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Filtered Search Results
Apexbio Technology LLC AM966 1228690-19-4 200mg
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AM966 (CAS 1228690-19-4) is an orally bioavailable small-molecule antagonist that selectively targets Lysophosphatidic acid type 1 receptor (LPA1) AM966 exhibits potent inhibitory activity against LPA1 receptors from humans and mice with IC50 values of approximately 17 nM and 19 nM respectively demonstrating selectivity over other LPA receptor subtypes (LPA2 5) In vitro AM966 blocks LPA-mediated chemotactic responses in IMR-90 human lung fibroblasts A2058 human melanoma cells and CHO cell lines In vivo AM966 effectively attenuates lung fibrosis inflammation and associated weight loss in bleomycin-induced murine pulmonary fibrosis models highlighting its utility in research on fibrotic diseases
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Apexbio Technology LLC Veliparib dihydrochloride 912445-05-7 200mg
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Veliparib dihydrochloride (CAS 912445-05-7) is a selective inhibitor of poly(ADP-ribose) polymerases PARP1 and PARP2 enzymes responsible for DNA repair processes frequently upregulated in various cancers Veliparib inhibits PARP1 and PARP2 with K(i) values of 5 2 and 2 9 nmol/L respectively In colon cancer cell lines (HCT-116 HT-29) veliparib enhances DNA damage and induces G2/M arrest when combined with SN38 or oxaliplatin In preclinical murine melanoma (B16F10) breast cancer (MX-1) and colon cancer (HCT-116) xenografts combination therapy with DNA-damaging agents shows improved antitumor effects
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Medchemexpress LLC PVD-06 | 3032975-48-4 | 98.3% | 1074.13 | 25 MG
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PVD-06 is a selective PROTAC PTPN2 degrader with a DC50 of 217 nM (selectivity index >60-fold over PTP1B). It induces PTPN2 degradation via a VHL-, ubiquitin, and proteasome-dependent pathway. PVD-06 can promote T cell activation and amplify IFN-γ-mediated anticancer activity. It can be used to further investigate PTPN2 in diseases such as leukemia and melanoma.
- Induces PTPN2 degradation
- Reduces PTPN2 protein levels
- Enhances phosphorylation of STAT1 in Jurkat cells
- Promotes T cell proliferation under CD3/CD28 stimulation
- Amplifies B16F10 cell growth inhibition in the presence of IFN-γ
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Medchemexpress LLC PVD-06 | 3032975-48-4 | 98.3% | 1074.13 | 1 MG
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PVD-06 is a selective PROTAC PTPN2 degrader with a DC50 of 217 nM. It induces PTPN2 degradation via a VHL-, ubiquitin, and proteasome-dependent pathway. PVD-06 can promote T cell activation and amplify IFN-γ-mediated anticancer activity, making it suitable for investigating PTPN2 in diseases such as leukemia and melanoma.
- Selective PROTAC PTPN2 degrader
- Induces PTPN2 degradation via VHL-, ubiquitin, and proteasome-dependent pathway
- Promotes T cell activation
- Amplifies IFN-γ-mediated anticancer activity
- Composed of a PTPN2 ligand, a linker, and a VHL ligand
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Medchemexpress LLC SCH772984 | 942183-80-4 | 99.8% | C33H33N9O2 | 200 MG
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SCH772984 is a highly selective and ATP-competitive ERK inhibitor, with IC50s of 4 nM for ERK1 and 1 nM for ERK2. It exhibits antitumor activity in both MAPK inhibitor-naive and MAPK inhibitor-resistant cells that contain BRAF or RAS mutations.
- Highly selective and ATP-competitive ERK inhibitor
- Exhibits antitumor activity in MAPK inhibitor-naive and resistant cells
- Induces G1 arrest and apoptosis in sensitive melanoma cells
- Inhibits ERK and RSK phosphorylation
- Shows EC50 values less than 500 nM in BRAF-mutant and RAS-mutant tumor lines
- Leads to significant tumor regression in animal models
- Well tolerated in vivo
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Medchemexpress LLC Selumetinib | 606143-52-6 | 99.6% | C17H15BrClF4O3 | 200 MG
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Selumetinib is a selective, non-ATP-competitive oral MEK1/2 inhibitor with an IC50 of 14 nM for MEK1. It inhibits ERK1/2 phosphorylation and can penetrate the blood-brain barrier. This compound causes a time- and dose-dependent reduction in DNA synthesis and cell viability, inducing growth arrest and apoptosis associated with ERK inactivation.
- Selective, non-ATP-competitive oral MEK1/2 inhibitor
- Inhibits ERK1/2 phosphorylation
- Penetrates the blood-brain barrier
- Induces growth arrest and apoptosis
- Shows anti-proliferative effects
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Medchemexpress LLC Linifanib | 796967-16-3 | 99.4% | C21H18FN5O | 200 MG
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Linifanib (ABT-869) is a potent, orally active, multi-target inhibitor of the VEGFR and PDGFR family. It demonstrates prominent antitumor activity and has significantly less activity against unrelated RTKs, soluble tyrosine kinases, or serine/threonine kinases. Linifanib also acts as a specific miR-10b inhibitor, blocking miR-10b biogenesis.
