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Filtered Search Results
Medchemexpress LLC AMG 579 | 1227067-61-9 | 99.0% | 50 MG
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AMG 579 is a potent, selective, and efficacious inhibitor of phosphodiesterase 10A (PDE10A) with an IC50 of 0.1 nM. It is intended for research use only. In vivo, AMG 579 has shown a statistically significant reduction of PCP-induced behavior in rats over a 2-hour period, with a minimum effective dose for efficacy in the PCP-LMA model determined to be 0.3 mg/kg. In dogs, it exhibits a superior oral bioavailability of 72%. One clinical trial (NCT01568203) is listed, sponsored by Amgen for Schizophrenia, with a start date of 2011-09, and it is in Phase 1.
- Potent, selective, and efficacious PDE10A inhibitor
- Demonstrates in vivo efficacy in reducing PCP-induced behavior in rats
- Exhibits superior oral bioavailability in dogs
- Underwent early-phase clinical trials for Schizophrenia
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Medchemexpress LLC IBT6A | 1022150-12-4 | 99.6% | 500 MG
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IBT6A is identified as an impurity of Ibrutinib and can be utilized in the synthesis of IBT6A Ibrutinib dimer and IBT6A adduct. Ibrutinib is a selective, irreversible Btk inhibitor. IBT6A can also be used in the synthesis of Ibrutinib and Ibrutinib-based activity-based probes (ABPs).
- Impurity of Ibrutinib
- Used in synthesis of Ibrutinib dimer and adduct
- Related to a selective, irreversible Btk inhibitor
- Utilized in synthesis of Ibrutinib and Ibrutinib-based activity-based probes (ABPs)
- Available as a white to yellow solid
- Molecular weight of 386.45
- Chemical formula is C22H22N6O
- Soluble in DMSO at 50 mg/mL (129.38 mM)
- Intended for research use only
- Long-term storage at -20°C for powder, -80°C for solvent
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Medchemexpress LLC MD2-TLR4-IN-1 | 2249801-12-3 | 98.2% | 10 MG
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MD2-TLR4-IN-1 is a myeloid differentiation protein 2/toll-like receptor 4 (MD2-TLR4) complex antagonist. It inhibits Lipopolysaccharides (LPS)-induced expression of TNF-α and IL-6 in macrophages with IC50 values of 0.89 μM and 0.53 μM, respectively. This compound can be utilized for the study of acute lung injury (ALI).
- Exerts anti-inflammatory activity by inhibiting NF-κB in RAW264.7 macrophages.
- Directly binds to the MD2-TLR4 complex and disrupts MD2-TLR4 activation.
- Suppresses NF-κB p65 subunit nuclear levels in LPS-induced macrophages.
- Significantly inhibits macrophage infiltration and ameliorates histopathological changes in lung tissues.
- Effectively reduces airspace inflammation and amends pulmonary lobule tissue structure.
- Decreases LPS-induced myeloperoxidase (MPO) activity and serum TNF-α levels.
- Reduces mRNA levels of TNF-α, IL-6, IL-1β, IL-12, IL-33, and COX-2 in lung tissues.
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Medchemexpress LLC Tivozanib hydrochloride hydrate | 682745-41-1 | 99.8% | 509.34 | 10 MG
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Tivozanib hydrochloride hydrate is the hydrate hydrochloride form of Tivozanib. It is a selective, orally active inhibitor for vascular endothelial growth factor receptor (VEGFR)-1, 2, and 3, with IC50s of 30, 6.5, and 15 nM, respectively. It exhibits antitumor efficacy.
- Selective, orally active inhibitor for VEGFR-1, 2, and 3.
- Exhibits antitumor efficacy.
- Inhibits the phosphorylation of VEGFR-1, VEGFR-2, and VEGFR-3.
- Inhibits VEGF-induced proliferation and migration of HUVECs.
- Selectively inhibits VEGF-stimulated phosphorylation of MAPKs in endothelial cells.
- Exhibits antitumor efficacy against various cancers in athymic mice models.
