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Results for "

modulation

" in TargetMol Product Catalog
  • Inhibitors & Agonists
    139
    TargetMol | Inhibitors_Agonists
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    TargetMol | Inhibitors_Agonists
Y-27632 dihydrochloride
Y-27632 2HCl
T1725129830-38-2
Y-27632 dihydrochloride (Y-27632 2HCl) is an orally potent, ATP-competitive inhibitor of ROCK-I and ROCK-II. Y-27632 dihydrochloride also inhibits isolation-induced apoptosis in mouse prostate stem or progenitor cells.
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XU1
Benzo[c][1,8]naphthyridin-6(5h)-One
T2917053439-81-9In house
XU1(Benzo[c][1,8]naphthyridin-6(5h)-One) is an Aurora protein kinase inhibitor used for the treatment of diseases suitable for inhibition, regulation or modulation of kinase signaling.
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6-8 weeks
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CGP 20376
CGP-20376, CGP20376
T3081981059-04-3In house
CGP 20376 is a benzothiazole compound, an anthelmintic, with dual dose-dependent modulation of in vitro effects on the respiratory burst of eosinophils and antifibrillatory properties.
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8-10weeks
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Viloxazine
Viloxazin, Emovit
T6032546817-91-8In house
Viloxazine (Viloxazin) (Viloxazin) is a dual-action compound that functions as a norepinephrine reuptake inhibitor and exhibits potent agonistic activity towards 5-HT 2C receptors while acting as an antagonist for 5-HT 2B receptors, with respective potency values of EC 50 = 32 μM and IC 50 = 27 μM. Its primary mechanism of action involves the modulation of serotonergic and noradrenergic pathways. Viloxazine is commonly employed in depression research [1] [2].
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6-8 weeks
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Ceramides Mixture
T10760100403-19-8
Ceramides Mixture, an endogenous ceramide, consists of hydroxy and non-hydroxy fatty acid-containing ceramides. It is involved in the regulation of cell cycle arrest, growth inhibition, and modulation of telomerase activity.
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2,2,5,7,8-Pentamethyl-6-Chromanol
PMC
T14008950-99-2
2,2,5,7,8-Pentamethyl-6-Chromanol (PMC) is the antioxidant component of vitamin E (α-tocopherol) and exhibits significant androgen receptor (AR) signaling modulation and anti-cancer activity against prostate cancer cell lines.
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Chrysotoxine
Phenol, 4-[2-(3,4-dimethoxyphenyl)ethyl]-2,6-dimethoxy-, 4-[2-(3,4-Dimethoxyphenyl)ethyl]-2,6-dimethoxyphenol
T27012156951-82-5
Chrysotoxine (Phenol, 4-[2-(3,4-dimethoxyphenyl)ethyl]-2,6-dimethoxy-) inhibits 6-hydroxydopamine induced apoptosis in SH-SY5Y cells via NF-κB modulation and mitochondria protection.
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shp099
SHP099 free base, SHP-099, SHP 099
T35641801747-42-1
SHP099 (SHP099 free base) free base is an effective, selective, orally bioavailable, and efficacious SHP2 inhibitor (IC50 =0.07 μM and p-ERK modulation in cells IC50 = 0.250 μM). SHP099 shows dose-dependent pathway inhibition and antitumor activity in xenograft models.
