NCGC00244536

SKU: orb1296243

Description

NCGC00244536

Research Area

Epigenetics & Chromatin

Key Properties

• CAS Number: 2003260-55-5
• MW: 382.45
• Purity: 99.72%
• Formula: C₂₅H₂₂N₂O₂
• SMILES: Oc1cc(cc2cccnc12)-c1cccc(c1)C(=O)NCCCc1ccccc1
• Target: Histone Demethylase
• Solubility: DMSO:100 mg/mL (261.47 mM)

Bioactivity

• Target IC50:
  KDM4B:10 nM
• In Vivo:
  Treatment with NCGC00244536 significantly inhibits tumor growth without causing major toxicity in animals, which appear normal. Tumors treated with NCGC00244536 show a substantial increase in cell apoptosis, necrosis, and fibrosis.
• In Vitro:
  NCGC00244536 significantly suppresses the growth of AR-positive cell lines such as LNCaP and VCaP, demonstrating inhibitory concentration values (IC50s) below one micromolar, while effectively eliminating androgen-induced LNCaP cell proliferation. It exhibits strong preference for rapidly proliferating AR-negative PC3 cells with a strikingly low IC50 of 40 nM, demonstrating greater than 100-fold selectivity compared to immortalized prostate epithelial cell lines PrEC1 and PrEC4. Additionally, NCGC00244536 effectively restricts the expansion of various other cancer cell lines, including breast cancer cell lines MDA-MB2 and MCF-7, showcasing its inhibitory potential across a broad spectrum of cancer types with IC50s in the micromolar range.
• Cell Research:
  LNCaP cells are treated with 0.1, 0.2, 1, 2.5, 5, 20 μM of NCGC00244536. Cell viability is measured using the MTT assay.
• Animal Research:
  For the xenograft animal model, PC3 cell suspension is injected into 4-6 weeks old severe combined immunodeficient (SCID) mice. When tumors become palpable, animals are randomly grouped for drug treatment. Alzet osmotic minipump containing NCGC00244536 (20 mg/kg)is subcutaneously inserted into each animal, which allowed continuous drug delivery to the tumor site for up to 5 days. Tumor volume is recorded every other days and calculated by using the ellipsoid formula.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Inhibitor, Histone Demethylase, HistoneDemethylase, KDM4B, KDM4B Inhibitor B3, inhibit, NCGC00244536, NCGC-00244536, NCGC 00244536

Compound Identifiers

PubChem CID

127030711