- Reversibly suppresses vascular permeability and angiogenesis.
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Medchemexpress LLC 4H-1-Benzopyran-4-one, 6-methoxy-5-nitro-2-(trifluoromethyl)- | 342795-08-8 | 99.85% | 289.16 | 50 MG
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Bragsin2 is a potent, selective, and noncompetitive nucleotide exchange factor BRAG2 inhibitor with an IC50 of 3 μM. It binds at the interface between the PH domain of BRAG2 and the lipid bilayer, preventing activation of lipidated Arf GTPase. This compound affects breast cancer stem cells.
- Potent, selective, and noncompetitive nucleotide exchange factor BRAG2 inhibitor with an IC50 of 3 μM.
- Binds at the interface between the PH domain of BRAG2 and the lipid bilayer.
- Leads to BRAG2 being unable to activate lipidated Arf GTPase.
- Affects breast cancer stem cells.
- Inhibits Arf GTPase activation in HeLa cells at 50 μM.
- Inhibits the growth of SUM149 and S68 cells at 50 μM.
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Medchemexpress LLC Apabetalone | 1044870-39-4 | 99.34% | 370.40 | 100 MG
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Apabetalone (RVX-208) is an inhibitor of BET transcriptional regulators, specifically targeting the second bromodomain (BD2) with high selectivity. It enhances the production of ApoA-I in hepatocytes, leading to an increase in high-density lipoprotein cholesterol (HDL-C). Its mechanism involves binding to bromodomains of the BET family by competing for acetylated lysine binding sites. This epigenetic modulation of ApoA-I production suggests it as a potential therapeutic agent for atherosclerosis.
- Selective BET transcriptional regulator inhibitor
- Targets the second bromodomain (BD2)
- Increases ApoA-I production in liver cells
- Elevates high-density lipoprotein cholesterol (HDL-C)
- Acts via an epigenetic mechanism
- Investigated for atherosclerosis treatment
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Medchemexpress LLC V-9302 | 1855871-76-9 | 99.5% | 538.68 | 100 MG
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V-9302 is a competitive antagonist of transmembrane glutamine flux. It selectively and potently targets the amino acid transporter ASCT2 (SLC1A5) but not ASCT1, inhibiting ASCT2-mediated glutamine uptake in HEK-293 cells.
- Selectively targets the amino acid transporter ASCT2 (SLC1A5) over ASCT1.
- Inhibits glutamine uptake (IC50=9.6 μM) in HEK-293 cells.
- Pharmacological blockade of ASCT2 leads to attenuated cancer cell growth and proliferation, increases cell death, and increases oxidative stress.
- Prevents tumor growth in HCT-116 and HT29 xenograft models (75 mg/kg; i.p.; daily for 21 days).
- When combined with CB-839, it elicits strong growth inhibition in SNU398 and MHCC97H xenograft models.
- High purity: 99.46%.
- Intended for research use only, not for sale to patients.
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![Medchemexpress LLC 2-Thiophenemethanamine, N-[(4-chloro-2-methylphenyl)methyl]-N-[(4-chlorophenyl)methyl]-5-nitro- (hydrochloride) | 98.5% | 457.80 | 10 MG](https://assets.fishersci.com/TFS-Assets/CCG/product-images/5000436961-Logo.png-250.jpg){kind=logo}
Medchemexpress LLC 2-Thiophenemethanamine, N-[(4-chloro-2-methylphenyl)methyl]-N-[(4-chlorophenyl)methyl]-5-nitro- (hydrochloride) | 98.5% | 457.80 | 10 MG
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GSK2945 hydrochloride is a tertiary amine, and is a highly specific Rev-erbα/REV-ERBα (mouse/human reverse erythroblastosis virus α) antagonist with EC50s of 21.5 μM and 20.8 μM, respectively. GSK2945 hydrochloride enhances cholesterol 7α-hydroxylase (CYP7A1) level and cholesterol metabolism. It is intended for research use only and is not sold to patients.
