1415340-63-4 Usage
Uses
Used in Pharmaceutical Industry:
MI-192 is used as an HDAC inhibitor for its ability to modulate gene expression and alter cellular processes, particularly in the context of cancer treatment. By inhibiting HDAC 2 and 3, MI-192 can promote differentiation and apoptosis in acute myeloid leukemia cells, making it a promising candidate for targeted cancer therapies.
Additionally, due to its cytotoxic effects, MI-192 may be utilized in the development of novel drug delivery systems to enhance its efficacy and bioavailability in treating specific types of cancer. This could involve the use of various organic and metallic nanoparticles as carriers for MI-192, aiming to improve its delivery and therapeutic outcomes in cancer treatment.
Biological Activity
mi-192 is a histone deacetylases (hdacs) inhibitor that preferentially inhibits hdac2 and hdac3 with ic50 values of 30 nm and 16 nm, respectively [1].histone acetylation is the most commonly employed mechanism utilized by transcription factors to activate gene expression. conversely, histone deacetylation is the most common mechanism used to inactivate genes. histone deacetylase inhibitors (hdacis) are in advanced clinical development as cancer therapeutic agents [1].mi-192 is a novel benzamide-based compound that had marked selectivity for the class i enzymes, hdac2 and hdac3. in hela cell extracts, mi-192 inhibited hdac activity with ic50 value of 1.5 μm. mi-192 selectively inhibited recombinant hdac2 and hdac3 with ic50 values of 30 nm and 16 nm, respectively over hdac1, 4, 6, 7, and 8 (ic50s = 4.8, 5, >10, 4.1, and >10 μm, respectively). mi-192 showed the greatest growth inhibitory effect against the leukemic cell lines with an effective dose of 0.1-0.4 μm. mi-192 was cytotoxic and promoted apoptosis and differentiation in leukaemic cell lines [1]. in the human prostate cancer cell line pc3, mi-192 significantly increased tubulin acetylation and ablated the dynamic behaviour of microtubules in live cells [2].
Biochem/physiol Actions
MI192 is a potent and selective histone deacetylase 3 (HDAc 3) inhibitor that inhibits IL-6 production in peripheral blood mononuclear cells (PBMCs) from rheumatoid arthritis (RA) but not healthy PBMCs.
references
[1]. boissinot, m.,inman, m.,hempshall, a., et al. induction of differentiation and apoptosis in leukaemic cell lines by the novel benzamide family histone deacetylase 2 and 3 inhibitor mi-192. leukemia research 36, 1304-1310 (2012).[2]. bacon t, seiler c, wolny m, et al. histone deacetylase 3 indirectly modulates tubulin acetylation. biochem j. 2015 dec 15;472(3):367-77.
Check Digit Verification of cas no
The CAS Registry Mumber 1415340-63-4 includes 10 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 7 digits, 1,4,1,5,3,4 and 0 respectively; the second part has 2 digits, 6 and 3 respectively.
Calculate Digit Verification of CAS Registry Number 1415340-63:
(9*1)+(8*4)+(7*1)+(6*5)+(5*3)+(4*4)+(3*0)+(2*6)+(1*3)=124
124 % 10 = 4
So 1415340-63-4 is a valid CAS Registry Number.
1415340-63-4Relevant articles and documents
N- (2 -AMINOPHENYL) BENZAMIDE DERIVATIVES AS HISTONE DEACETYLASE INHIBITORS
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, (2014/05/20)
This invention relates to the discovery of novel compounds, or pharmaceutically acceptable salts thereof, which possess HDAC inhibitory activity. In particular, the compounds of the invention demonstrate selectivity towards Class I HDAC enzymes, and are a
1, 2, 4-Thiadiazol-5-Ylpiperazine derivatives useful in the treatment of neurodegenerative diseases
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, (2014/05/20)
The present invention relates to a compound of formula (IA) The present invention also relates to the use of the compound of formula IA for treating certain neurodegenerative disorders characterized by cytotoxic TAU misfolding and/or aggregation.
N- (2 -AMINOPHENYL) BENZAMIDE DERIVATIVES AS HISTONE DEACETYLASE INHIBITORS
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, (2013/03/26)
This invention relates to the discovery of novel compounds, or pharmaceutically acceptable salts thereof, which possess HDAC inhibitory activity. In particular, the compounds of the invention demonstrate selectivity towards Class I HDAC enzymes, and are a
1, 2, 4 -THIADIAZOL- 5 -YLPIPERAZINE DERIVATIVES USEFUL IN THE TREATMENT NEURODEGENERATIVE DISEASES
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, (2013/03/26)
The present invention relates to a compound of formula (IA) The present invention also relates to the use of the compound of formula IA for treating certain neurodegenerative disorders characterized by cytotoxic TAU misfolding and/or aggregation.