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Punicalagin
T392165995-63-3
Punicalagin is a major ellagitannin found in pomegranates that is reported to produce antioxidant, anti-inflammatory, and anticancer effects. It has been shown to prevent high-fat diet-induced obesity-associated accumulation of cardiac triglyceride and ch
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AMAROGENTIN
T549721018-84-8
Amarogentin is mainly extracted from Swertia and Gentiana roots. It plays cemopreventive therapeutic role during liver carcinogenesis through modulation of cell cycle and apoptosis
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Flavokawain B
Flavokavain B, Flavokawin B, 2'-Hydroxy-4',6'-Dimethoxychalcone
T6S07351775-97-9
1. Flavokawain B (Flavokavain B) has potent anti-inflammatory activity, can significantly inhibit production of NO and PGE2 in LPS-induced RAW 264.7 cells. 2. Flavokawain B, the hepatotoxic constituent from kava root, induces GSH-sensitive oxidative stress through modulation of IKK NF-κB and MAPK signaling pathways. 3. Flavokawain B induces apoptosis, has the potential usefulness of FKB for prevention and treatment of hormone-refractory prostate cancer in an adjuvant setting. 4. Flavokawain B acts through ROS generation and GADD153 up-regulation to regulate the expression of Bcl-2 family members, thereby inducing mitochondrial dysfunction and apoptosis in HCT116 cells.
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Oroxylin A
Baicalein 6-methyl ether, 6-Methoxybaicalein
T6S1315480-11-5
1. Oroxylin A (Baicalein 6-methyl ether) has various anti-tumor effects including apoptosis, cell cycle arrest, drug-resistant reversion. 2. Oroxylin A possesses abilities of inhibiting the ATRA-induced IL-6 production via modulation of LAP LIP CHOP in leukemia cell lines, which could providing a therapeutic strategy for RAS. 3. Oroxylin A inhibits UCP2s triggers the MPTP opening, and promotes the apoptosis in CaCo-2 cells; uncoupling protein 2 plays a key role in mitochondrial apoptotic pathway. 4. Oroxylin A inhibits N1ICD translocating to the nucleus and binding to epithelial-mesenchymal transition-related transcription factor Snail, thus suppressing the invasion and migration of MCF-7 cells. 5. Oroxylin A improves the sensitivity of K562 ADM cells by increasing apoptosis in leukemic cells and decreasing the expression of CXCR4 and PI3K Akt NF-κB pathway, and probably served as a most promising agent for CML treatment.
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Cynarin
Cynarine, Cyclohexanecarboxyli​c acid, 1,​3-​bis[[3-​(3,​4-​dihydroxyphenyl)​-​1-​oxo-​2-​propen-​1-​yl]​oxy]​-​4,​5-​dihydroxy-​, (1R,​3R,​4S,​5R)​-, 1,5-Dicaffeoylquinic acid
T6S152930964-13-7
Cynarin (1,5-Dicaffeoylquinic acid) has neuroprotective, and antioxidant effects, it can inhibition of GSK3β as well as the modulation of Bcl-2 Bax.
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Shogaol
[6]-Shogaol, 6-Shogaol
T6S1699555-66-8
1. 6-Shogaol (6-Shogaol) has antipyretic and analgesic effects in addition to inhibitory effect on lipoxygenase activity. 2. 6-shogaol has anti-inflammatory property, reduces the inflammatory response and protected the femoral cartilage from damage produced in a CFA monoarthritic model of the knee joint of rats. 3. 6-Shogaol inhibits the growth of human cancer cells and induces apoptosis in COLO 25 cells through modulation of mitochondrial functions regulated by reactive oxygen species (ROS). 4. 6-Shogaol effectively inhibit invasion and metastasis of hepatocellular carcinoma through diverse molecular mechanisms, including inhibition of the MAPK and PI3k Akt pathways and NF-κB and STAT3 activities to suppress expression of MMP-2 -9 and uPA and block angiogenesis, could further regulate urokinase-type plasminogen activity.
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Rosmanol
T703380225-53-2
Rosmanol has antioxidant activity, it can activate the antioxidant response element. Rosmanol has biphasic modulation of GABAA receptors, demonstrates CNS activity in mouse models of antinociception, antidepressant and anxiolysis. Rosmanol potently induce
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5'-N-Ethylcarboxamidoadenosine
NECA
T734035920-39-9
5'-N-Ethylcarboxamidoadenosine (NECA), an agonist of the Adenosine receptor, increases cerebral extravasation of fluorescein and low molecular weight dextran independent of blood-brain barrier modulation.
