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Filtered Search Results
MEDCHEMEXPRESS LLC Romaciclib monohydrochloride | 2443816-41-7 | 99.3% | 450.60 | 25 MG
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Romaciclib monohydrochloride is an ATP-competitive and selective CDK8 inhibitor. It inhibits kinase activities of CDK8/CycC and CDK19/CycC complexes with IC50s of 4.4 nM and 10.4 nM, respectively, and has a Kd of 3 nM for CDK8. It weakly inhibits CDK9 but shows no significant activity against CDK1, 2, 4, 6, 5, or 7. This compound inhibits phosphorylation of STAT1 S727 and STAT5 S726, demonstrating anti-tumor activity.
- ATP-competitive and selective CDK8 inhibitor.
- Inhibits kinase activities of CDK8/CycC and CDK19/CycC complexes.
- Weakly inhibits CDK9 and shows no obvious activity against several other CDKs (CDK1, 2, 4, 6, 5, 7).
- Inhibits phosphorylation of STAT1 S727 and STAT5 S726.
- Possesses anti-tumor activity.
- Decreases IRF9 and STAT1 mRNA expression and mitogen-induced IER expression.
- Inhibits growth of AML tumors in a dose-dependent manner in SCID mice.
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MEDCHEMEXPRESS LLC BSJ-03-204 (triTFA) | 99.9% | 1174.97 | 25 MG
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BSJ-03-204 triTFA is a PROTAC connected by ligands for Cereblon and CDK. It is a potent and selective Palbociclib-based CDK4/6 dual degrader, with IC50s of 26.9 nM for CDK4/D1 and 10.4 nM for CDK6/D1. This compound does not induce IKZF1/3 degradation and demonstrates anti-cancer activity.
- PROTAC connected by ligands for Cereblon and CDK.
- Potent and selective Palbociclib-based CDK4/6 dual degrader.
- Demonstrates potent anti-proliferative effects on MCL cell lines.
- Induces a G1 arrest.
- Selectively degrades CDK4/6 in WT cells without affecting IKZF1/3 degradation.
- Exhibits anti-cancer activity.
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MEDCHEMEXPRESS LLC IKK 16 | 873225-46-8 | 99.9% | 483.63 | 200 MG
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IKK 16 is an orally active IKK inhibitor that targets IKK2, IKK complex, IKK1, and LRRK2. It also acts as a pan-PKD inhibitor and an ABCB1 inhibitor. IKK 16 provides protection against LPS-induced multiple organ dysfunction, aids in restoring renal function and reducing fibrosis in acute kidney injury, and lessens cardiac dysfunction linked to polymicrobial sepsis in type 2 diabetes mellitus models by inhibiting the NF-κB pathway.
- Orally active IKK inhibitor
- Targets IKK2, IKK complex, IKK1, and LRRK2
- Pan-PKD and ABCB1 inhibitor
- Protects against LPS-induced multiple organ dysfunction
- Restores renal function and reduces fibrosis in acute kidney injury
- Lessens cardiac dysfunction in polymicrobial sepsis in T2DM models
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MEDCHEMEXPRESS LLC m-PEG15-amine | 100MG
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m-PEG15-amine | 100MG
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MEDCHEMEXPRESS LLC MSA-2 | 129425-81-6 | 99.8% | 294.32 | 200 MG
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MSA-2 is a potent and orally available non-nucleotide STING agonist that binds to STING as a noncovalent dimer with nanomolar affinity. It stimulates interferon-β secretion in tumors, induces tumor regression with durable antitumor immunity, and synergizes with anti-PD-1 in syngeneic mouse tumor models.
- Potent and orally available non-nucleotide STING agonist
- Binds to STING as a noncovalent dimer with nanomolar affinity
- Stimulates interferon-β secretion in tumors
- Induces tumor regression with durable antitumor immunity
- Synergizes with anti-PD-1 in syngeneic mouse tumor models
- Achieves comparable exposure in tumor and plasma
- Exhibits dose-dependent antitumor activity
- Induces elevations of IFN-β, IL-6, and TNF-α in tumors
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MEDCHEMEXPRESS LLC DOTMA | 104872-42-6 | 99.91% | 670.57 | 200 MG
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DOTMA is a cationic lipid used as a non-viral vector for gene therapy. It is a component of liposomes for encapsulating siRNA, microRNA, and oligonucleotides, and for in vitro gene transfection. DOTMA promotes effective interaction between liposomes and cell membranes by inducing positive charge on the liposomes. It has demonstrated good gene transfection effects both in vitro and in vivo.
- Cationic lipid
- Non-viral vector for gene therapy
- Component of liposomes for encapsulating siRNA, microRNA, and oligonucleotides
- Used for in vitro gene transfection
- Promotes effective interaction between liposomes and cell membranes
- Induces positive charge on liposomes
- Good gene transfection effects both in vitro and in vivo
- High intravenous transfection activity in CD-1 mouse
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MEDCHEMEXPRESS LLC Revumenib | 2169919-21-3 | 99.99% | 630.82 | 200 MG
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Revumenib (SNDX-5613) is a potent and specific Menin-MLL inhibitor with a binding Ki of 0.149 nM and a cell-based IC50 of 10-20 nM. It is intended for the research of MLL-rearranged (MLL-r) acute leukemias, including acute lymphoblastic leukemia (ALL) and acute myeloid leukemia (AML). For research use only; not for sale to patients.
