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926259-99-6

N-(2-Aminophenyl)pyrazine-2-carboxamide, also known as BG45, is an HDAC class I inhibitor with selectivity for HDAC3. It is a small molecule compound that has the ability to inhibit the activity of histone deacetylases, which are enzymes that regulate gene expression by removing acetyl groups from an ε-N-acetyl lysine amino acid on a histone. BG45 has been shown to have potent inhibitory effects on HDAC3 with an IC50 of 289 nM, while it inhibits HDAC1, HDAC2, and HDAC6 with greatly reduced potency.
Used in Pharmaceutical Industry:
N-(2-Aminophenyl)pyrazine-2-carboxamide is used as an HDAC class I inhibitor for treating various cancers, including multiple myeloma cancer. It modulates the activity of histone deacetylases, leading to changes in gene expression that can inhibit tumor growth and progression. BG45 has been shown to dose-dependently inhibit tumor growth in a mouse model of multiple myeloma, either alone or in combination with bortezomib.
Additionally, N-(2-Aminophenyl)pyrazine-2-carboxamide may have potential applications in other therapeutic areas, such as neurodegenerative diseases and inflammatory disorders, due to the role of HDACs in regulating gene expression and cellular processes. However, further research is needed to fully understand its potential applications and mechanisms of action in these areas.

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  • 926259-99-6 Structure

  • Basic information

    1. Product Name: N-(2-Aminophenyl)pyrazine-2-carboxamide
    2. Synonyms: BG45;N-(2-Aminophenyl)pyrazine-2-carboxamide;BG45, 98%, a HDAC class I inhibitor with selectivity for HDAC3;BG45, HDAC3 Inhibitor
    3. CAS NO:926259-99-6
    4. Molecular Formula: C11H10N4O
    5. Molecular Weight: 214.2233
    6. EINECS: N/A
    7. Product Categories: Inhibitors
    8. Mol File: 926259-99-6.mol

  • Chemical Properties

    1. Melting Point: N/A
    2. Boiling Point: N/A
    3. Flash Point: N/A
    4. Appearance: white to beige/
    5. Density: N/A
    6. Refractive Index: N/A
    7. Storage Temp.: 2-8°C
    8. Solubility: DMSO: soluble20mg/mL, clear
    9. CAS DataBase Reference: N-(2-Aminophenyl)pyrazine-2-carboxamide(CAS DataBase Reference)
    10. NIST Chemistry Reference: N-(2-Aminophenyl)pyrazine-2-carboxamide(926259-99-6)
    11. EPA Substance Registry System: N-(2-Aminophenyl)pyrazine-2-carboxamide(926259-99-6)

  • Safety Data

    1. Hazard Codes: Xi
    2. Statements: 36/37/38
    3. Safety Statements: 36/37/39
    4. WGK Germany: 3
    5. RTECS:
    6. HazardClass: N/A
    7. PackingGroup: N/A
    8. Hazardous Substances Data: 926259-99-6(Hazardous Substances Data)

926259-99-6 Usage

in vitro

bg45 is reported as an hdac class i inhibitor with selectivity for hdac3 over hdac1, 2. consistent with hdac3 knockdown data, bg45 significantly inhibited mm cell growth dose-dependently. importantly, bg45 also triggered a potent growth inhibitory effect against patient-derived mm cells, without affecting normal donor pbmcs [1].

in vivo

bg45 significantly inhibited mm tumor growth in a dose-dependent fashion. for example, significant differences were observed in control versus bg45 15 mg/kg, control versus bg45 50 mg/kg, and bg45 15 mg/kg versus bg45 50 mg/kg at day 22. moreover, bg45 50 mg/kg in combination with bortezomib enhanced either single agent activity further. these results confirmed that bg45 triggers in vivo anti-mm activities [1].

IC 50

289 nm

references

[1] minami j, suzuki r, mazitschek r, gorgun g, ghosh b, cirstea d, hu y, mimura n, ohguchi h, cottini f, jakubikova j, munshi nc, haggarty sj, richardson pg, hideshima t, anderson kc. histone deacetylase 3 as a novel therapeutic target in multiple myeloma. leukemia. 2014 mar;28(3):680-9.

Check Digit Verification of cas no

The CAS Registry Mumber 926259-99-6 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 9,2,6,2,5 and 9 respectively; the second part has 2 digits, 9 and 9 respectively.
Calculate Digit Verification of CAS Registry Number 926259-99:
(8*9)+(7*2)+(6*6)+(5*2)+(4*5)+(3*9)+(2*9)+(1*9)=206
206 % 10 = 6
So 926259-99-6 is a valid CAS Registry Number.

926259-99-6 Well-known Company Product Price

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  • Sigma

  • (SML0867)  BG45  ≥98% (HPLC)

  • 926259-99-6

  • SML0867-5MG

  • 983.97CNY

  • Detail

  • Sigma

  • (SML0867)  BG45  ≥98% (HPLC)

  • 926259-99-6

  • SML0867-25MG

  • 3,970.98CNY

  • Detail

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