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Nutlin-3 is a commercial available p53-MDM2 inhibitor, with K i of 90 nM. Uses: Scientific research. Group: Signaling pathways. CAS No. 548472-68-0. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 25 mg; 50 mg; 100 mg. Product ID: HY-50696.
Nutlin-3
Nutlin-3 is an MDM2 antagonist, inhibiting p53-Mdm2 interaction (IC50=0.09 μM) via affecting p53 binding pocket of MDM2. It has been studied in anticancer reseaches. Synonyms: (±)-4-[4,5-Bis(4-chlorophenyl)-2-(2-isopropoxy-4-methoxy-phenyl)-4,5-dihydro-imidazole-1-carbonyl]-piperazin-2-one; 4-[4,5-bis(4-chlorophenyl)-2-(4-methoxy-2-propan-2-yloxyphenyl)-4,5-dihydroimidazole-1-carbonyl]piperazin-2-one. Grades: >98%. CAS No. 548472-68-0. Molecular formula: C30H30Cl2N4O4. Mole weight: 581.49.
Cell-permeable. Nutlin-3 is a Mdm2 (mouse double minute 2) antagonist (IC50=90nM for Nutlin-3a and 13.6uM for Nutlin-3b), p53 pathway activator, and apoptosis inducer. Group: Biochemicals. Grades: Highly Purified. CAS No. 548472-68-0. Pack Sizes: 1mg, 5mg. US Biological Life Sciences.
Worldwide
Nutlin-3a
Nutlin-3a is an inhibitor of MDM2 (human homolog of murine double minute 2), which disrupts its interaction with p53, leading to the stabilization and activation of p53. Nutlin-3a activates the p53 pathway and efficiently induces apoptosis in tumours with amplified MDM2 gene and overexpression of MDM2 protein. Synonyms: rebemadlin; (-)-Nutlin-3; Nutlin-3a chiral. Grades: >98%. CAS No. 675576-98-4. Molecular formula: C30H30Cl2N4O4. Mole weight: 581.5.
Nutlin-3a
Nutlin-3a (Rebemadlin), an active enantiomer of Nutlin-3, is a potent murine double minute (MDM2) inhibitor ( IC 50 =90 nM). Nutlin-3a inhibits MDM2-p53 interactions and stabilizes the p53 protein, and induces cell autophagy and apoptosis. Nutlin-3a has the potential for the study of TP53 wild-type ovarian carcinomas [1] [2]. Uses: Scientific research. Group: Signaling pathways. Alternative Names: Rebemadlin. CAS No. 675576-98-4. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 25 mg; 50 mg; 100 mg. Product ID: HY-10029.
Nutlin-3b
Nutlin-3b, the active enantiomer of Nutlin-3, inhibits the p53/MDM2 interaction with IC50 of 90 nM. Synonyms: Nutlin-3; nutlin 3; Nutlin 3b; FJA1772CVW; (+)-Nutlin-3; CHEMBL2152332; CHEBI:46742; 4-[(4R,5S)-4,5-Bis(4-chlorophenyl)-2-(4-methoxy-2-propan-2-yloxyphenyl)-4,5-dihydroimidazole-1-carbonyl]piperazin-2-one; 2-Piperazinone, 4-(((4R,5S)-4,5-bis(4-chlorophenyl)-4,5-dihydro-2-(4-methoxy-2-(1-methylethoxy)phenyl)-1H-imidazol-1-yl)carbonyl)-; 4-((4R,5S)-4,5-Bis(4-chlorophenyl)-2-(2-isopropoxy-4-methoxyphenyl)-4,5-dihydro-1H-imidazole-1-carbonyl)piperazin-2-one; 4-[(4R,5S)-4,5-Bis(4-chlorophenyl)-2-(2-isopropoxy-4-methoxyphenyl)-4,5-dihydro-1H-imidazole-1-carbonyl]piperazin-2-one; 4-[[(4R,5S)-4,5-bis(4-chlorophenyl)-4,5-dihydro-2-[4-methoxy-2-(1-methylethoxy)phenyl]-1H-imidazol-1-yl]carbonyl]-2-piperazinone; cis-4-{[4,5-bis(4-chlorophenyl)-2-(2-isopropoxy-4-methoxyphenyl)-4,5-dihydroimidazol-1-yl]carbonyl}piperazin-2-one. Grades: >98%. CAS No. 675576-97-3. Molecular formula: C30H30Cl2N4O4. Mole weight: 581.49.
MDM2 Antagonist IV, Nutlin-3a ((-)-4-(4,5-bis-(4-Chlorophenyl)-2-(2-isopropoxy-4-methoxyphenyl)-4,5-dihydroimidazole-1-carbonyl)piperazine-2-one)
A cell-permeable and highly potent active enantiomer of Nutlin-3 that binds to the p53-binding pocket and blocks the interaction of p53 and MDM2 (IC50=90nM). Exhibits over 150-fold greater affinity for MDM2 than its less active enantiomer, Nutlin-3b. Induces p53 mediated apoptosis by both transcription-dependent and independent mechanisms. Shown to greatly potentiate the cytotoxic effects of chemotherapeutic agents and reduce tumor burden in vivo. Also shown to overcome ATM-mediated resistance to fludarabine in chronic lymphocyte leukemia. Cells treated with Nutlin-3a permanently lose their ability to proliferate and enter into a pattern of permanent senescence. Mouse embryonic fibroblasts with p53+/+ MEFs show significantly reduced reprogramming capabilities following Nutlin-3a treatment. Group: Biochemicals. Grades: Highly Purified. CAS No. 675576-98-4. Pack Sizes: 5mg. Molecular Formula: C??H??Cl?N?O?. US Biological Life Sciences.
Worldwide
CAY10682
The MDM2 protein is a negative regulator of p53. After binding to p53, it inhibits its transcriptional activity, favours its nuclear export and stimulates its degradation. The MDM2-TP53 pathway is a tumor-suppressor pathway that is often disrupted in cancer. CAY10682 is a pyrrolo[3,4c]pyrazole derivative that inhibits the p53-Mdm2 interaction as potently as (±)-nutlin-3 with Ki of 83 nM. It also blocks the growth of cancer cells with IC50 of 2-6 μM in vitro and inhibits the growth of A549 cell xenografts in mice. Synonyms: CAY 10682; CAY-10682. Grades: ≥98%. CAS No. 1542066-74-9. Molecular formula: C30H25BrFN5O. Mole weight: 570.5.
Caylin-2
Caylin-2, a Nutlin-3 analog, is a MDM2 inhibitor. Caylin-2 can bind to Bcl-X L [1]. Uses: Scientific research. Group: Signaling pathways. CAS No. 1392830-09-9. Pack Sizes: 1 mg. Product ID: HY-117585.
A cell-permeable tetrahydro-b-carbolinylbarbiturate compound that selectively inhibits the E3 ligase activity of Mdm2-MdmX hetero-complex over that of Mdm2-Mdm2 homo-complex (70.6% vs. 17.6% inhibition, respectively, at 100uM), without affecting Mdm2-MdmX complex formation or the activity of two other UbcH5C-utilizing ligase complexes Roc1-Cul1 and BRCA1-BARD1. Effectively inhibits ubiquitination and proteasomal degradation of cellular Mdm2 and p53 (effective conc.=14uM in U2OS, RKO, and HCT116 cultures) and induce RKO and MEF cell death in a p53- and Mdm2-dependent manner. Unlike Nutlin-3, MEL23 does not interfere with Mdm2-p53 interaction. Group: Biochemicals. Grades: Highly Purified. Pack Sizes: 10mg. US Biological Life Sciences.
Worldwide
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