1639159-47-9
1639159-47-9
Chemical Structure
UniPR129
- CAS. Nr.: 1639159-47-9
- Formula:C36H52N2O4
- Molecular Weight:576.81
IUPAC Name: (S)-3-((R)-4-((3R,5R,8R,9S,10S,13R,14S,17R)-3-hydroxy-10,13-dimethylhexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)pentanamido)-4-(1H-indol-3-yl)butanoic acid
InChIKey: JGYYGEYIQBZUCC-ZOOAIUBFSA-N
SMILES: C[C@@]12[C@](CC[C@]2([H])[C@H](C)CCC(N[C@H](CC(O)=O)CC3=CNC4=CC=CC=C34)=O)([H])[C@@]5([H])[C@]([C@@]6([C@](C[C@H](O)CC6)([H])CC5)C)([H])CC1
Biological Activity: UniPR129 is a potent and orally active Eph/ephrin antagonist. UniPR129 can inhibit EphA2-ephrin-A1 interaction with an IC50 of 945 nM and a Ki of 370 nM. UniPR129 can inhibit angiogenesis and show antitumor and neuroprotective effect. UniPR129 can be used for the researches of cancer and neurological disease, such as colorectal cancer and optic neuropathy[1][2][3][4].
| Art. -Nr. | Produktname | Reinheit | Beschreibung | Pricing | |||||||||||||||||||
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UniPR129 | 99.09% | UniPR129 is a potent and orally active Eph/ephrin antagonist. UniPR129 can inhibit EphA2-ephrin-A1 interaction with an IC50 of 945 nM and a Ki of 370 nM. UniPR129 can inhibit angiogenesis and show antitumor and neuroprotective effect. UniPR129 can be used for the researches of cancer and neurological disease, such as colorectal cancer and optic neuropathy. | ||||||||||||||||||||
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UniPR1331 | 99.77% | UniPR1331 is an orally active 3β-hydroxy-Δ5-choline acid derivative that inhibits Eph-ephrin interactions. UniPR1331 blocks the interaction of VEGFR2 with its natural ligand vascular endothelial growth factor and inhibits subsequent autophosphorylation, signaling, and pro-angiogenic activation of endothelial cells. UniPR1331 exhibits anti-angiogenesis, anti-cancer and anti-inflammation effects. UniPR1331 can be used for the researches of cancer and inflammation, such as glioma and colitis. | ||||||||||||||||||||
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UniPR505 | 99.68% | UniPR505 (Compound 14) is an EphA2 antagonist with an IC50 of 0.95 µM. UniPR505 displays anti-angiogenic properties. | ||||||||||||||||||||
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UniPR1447 | 99.46% | UniPR1447 is Dual EphA2 and EphB2 antagonist, with an IC50 of 6.6 μM for EphA2−ephrin-A1 binding. | ||||||||||||||||||||
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Antibacterial agent 258 | Antibacterial agent 258 (Compound 11e) is an antibacterial agent, that destory the bacteria cell membrane, and inhibits various gram-positive bacteria (MIC for Staphylococcus aureus is 1-2 μg/mL). Antibacterial agent 258 exhibits low hemolytic activity and low cytotoxicity. Antibacterial agent 258 exhibits anti-infectious efficacy in mouse models. | |||||||||||||||||||||
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UniPR500 | UniPR500, a UniPR129 derivative, is a competitive EphA2 receptor antagonist with a Ki of 0.78 μM. UniPR500 dose-dependently reduces binding of biotinylated ephrin-A1 to EphA2 with an IC50 value of 1.1 μM. | |||||||||||||||||||||
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ST6GAL1-IN-1 | 99.33% | ST6GAL1-IN-1 is an orally active selective ST6GAL1 inhibitor (IC50 = 20 μM). ST6GAL1-IN-1 exhibits high antimetastatic potential, effectively inhibiting the migration of MDA-MB-231 cells at noncytotoxic concentrations. ST6GAL1-IN-1 can disrupt integrin sialylation in MDA-MB-231 cells. ST6GAL1-IN-1 inhibits tumor angiogenesis and cancer metastasis via the Integrin/VEGFR2-mediated signaling pathway. ST6GAL1-IN-1 effectively suppresses both tumor growth and cancer metastasis on the MDA-MB-231 xenograft model. ST6GAL1-IN-1 can be used for the study of Triple-negative breast cancer (TNBC). | ||||||||||||||||||||
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HBV/HDV-IN-5 | HBV/HDV-IN-5 (example 4) is an inhibitor of hepatitis B virus (HBV) and hepatitis D virus (HDV). | |||||||||||||||||||||
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N-Choloylphenylalanine | 93.70% | N-Choloylphenylalanine (Compound 6273) (PheCA) is a VPR-induced growth arrest inhibitor. N-Choloylphenylalanine alleviates VPR-induced growth arrest. N-Choloylphenylalanine can be used in yeast and HIV-1 infection research. | ||||||||||||||||||||
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Cholyl-L-tyrosine | Cholyl-L-tyrosine (TyrCA) is a cholyl conjugate of L-tyrosine (HY-N0473). Cholyl-L-tyrosine can be effectively hydrolyzed by pancreatic juice. | |||||||||||||||||||||
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Tryptophan-cholic acid | 99.75% | Tryptophan-cholic acid (Trp-CA) is a microbial amino acid-conjugated bile acid that acts as an endogenous ligand and agonist (EC50=9.6 μM) for the orphan G protein-coupled receptor (GPCR) MRGPRE (Mas-related G protein-coupled receptor family member E). Tryptophan-cholic acid is orally effective but has poor oral absorption and does not cross the blood-brain barrier. Tryptophan-cholic acid promotes the secretion of glucagon-like peptide GLP-1, thereby improving glucose tolerance in diabetic mice. Tryptophan-cholic acid improves glucose tolerance, promotes insulin secretion, and alleviates high-fat diet-induced hepatic steatosis without causing pruritus side effects. Tryptophan-cholic acid is primarily used in research on type 2 diabetes (T2D). | ||||||||||||||||||||
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References
- [1]. Hassan-Mohamed I, et al. UniPR129 is a competitive small molecule Eph-ephrin antagonist blocking in vitro angiogenesis at low micromolar concentrations. Br J Pharmacol. 2014 Dec;171(23):5195-208. [Content Brief]
- [2]. Corrado M, et al. Evaluation of the Anti-Tumor Activity of Small Molecules Targeting Eph/Ephrins in APC min/J Mice. Pharmaceuticals (Basel). 2020 Apr 16;13(4):69. [Content Brief]
- [3]. Strong TA, et al. Activation of multiple Eph receptors on neuronal membranes correlates with the onset of optic neuropathy. Eye Vis (Lond). 2023 Oct 2;10(1):42. [Content Brief]
- [4]. Giorgio C, et al. Pharmacological evaluation of new bioavailable small molecules targeting Eph/ephrin interaction. Biochem Pharmacol. 2018 Jan;147:21-29. [Content Brief]