- Potent and specific Menin-MLL inhibitor.
- Applicable for research in MLL-rearranged acute leukemias (ALL and AML).
- Shows in vivo plasma IC50 of 53 nM.
- Provides significant survival benefit and leukemic control in aggressive MOLM-13 disseminated xenografts in vivo.
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MEDCHEMEXPRESS LLC Amino-PEG3-C2-sulfonic acid | 1817735-43-5 | 99.47% | 257.30 | 100 MG
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Amino-PEG3-C2-sulfonic acid is a PEG-based PROTAC linker utilized in the synthesis of PROTACs. PROTACs consist of two distinct ligands connected by a linker, with one targeting an E3 ubiquitin ligase and the other targeting the protein of interest. PROTACs exploit the intracellular ubiquitin-proteasome system to selectively degrade target proteins.
- Utilized in the synthesis of PROTACs
- Contains two distinct ligands connected by a linker
- Exploits intracellular ubiquitin-proteasome system
- Selectively degrades target proteins
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MEDCHEMEXPRESS LLC Tamoxifen | 10540-29-1 | 99.96% | 371.51 | 200 MG
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Tamoxifen is an orally active, selective estrogen receptor modulator (SERM) that blocks estrogen action in breast cells and can activate estrogen activity in other cells, such as bone, liver, and uterine cells. It is a potent Hsp90 activator, enhancing the Hsp90 molecular chaperone ATPase activity. It activates autophagy and induces apoptosis. Tamoxifen can also be dissolved in corn oil for use in inducing gene knockout in CreER transgenic mice.
- Orally active, selective estrogen receptor modulator (SERM)
- Blocks estrogen action in breast cells
- Can activate estrogen activity in bone, liver, and uterine cells
- Potent Hsp90 activator
- Enhances Hsp90 molecular chaperone ATPase activity
- Inhibits infectious EBOV Zaire and Marburg (MARV) with IC50 values of 0.1 μM and 1.8 μM
- Activates autophagy and induces apoptosis
- Can be dissolved in corn oil for gene knockout in CreER transgenic mice
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MEDCHEMEXPRESS LLC 2-(2,6-Dioxopiperidin-3-yl)phthalimidine | 26581-81-7 | 99.7% | 244.25 | 200 MG
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2-(2,6-Dioxopiperidin-3-yl)phthalimidine (EM-12) is a teratogenic Thalidomide analogue that is more active than Thalidomide and is more stable for hydrolysis. It enhances 1,2-dimethylhydrazine-induction of rat colon adenocarcinomas. It is an off-white to gray solid.
- Teratogenic thalidomide analogue
- More active than thalidomide
- More stable to hydrolysis
- Enhances 1,2-dimethylhydrazine-induction of rat colon adenocarcinomas
- Off-white to gray solid
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MEDCHEMEXPRESS LLC L-azidonorleucine (hydrochloride) | 1454334-76-9 | 98.0% | 200 MG
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L-Azidonorleucine hydrochloride is an unnatural amino acid that serves as a methionine surrogate. It is used to label mammalian cell proteins and identify various methionyl-tRNA synthetase (MetRS) mutants. This compound functions as a click chemistry reagent due to its azide group, which enables copper-catalyzed azide-alkyne cycloaddition (CuAAc) reactions with alkyne-containing molecules. It can also participate in strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.
- Unnatural amino acid and methionine surrogate
- Labels mammalian cell proteins
- Identifies methionyl-tRNA synthetase (MetRS) mutants
- Functions as a click chemistry reagent
- Enables copper-catalyzed azide-alkyne cycloaddition (CuAAc) reactions
- Participates in strain-promoted alkyne-azide cycloaddition (SPAAC) reactions
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MEDCHEMEXPRESS LLC BPTES | 314045-39-1 | 98.0% | 200 MG
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BPTES is an allosteric and selective glutaminase inhibitor with an IC50 of 0.16 μM. It is for research use only.
- Inhibits glutaminase activity
- Diminishes glutamate and α-KG levels
- Increases glycolytic intermediates
- Inhibits PDAC cell proliferation
- Slows growth of mutant IDH1 cells
- Shows synergistic anti-cancer effect with 5-FU in A549 and EKVX cell lines
- Reduces growth in most NSCLC cell lines
- Reduces levels of TCA cycle metabolites
- Reduces ATP production
- Attenuates tumor growth in patient-derived pancreatic orthotopic tumor models
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MEDCHEMEXPRESS LLC (S,R,S)-AHPC-amido-C5-acid | 2162120-87-6 | >99.5% | 25 MG
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(S,R,S)-AHPC-amido-C5-acid is a laboratory chemical identified by CAS number 2162120-87-6. It is supplied as a solid and exhibits chemical stability under recommended storage conditions, making it suitable for various research applications.
- Stable under recommended storage conditions.
- Solid appearance.
- Suitable for laboratory chemical applications.
- Recommended storage at -20°C, sealed, away from moisture and light.
- Shipping at room temperature if less than two weeks.
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MEDCHEMEXPRESS LLC Romaciclib monohydr | 1 ML
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Romaciclib monohydr | 1 ML
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MEDCHEMEXPRESS LLC Adavosertib 200mg | 10 MG
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Adavosertib 200mg | 10 MG
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