详情描述
BTYNB is an inhibitor of the oncofetal mRNA-binding protein IMP1 (IC50 = 5 μM for IMP1 binding to c-Myc mRNA). BTYNB downregulates β-TrCP1 mRNA and reduces activation of nuclear transcriptional factors-kappa B (NF-κB). BTYNB disrupts this enhancer function by impairing IGF2 mRNA-binding protein 1 (IGF2BP1)-RNA association.
Product information
CAS Number: 304456-62-0
Molecular Weight: 309.18
Formula: C12H9BrN2OS
Chemical Name: 2-[(E)-[(5-bromothiophen-2-yl)methylidene]amino]benzamide
Smiles: NC(=O)C1=CC=CC=C1/N=C/C1=CC=C(Br)S1
InChiKey: OZEADOPONHLEDS-VIZOYTHASA-N
InChi: InChI=1S/C12H9BrN2OS/c13-11-6-5-8(17-11)7-15-10-4-2-1-3-9(10)12(14)16/h1-7H,(H2,14,16)/b15-7+
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: Solubility (25°C) DMSO: 62 mg/mL(200.53 mM). Water: Insoluble.
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥360 days if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
In cells, BTYNB downregulates several mRNA transcripts regulated by IMP1. BTYNB destabilizes c-Myc mRNA, resulting in downregulation of c-Myc mRNA and protein. BTYNB downregulates β-TrCP1 mRNA and reduces activation of nuclear transcriptional factors-kappa B (NF-κB). The oncogenic translation regulator, eEF2, emerges as a new IMP1 target mRNA, enabling BTYNB to inhibit tumor cell protein synthesis. BTYNB potently inhibits proliferation of IMP1-containing ovarian cancer and melanoma cells with no effect in IMP1-negative cells. Overexpression of IMP1 reverses BTYNB inhibition of cell proliferation. BTYNB completely blocks anchorage-independent growth of melanoma and ovarian cancer cells in colony formation assays.
References:
- Lily Mahapatra, et al. Transl Oncol. 2017 Oct;10(5):818-827.
Products are for research use only. Not for human use.