated in the modulation of neuronal processes and holds potential for research in neurodegenerative diseases [1].

CDN1163 is a small molecule activator of sarco endoplasmic reticulum Ca2+-ATPase (SERCA).

Gingerenone A is an effective Nrf2-Gpx4 activator. It is a small molecule compound isolated from ginger. It has anti-cancer activity, can prolong the cell cycle of cancer cells, and can inhibit dextran sodium sulfate (DSS)-induced colitis. Ferroptosis in secondary liver injury (SLI) in mice.

STING agonist-23 (CF510) is a non-nucleotide, small-molecule activator of the STING pathway. It initiates the phosphorylation of STING, TBK1, and IRF3, enhancing the production of IFN-β, IL-6, CXCL-10, TNF-α, ISG-15, and CCL-5 in tumor cells. Notably, it demonstrates activity against SARS-CoV series strains [1].

Tirasemtiv (CK-2017357)(CK 2017357) is a small-molecule fast-skeletal-troponin activator, with a potential treatment for muscle weakness and neuromuscular dysfunction.

NAMPT activator-6, a regulatory molecule for the optical control system of NAMPT and NAD+, can be used to design efficient photoswitchable proteolysis-targeting chimeras (PS-PROTACs) for light-dependent, reversible regulation of NAMPT and NAD+, thereby reducing toxicity associated with inhibitor-based PS-PROTACs. This enables antitumor activity and in vivo modulation of NAMPT and NAD+ through optical manipulation [1].

CTX1 is a small molecule activator of p53.