- Highly specific Rev-erbα/REV-ERBα antagonist
- Enhances cholesterol 7α-hydroxylase (CYP7A1) level
- Promotes cholesterol metabolism
- Increases the transcriptional activity of Rev-erbα
- Upregulates Lrh-1/LRH-1 mRNA and protein
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Medchemexpress LLC GNE-371 | 1926986-36-8 | 98.1% | 431.49 | 10 MG
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GNE-371 is a potent and selective chemical probe for the second bromodomains of human transcription-initiation-factor TFIID subunit 1 and transcription-initiation-factor TFIID subunit 1-like. It binds TAF1(2) with an IC50 of 10 nM, showing excellent selectivity over other bromodomain-family members. It is also active in a cellular TAF1(2) target-engagement assay (IC50=38 nM) and demonstrates anti-proliferative synergy with the BET inhibitor JQ1, supporting its use in mechanistic and target-validation studies.
- Potent and selective chemical probe for the second bromodomains of human transcription-initiation-factor TFIID subunit 1 and transcription-initiation-factor TFIID subunit 1-like.
- IC50 of 10 nM for TAF1(2).
- Active in a cellular TAF1(2) target-engagement assay (IC50=38 nM).
- Exhibits anti-proliferative synergy with the BET inhibitor JQ1.
- Appearance: Solid, white to off-white.
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Medchemexpress LLC GNE-371 | 1926986-36-8 | 98.06% | 431.49 | 100 MG
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GNE-371 is a potent and selective chemical probe designed to target the second bromodomains of human transcription-initiation-factor TFIID subunit 1 and transcription-initiation-factor TFIID subunit 1-like. It demonstrates an IC50 of 10 nM for TAF1(2).
- Potent and selective chemical probe for TAF1(2) bromodomains.
- Binds TAF1(2) with an IC50 of 10 nM.
- Maintains excellent selectivity over other bromodomain-family members.
- Active in cellular-TAF1(2) target-engagement assay (IC50=38 nM).
- Exhibits anti-proliferative synergy with the BET inhibitor JQ1.
- Supports use in mechanistic and target-validation studies.
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Medchemexpress LLC HY-N7128 100mg Medchemexpress, Flavanone CAS:487-26-3 Purity:>98%
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Medchemexpress, HY-N7128 100mg Flavanone CAS:487-26-3 Flavanone is used to characterize the authenticity of lemon juice by monitoring of flavanone content. Purity:>98% Medchemexpress has over 10000 novel life-science reagents, reference compounds, APIs and natural compounds for laboratory and scientific use. Other quantity can also be offered.
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eMolecules AstaTech / 5-BROMO-2-ETHOXYBENZAMIDE / 0.1g / 696739802 / A12625 / 95.000 / 54924-78-6 / MFCD07551819 / 244.088 / C9H10BrNO2
AstaTech / 5-BROMO-2-ETHOXYBENZAMIDE / 0.1g / 696739802 / A12625 / 95.000 / 54924-78-6 / MFCD07551819 / 244.088 / C9H10BrNO2
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eMolecules Medchem Express / Lofexidine (hydrochloride) / 50mg / 482204536 / HY-B1052 / / 21498-08-8 / MFCD00917022 / 295.590 / C11H13Cl3N2O
Medchem Express / Lofexidine (hydrochloride) / 50mg / 482204536 / HY-B1052 / / 21498-08-8 / MFCD00917022 / 295.590 / C11H13Cl3N2O
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eMolecules Medchem Express / Icotinib (Hydrochloride) / 5mg / 446265065 / HY-15164 / / 1204313-51-8 / MFCD22124500 / 427.890 / C22H22ClN3O4
Medchem Express / Icotinib (Hydrochloride) / 5mg / 446265065 / HY-15164 / / 1204313-51-8 / MFCD22124500 / 427.890 / C22H22ClN3O4
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Chem-Impex International, Inc. 2-Ethoxyphenylacetic acid | MFCD00016824 | 5G
2-Ethoxyphenylacetic acid, MFCD00016824, 5G
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