- Potent and orally active multi-target inhibitor of VEGFR and PDGFR family
- Exhibits prominent antitumor activity
- Significantly less activity against unrelated RTKs, soluble tyrosine kinases, or serine/threonine kinases
- Acts as a specific miR-10b inhibitor, blocking miR-10b biogenesis
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Medchemexpress LLC (S,R,S)-AHPC-amido-C5-acid | 2162120-87-6 | 572.72 | 100 MG
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This product is (S,R,S)-AHPC-amido-C5-acid, a solid laboratory chemical identified as an E3 Ligase Ligand-Linker Conjugate involved in PROTAC design. It is used in the manufacture of various substances and for research purposes.
- Harmful if swallowed
- Causes skin irritation
- Causes serious eye irritation
- May cause respiratory irritation
- Stable under recommended storage conditions
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Medchemexpress LLC (S)-Rasagiline | 185517-74-2 | >98% | C12H13N | 200 MG
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(S)-Rasagiline (TVP1022) is the relatively inactive S-enantiomer form of Rasagiline. It is a highly potent, selective, irreversible MAO inhibitor with IC50s of 4.43 nM and 412 nM for rat brain MAO B and A activity, respectively. It also functions as a click chemistry reagent.
- Relatively inactive S-enantiomer form of rasagiline
- Highly potent, selective, irreversible MAO inhibitor
- IC50s of 4.43 nM and 412 nM for rat brain MAO B and A activity
- Functions as a click chemistry reagent
- Contains an alkyne group
- Undergoes copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing azide groups
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Medchemexpress LLC Sulfo-Cy5 azide | 1782950-80-4 | 98.97% | C37H48N6O10S3 | 100 MG
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Sulfo-Cy5 azide is a near-infrared fluorescent probe that exhibits favorable click chemistry reactivity. It is used for fluorescence imaging, tissue and cellular visualization, and site-specific modification of antibodies. It can also be applied for RNA labeling and imaging and conjugated to targeting agents for fluorescence imaging in models of atherosclerosis and breast cancer.
- Near-infrared fluorescent probe
- Favorable click chemistry reactivity
- Enables fluorescence imaging
- Used for tissue and cellular visualization of PD-L1 in tumors
- Allows site-specific modification of anti-PD-L1 antibodies
- Applicable for RNA labeling and imaging
- Can be conjugated to targeting agents for fluorescence imaging in atherosclerosis and breast cancer models
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Medchemexpress LLC Ipragliflozin | 761423-87-4 | 404.45 | 200 MG
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Ipragliflozin | 761423-87-4 | 404.45 | 200 MG
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Medchemexpress LLC Tamibarotene | 94497-51-5 | 99.57% | 351.44 | 200 MG
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Tamibarotene is an orally active retinoic acid receptor α (RARα) agonist, demonstrating high selectivity over RARγ. It is intended for research use only.
- Orally active retinoic acid receptor α (RARα) agonist
- High selectivity over RARγ
- Suitable for research use only
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Medchemexpress LLC ACT-1004-1239 | 2178049-58-4 | 98.8% | C27H28F2N6O3 | 1 ML
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ACT-1004-1239 is a potent, selective, orally active CXCR7 antagonist with an IC50 value of 3.2 nM. It is intended for research use only and not sold to patients.
- Inhibits human, dog, rat, mouse, guinea pig, and macaque CXCR7 with IC50s ranging from 0.6 to 3.2 nM.
- Promotes oligodendrocyte precursor cell (OPC) differentiation by increasing CXCL12 levels.
- Increases plasma CXCL12 concentration in vivo.
- Reduces disease severity in an EAE model.
- Increases myelination in a Cuprizone-induced demyelination model.
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Medchemexpress LLC Bromocriptine mesylate | 22260-51-1 | 99.9% | 750.70 | 50 MG
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Bromocriptine mesylate is a potent dopamine D2/D3 receptor agonist, binding to the D2 dopamine receptor with a pKi of 8.05. It is permeable to the blood-brain barrier. It stimulates [35S]-GTPγS binding at D2 dopamine receptors and acts as a strong inhibitor of brain nitric oxide synthase (neuronal NOS) and a potent inhibitor of CYP3A4.
- Potent dopamine D2/D3 receptor agonist
- Permeable to the blood-brain barrier
- Stimulates [35S]-GTPγS binding at D2 dopamine receptors
- Strong inhibitor of brain nitric oxide synthase (neuronal NOS)
- Potent inhibitor of CYP3A4
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Medchemexpress LLC 6-Bromoisoquinoline | 34784-05-9 | 98.2% | C9H6BrN | 25 G
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6-Bromoisoquinoline is a biochemical reagent used as a biological material or organic compound for life science research. It serves as a synthetic intermediate for pharmaceutical synthesis.
- Biochemical reagent for life science research
- Synthetic intermediate for pharmaceutical synthesis
- Store powder at -20°C for 3 years or 4°C for 2 years
- Store in solvent at -80°C for 6 months or -20°C for 1 month
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