SML4049
TT-012, MITF dimer disruptor
≥98% (HPLC)
别名:
(2E,2′E)-N,N′-(Pyridine-2,6-diyl)bis(3-(furan-2-yl)acrylamide), (2E,2′E)-N,N′-2,6-Pyridinediylbis[3-(2-furanyl)-2-propenamide], TT 012, TT012
InChI
1S/C19H15N3O4/c23-18(10-8-14-4-2-12-25-14)21-16-6-1-7-17(20-16)22-19(24)11-9-15-5-3-13-26-15/h1-13H,(H2,20,21,22,23,24)/b10-8+,11-9+
InChI key
YUFJMFXVUUMVCA-GFULKKFKSA-N
SMILES string
O=C(NC1=CC=CC(NC(/C=C/C2=CC=CO2)=O)=N1)/C=C/C3=CC=CO3
assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 2 mg/mL, clear
storage temp.
2-8°C
Quality Level
Biochem/physiol Actions
Potent and selective MITF dimerization disruptor with significant efficacy against melanoma both in vitro and in vivo.
TT-012 is a highly effective microphthalmia-associated transcription factor (MITF) dimerization inhibitor (Kd = 15.5 nM for the bHLH-LZ domain) that specifically targets melanoma by disrupting MITF′s DNA-binding activity. TT012 exhibits notable potency in inhibiting MITF dimer formation (IC50 = 13.1 nM) and reducing the growth of B16F10 melanoma cells (IC50 = 499 nM), while also lowering mRNA levels of MITF target genes in these cells (IC50 < 3.12 µM). TT 012 is particularly effective against melanoma cells with elevated MITF expression and markedly diminishes tumor growth and pulmonary metastasis in mice, achieving reductions of 79.7% and 93.9% at dosages of 2 mg/kg and 5 mg/kg, respectively, compared to controls.
TT-012 is a highly effective microphthalmia-associated transcription factor (MITF) dimerization inhibitor (Kd = 15.5 nM for the bHLH-LZ domain) that specifically targets melanoma by disrupting MITF′s DNA-binding activity. TT012 exhibits notable potency in inhibiting MITF dimer formation (IC50 = 13.1 nM) and reducing the growth of B16F10 melanoma cells (IC50 = 499 nM), while also lowering mRNA levels of MITF target genes in these cells (IC50 < 3.12 µM). TT 012 is particularly effective against melanoma cells with elevated MITF expression and markedly diminishes tumor growth and pulmonary metastasis in mice, achieving reductions of 79.7% and 93.9% at dosages of 2 mg/kg and 5 mg/kg, respectively, compared to controls.
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
法规信息
新产品
此项目有
Zaizhou Liu et al.
Cell research, 33(1), 55-70 (2023-01-02)
Microphthalmia transcription factor (MITF) regulates melanocyte development and is the "lineage-specific survival" oncogene of melanoma. MITF is essential for melanoma initiation, progression, and relapse and has been considered an important therapeutic target; however, direct inhibition of MITF through small molecules
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