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Chemical Structure| 432529-82-3 Chemical Structure| 432529-82-3

Structure of BCI-121
CAS No.: 432529-82-3

Chemical Structure| 432529-82-3

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BCI-121 (BCI121) is a substrate-competitive inhibitor of SMYD3 that inhibits SMYD3-substrate interaction and chromatin recruitment It can significantly reduce the proliferation of various cancer cells.

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Product Details of BCI-121

CAS No. :432529-82-3
Formula : C14H18BrN3O2
M.W : 340.22
SMILES Code : O=C(C1CCN(CC(NC2=CC=C(Br)C=C2)=O)CC1)N
MDL No. :MFCD02149239
InChI Key :KSUYPIXCRPCPGF-UHFFFAOYSA-N
Pubchem ID :795875

Safety of BCI-121

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

Related Pathways of BCI-121

epigenetics

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
A2780 cells 100 µM or 120 µM 48 hours Inhibited A2780 cell proliferation J Cancer. 2019 Jul 8;10(17):4072-4084.
UM-SCC-1 350 µM Inhibited tumorsphere formation and cell proliferation Clin Epigenetics. 2023 May 26;15(1):92.
CAL-27 200 µM Inhibited tumorsphere formation and cell proliferation Clin Epigenetics. 2023 May 26;15(1):92.
MB002 80 µM 24 hours Evaluate the inhibitory effect of BCI-121 on SMYD3 and its impact on cell proliferation Cancers (Basel). 2022 Mar 25;14(7):1673.
D458 80 µM 24 hours Evaluate the inhibitory effect of BCI-121 on SMYD3 and its impact on cell proliferation Cancers (Basel). 2022 Mar 25;14(7):1673.
D425 80 µM 24 hours Evaluate the inhibitory effect of BCI-121 on SMYD3 and its impact on cell proliferation Cancers (Basel). 2022 Mar 25;14(7):1673.
D283 80 µM 24 hours Evaluate the inhibitory effect of BCI-121 on SMYD3 and its impact on cell proliferation Cancers (Basel). 2022 Mar 25;14(7):1673.
SKOV-3 100 µM 48 hours BCI-121 significantly inhibited the proliferation of SKOV-3 cells and reduced the expression levels of SMYD3 target genes. J Cell Physiol. 2015 Oct;230(10):2447-2460.
OVCAR-3 100 µM 48 hours BCI-121 significantly inhibited the proliferation of OVCAR-3 cells and reduced the expression levels of SMYD3 target genes. J Cell Physiol. 2015 Oct;230(10):2447-2460.
HCT116 100 µM 48 hours BCI-121 significantly inhibited the proliferation of HCT116 cells and reduced the expression levels of SMYD3 target genes. J Cell Physiol. 2015 Oct;230(10):2447-2460.
HT29 100 µM 48 hours BCI-121 significantly inhibited the proliferation of HT29 cells and reduced the expression levels of SMYD3 target genes. J Cell Physiol. 2015 Oct;230(10):2447-2460.
SGC-7901 cells 100 µM BCI-121 significantly inhibited the proliferation of SGC-7901 cells Cell Death Dis. 2023 Jun 29;14(6):386.
HGC-27 cells 100 µM BCI-121 significantly inhibited the proliferation of HGC-27 cells Cell Death Dis. 2023 Jun 29;14(6):386.

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mice P301S Tau transgenic mice Intraperitoneal injection 1 mg/kg Once daily for 3 days BCI-121 treatment significantly reduced H3K4me3 levels in the prefrontal cortex of Tau mice and improved cognitive behavioral deficits, restoring synaptic NMDAR function and expression Nat Commun. 2023 Jan 6;14(1):91
Balb/c nude mice Subcutaneous injection of SGC-7901 cells model Intratumoral injection 100 μM Twice a week for 1 week BCI-121 significantly inhibited the growth of SGC-7901 cells in vivo Cell Death Dis. 2023 Jun 29;14(6):386.
BALB/c nude mice Subcutaneous tumor model Intratumoral injection 50 µl (1000 µM) Three times a week for 25 days Suppressed tumor growth and proliferation Clin Epigenetics. 2023 May 26;15(1):92.
Nude mice Endometrial cancer xenograft model Intratumoral injection 50μM Twice a week for 4 weeks Evaluate the inhibitory effect of BCI-121 on tumor growth in endometrial cancer xenograft model Oncogenesis. 2024 Jan 8;13(1):3

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.94mL

0.59mL

0.29mL

14.70mL

2.94mL

1.47mL

29.39mL

5.88mL

2.94mL

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