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Chemical Structure| 926259-99-6 Chemical Structure| 926259-99-6

Structure of BG45
CAS No.: 926259-99-6

Chemical Structure| 926259-99-6

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BG45 is a selective inhibitor for HDAC3 with IC50 of 289 nM.

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Product Details of BG45

CAS No. :926259-99-6
Formula : C11H10N4O
M.W : 214.22
SMILES Code : O=C(C1=NC=CN=C1)NC2=CC=CC=C2N
MDL No. :MFCD09046162
InChI Key :LMWPVSNHKACEKW-UHFFFAOYSA-N
Pubchem ID :16773791

Safety of BG45

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Related Pathways of BG45

epigenetics

Isoform Comparison

Biological Activity

Target
  • HDAC3

    HDAC3, IC50:289 nM

  • HDAC2

    HDAC2, IC50:2.2 μM

  • HDAC1

    HDAC1, IC50:2 μM

In Vitro:

Cell Line
Concentration Treated Time Description References
MM.1S cells 20 μM 24 h BG45 treatment downregulated DNMT1 protein levels. Leukemia. 2017 Dec;31(12):2670-2677.
NCI-H929 cells 20 μM 24 h BG45 treatment downregulated DNMT1 protein levels. Leukemia. 2017 Dec;31(12):2670-2677.
RPMI 8226 cells 20 μM 24 h BG45 treatment downregulated DNMT1 protein levels. Leukemia. 2017 Dec;31(12):2670-2677.
NCI-H929 cells 20 μM 10 h BG45 treatment downregulated c-Myc protein levels without altering mRNA levels. Leukemia. 2017 Dec;31(12):2670-2677.
RPMI 8226 cells 20 μM 10 h BG45 treatment downregulated c-Myc protein levels without altering mRNA levels. Leukemia. 2017 Dec;31(12):2670-2677.
MM.1S cells 20 μM 10 h BG45 treatment downregulated c-Myc protein levels without altering mRNA levels. Leukemia. 2017 Dec;31(12):2670-2677.
MM.1S 15 µM To evaluate the effect of BG45 on apoptosis in MM.1S cells, results showed that BG45 induced cleavage of caspase-3 and PARP. Leukemia. 2014 Mar;28(3):680-9.
RPMI8226 1.875 – 30 µM 48 h and 72 h To evaluate the inhibitory effect of BG45 on MM cell growth, results showed that BG45 significantly inhibited MM cell growth. Leukemia. 2014 Mar;28(3):680-9.
SH-SY5Y cells 15 μM 36 h BG45 increased cell viability, increased the expression of PSD-95 and spinophilin, and improved the cytoskeleton Front Aging Neurosci. 2021 Jan 19;12:619866.
SH-SY5Y cells 15 μM 36 h BG45 significantly increased the viability of APPsw-positive cells and decreased the expression of HDAC1, HDAC2, and HDAC3 Molecules. 2022 Jun 29;27(13):4160.
primary cortical neurons 10 μM 48 h BG45 can upregulate the expression levels of synaptotagmin-1 (SYT-1) and neurofilament light chain (NF-L) in primary neurons Pharmaceuticals (Basel). 2022 Nov 28;15(12):1481.

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mice Murine xenograft model of human MM 20 mg/kg 5 days/week, 3 weeks Combination of BG45 and AZA significantly inhibited tumor growth and prolonged survival. Leukemia. 2017 Dec;31(12):2670-2677.
CB17 SCID mice Human MM.1S xenograft model Intraperitoneal injection 15 mg/kg and 50 mg/kg 5 days a week for 3 weeks To evaluate the inhibitory effect of BG45 alone or in combination with bortezomib on tumor growth, results showed that BG45 significantly inhibited tumor growth, and the combination with bortezomib was more effective. Leukemia. 2014 Mar;28(3):680-9.
Kunming mice Alzheimer's disease-related model Intraperitoneal injection 30 mg/kg 9 consecutive days BG45 decreased the expression of HDAC1 and 2, increased the expression of PSD-95, spinophilin, and synaptophysin (SYP) Front Aging Neurosci. 2021 Jan 19;12:619866.
APP/PS1 transgenic mice Alzheimer's disease model Intraperitoneal injection 30 mg/kg Once daily for 12 days BG45 alleviates inflammation and improves synaptic protein expression by regulating the CREB/BDNF/NF-kB pathway, with more significant effects observed with early and repeated administration. Int J Mol Sci. 2023 Mar 2;24(5):4805
APP/PS1 transgenic mice APP/PS1 transgenic mice Intraperitoneal injection 30 mg/kg 12 consecutive days BG45 alleviated the apoptosis-mediated loss of hippocampal neurons, upregulated synapse-related proteins, reduced Aβ deposition and phosphorylation of tau, and increased the levels of the synapse-related genes GRIK2, SCN3B, SYP, Grm2, and Grid2IP Molecules. 2022 Jun 29;27(13):4160.
APPswe/PS1dE9 transgenic mice Alzheimer's disease model Intraperitoneal injection 30 mg/kg Once daily for 12 days BG45 can alleviate damage to dendritic spines, reduce Aβ deposition, and improve learning and memory function Pharmaceuticals (Basel). 2022 Nov 28;15(12):1481.

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

4.67mL

0.93mL

0.47mL

23.34mL

4.67mL

2.33mL

46.68mL

9.34mL

4.67mL

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