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Nitroaspirin
NCX 4016
T16328175033-36-0
Nitroaspirin (NCX 4016) is a nitric oxide donor and a nitro-derivative of Aspirin that inhibits cyclooxygenase. It induces cell cycle arrest and apoptosis in Cisplatin-resistant human ovarian cancer cells by down-regulating EGFR PI3K STAT3 signaling and modulating Bcl-2 family proteins. Additionally, Nitroaspirin possesses antithrombotic and antiplatelet properties and acts as a direct and irreversible inhibitor of COX-1.
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COR659
T36520544450-68-2
COR659 is a GABAB positive allosteric modulator (PAM) . COR659 suppresses alcohol and chocolate self-administration in rats[1]. COR659 apparently exerts its effects via a composite mechanism, including positive allosteric modulation of the GABAB receptor and an action at the cannabinoid CB1 receptor[3]. COR659 (0, 2.5, 5 and 10 mg kg) treatment is completely ineffective on lever-responding (FR10) for regular food pellets in food-deprived Wistar rats[1].COR659 is able to suppress lever-responding for a sucrose solution in sP rats and a chocolate solution in Wistar rats[2]. Animal Model: Male sP and Wistar rats[1]. [1]. Paola Maccioni, et al. Suppressing effect of COR659 on alcohol, sucrose, and chocolate self-administration in rats: involvement of the GABA B and cannabinoid CB 1 receptors. Psychopharmacology (Berl). 2017 Sep;234(17):2525-2543. [2]. Francesca Ferlenghi, et al. The GABA B receptor positive allosteric modulator COR659: In vitro metabolism, in vivo pharmacokinetics in rats, synthesis and pharmacological characterization of metabolically protected derivatives. Eur J Pharm Sci. 2020 Dec 1;155:105544. [3]. Paola Maccioni, et al. Anti-addictive properties of COR659 - Additional pharmacological evidence and comparison with a series of novel analogues. Alcohol. 2019 Mar;75:55-66.
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6-8 weeks
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NR2F6 modulator-1
T62204904449-84-9
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.
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6-8 weeks
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(+)-Dropropizine
(+)-Dropropizine
T0217L99291-24-4
(+)-Dropropizine can inhibit histamine receptor, anti-allergic, and reduce a cough by modulation of neuropeptides involved in the cough reflex and by interfering with stimulus activation of peripheral endings of sensory nerves.
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gamma-secretase modulator 2
T113591093978-89-2
Gamma-secretase modulator 2 is a potent, selective compound for the treatment of Alzheimer's disease, specifically designed to modulate γ-secretase activity. This modulation selectively attenuates the production of Aβ(1-42), addressing diseases associated with Aβ deposition in the brain, particularly Alzheimer's disease.
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6-8 weeks
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RR-11a
T127691361390-56-8
RR-11a is a synthetic enzyme legumain inhibitor. This compound specifically targets and inhibits the activity of legumain, an enzyme implicated in various biological processes. RR-11a's synthetic nature allows for precise modulation of legumain activity, making it a valuable tool in biochemical research and potential therapeutic applications.
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7-10 days
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(R)-BAY1238097
T134421564269-85-7
(R)-BAY1238097 represents the R-isomer of BAY1238097, which exhibits relatively lower activity compared to its counterpart. BAY1238097 is a highly potent and selective inhibitor targeting the binding of BET proteins to histones, demonstrating significant anti-proliferative effects in various acute myeloid leukemia (AML) and multiple myeloma (MM) models. The high activity is achieved through the down-regulation of c-Myc levels and the subsequent modulation of its downstream transcriptome.
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6-8 weeks
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AP5
T135501623194-37-5
AP5 is a potent and selective agonist for the GPR40 receptor with positive allosteric modulation of endogenous ligands (AgoPAM). AP5 demonstrates a rat hIP1 EC50 of 0.49 nM against the GPR40 receptor.
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3-6 months
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