CLZ-8 - Moligand™, ≥98% , CAS No.678158-55-9

CAS: 678158-55-9 Cat. No.: C647817 Summenformel: C₂₂H₂₃N₃O₂S Molekulargewicht: 393.50 PubChem CID: 988971

GRADE & PURITY Moligand™, ≥98%

Storage

Store at -20°C

Shipped In

Ice chest + Ice pads

Übersicht

CLZ-8 (Compound 8) is an orally active Mcl-1-PUMA interface inhibitor, with a K i of 0.3 μM. CLZ-8 exhibits dual activity on reduce PUMA-dependent apoptosis while deactivating Mcl-1-mediated anti-apoptosis in cancer cells

In Vitro

CLZ-8 (Compound 8) (0-160 μM, 48 h) significantly inhibits PUMA-dependent apoptosis. CLZ-8 (0-1 μM, 2 h) significantly enhance the irradiated cell viability in a dose-dependent manner, provides significant protection for HUVECs, and inhibits overexpressed PUMA. CLZ-8 (0-1 μM, 24 h) attenuates the radiation-induced apoptosis. CLZ-8 (1 μM, 2 h) protects HUVECs from DNA breaks. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Apoptosis Analysis Cell Line: DLD-1 cells or HUVEC cells Concentration: 0-160 μM (DLD-1) or 0.01, 0.1 and 1 μM (HUVECs) Incubation Time: 48 h (DLD-1) or 24 h (HUVECs) Result: Significantly inhibited PUMA-dependent apoptosis with an IC 50 of 38.93 ± 0.91 μM. Attenuated the radiation-induced apoptosis. Western Blot AnalysisCell Line: HUVEC cells Concentration: 0.001, 0.01, 0.1 and 1 μM Incubation Time: 2 h Result: Suppressed induction of PUMA after radiation, significantly decreased the level of p53. Significantly decreased the level of MCL-1 and increased the level of Bcl-XL.

In Vivo

CLZ-8 (0-400 mg/kg; i.g.; once) shows powerful anti-radiation effects in mice. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: 6-8 week-old male BALB/c miceDosage: 100, 200 and 400 mg/kg Administration: Intragastric administration, once, 30 min prior to irradiation Result: Increased the survival rate of irradiated mice.

Form:Solid

IC50& Target:Mcl-1 0.3 μM (Ki) PUMA

Specifications

Spezifikationen & Reinheit

Moligand™, ≥98%

Biochemische und physiologische Mechanismen

CLZ-8 (Compound 8) is an active Mcl-1-PUMA interface inhibitor, with a K i of 0.3 μM. CLZ-8 exhibits dual activity on reduce PUMA-dependent apoptosis while deactivating Mcl-1-mediated anti-apoptosis in cancer cells.

Storage

Store at -20°C

Verschickt in

Ice chest + Ice pads

Dieses Produkt erfordert Kühlkettenversand. Grundversand und andere Economy-Optionen sind nicht verfügbar.

Note

Moligand™

Aktionsart

INHIBITOR

Reinheit

≥98%

Namen und Kennungen

• Kanonisches Lächeln: C1CN(CCN1CCO)C2=NC(=O)C(=CC3=CC=C(C=C3)C4=CC=CC=C4)S2
• IUPAC Name: (5Z)-2-[4-(2-hydroxyethyl)piperazin-1-yl]-5-[(4-phenylphenyl)methylidene]-1,3-thiazol-4-one
• InChIKey: IBEWMFVUBLAYJT-SILNSSARSA-N
• INCHI: 1S/C22H23N3O2S/c26-15-14-24-10-12-25(13-11-24)22-23-21(27)20(28-22)16-17-6-8-19(9-7-17)18-4-2-1-3-5-18/h1-9,16,26H,10-15H2/b20-16-
• Isomere SMILES: C1CN(CCN1CCO)C2=NC(=O)/C(=C/C3=CC=C(C=C3)C4=CC=CC=C4)/S2
• PubChem CID: 988971
• Molekulargewicht: 393.50

Taxonomic Classification

Taxonomy Tree

• Kingdom Organic compounds
  • Superclass Benzenoids
    • Klasse Benzene and substituted derivatives
      • Subclass Biphenyls and derivatives

• Kingdom: Organic compounds
• Superclass: Benzenoids
• Klasse: Benzene and substituted derivatives
• Subclass: Biphenyls and derivatives
• Intermediate Tree Nodes: Not available
• Direct Parent: Biphenyls and derivatives
• Alternative Parents: N-alkylpiperazines Thiazolines Trialkylamines N-acylimines Isothioureas Amino acids and derivatives 1,2-aminoalcohols Propargyl-type 1,3-dipolar organic compounds Carboximidamides Azacyclic compounds Primary alcohols Organopnictogen compounds Organic oxides Hydrocarbon derivatives Carbonyl compounds
• Molecular Framework: Aromatic heteromonocyclic compounds
• Substituents: Biphenyl - N-alkylpiperazine - 1,4-diazinane - Piperazine - Meta-thiazoline - 1,2-aminoalcohol - Amino acid or derivatives - Isothiourea - Tertiary amine - Tertiary aliphatic amine - N-acylimine - Alkanolamine - Carboxylic acid derivative - Azacycle - Organoheterocyclic compound - Organic 1,3-dipolar compound - Propargyl-type 1,3-dipolar organic compound - Carboximidamide - Organonitrogen compound - Hydrocarbon derivative - Organic oxide - Alcohol - Carbonyl group - Organooxygen compound - Organic nitrogen compound - Primary alcohol - Amine - Organic oxygen compound - Organopnictogen compound - Aromatic heteromonocyclic compound
• Beschreibung: This compound belongs to the class of organic compounds known as biphenyls and derivatives. These are organic compounds containing to benzene rings linked together by a C-C bond.
• External Descriptors: Not available

Data sources

1. Djoumbou Feunang Y, Eisner R, Knox C, Chepelev L, Hastings J, Owen G, Fahy E, Steinbeck C, Subramanian S, Bolton E, Greiner R, and Wishart DS. ClassyFire: Automated Chemical Classification With A Comprehensive, Computable Taxonomy. Journal of Cheminformatics, 2016, 8:61.

DOI: 10.1186/s13321-016-0174-y

Chemische und physikalische Eigenschaften

• Löslichkeit: DMSO : 50 mg/mL (127.06 mM; Need ultrasonic)
• Molekulargewicht: 393.500 g/mol
• XLogP3: 3.200
• Hydrogen Bond Donor Count: 1
• Hydrogen Bond Acceptor Count: 4
• Rotatable Bond Count: 5
• Exact Mass: 393.151 Da
• Monoisotopic Mass: 393.151 Da
• Topological Polar Surface Area: 81.400 Ų
• Heavy Atom Count: 28
• Formal Charge: 0
• Complexity: 599.000
• Isotope Atom Count: 0
• Defined Atom Stereocenter Count: 0
• Undefined Atom Stereocenter Count: 0
• Defined Bond Stereocenter Count: 1
• Undefined Bond Stereocenter Count: 0
• The total count of all stereochemical bonds: 1
• Covalently-Bonded Unit Count: 1

Häufig gestellte Fragen

How is this product shipped?

This product ships in an insulated container with ice pads. Unpack on arrival and transfer it to the storage condition stated above.