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Chemical Structure| 1245792-51-1 Chemical Structure| 1245792-51-1

Structure of BCI
CAS No.: 1245792-51-1

Chemical Structure| 1245792-51-1

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(E)-BCI is an allosteric inhibitor of dual specificity phosphatase (DUSP). (E)-BCI specifically inhibits DUSP6 and DUSP1 with EC50s of 13.3 and 8.0 μM in cells, respectively, but does not inhibit DUSP5.

Synonyms: (E)-BCI

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Product Details of BCI

CAS No. :1245792-51-1
Formula : C22H23NO
M.W : 317.42
SMILES Code : O=C1/C(C(NC2CCCCC2)C3=C1C=CC=C3)=C/C4=CC=CC=C4
Synonyms :
(E)-BCI
MDL No. :MFCD20232928
InChI Key :XJDKPLZUXCIMIS-HMMYKYKNSA-N
Pubchem ID :6419844

Safety of BCI

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P264-P270-P271-P280-P301+P312-P302+P352-P304+P340-P305+P351+P338-P330-P332+P313-P337+P313-P362-P403+P233-P405-P501

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
STS26T MPNST cells 2-4 μM 72 h Evaluate the effect of BCI on MPNST cell growth, results showed cells were less sensitive to BCI Clin Cancer Res. 2019 Jul 1;25(13):4117-4127.
iHSC-1λ Schwann cells 2-4 μM 72 h Evaluate the effect of BCI on Schwann cell growth, results showed cells were less sensitive to BCI Clin Cancer Res. 2019 Jul 1;25(13):4117-4127.
S462.TY MPNST cells 2-4 μM 72 h Evaluate the effect of BCI on MPNST cell growth, results showed BCI significantly inhibited cell growth Clin Cancer Res. 2019 Jul 1;25(13):4117-4127.
ST8814 MPNST cells 2-4 μM 72 h Evaluate the effect of BCI on MPNST cell growth, results showed BCI significantly inhibited cell growth Clin Cancer Res. 2019 Jul 1;25(13):4117-4127.
HeLa cells 10 μM 15 min BCI treatment restored p-ERK levels in Dusp6-Myc transfected cells, indicating that BCI directly inhibited Dusp6-Myc function Nat Chem Biol. 2009 Sep;5(9):680-7.
Mouse bone marrow-derived macrophages (BMMs) 1 μM 6 days To investigate the effect of (E/Z)-BCI on osteoclast differentiation, results showed that (E/Z)-BCI significantly accelerated osteoclastogenesis. Cell Death Dis. 2021 Sep 2;12(9):825.
BaF3 cells 400 nM 1 week To evaluate the effect of BCI on CSF3R mutant-induced CFU formation, results showed that BCI alone or in combination with ruxolitinib significantly suppressed CSF3R mutant-induced CFU formation. Blood Adv. 2024 Jun 11;8(11):2765-2776.
SH-SY5Y neuroblastoma cells 5 μM 24 h BCI enhances P2X7 receptor expression Front Cell Dev Biol. 2022 Dec 15;10:1049566.
N2a neuroblastoma cells 5 μM 24 h BCI enhances P2X7 receptor expression Front Cell Dev Biol. 2022 Dec 15;10:1049566.

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mice Jak2V617F-induced MPN model Oral 100 mg/kg Daily, for 40 weeks Evaluate the selective eradication effect of BCI on Jak2V617F clones Leukemia. 2023 Aug;37(8):1686-1697.
Zebrafish Ventricular resection model Intraperitoneal injection 10 µM Once daily until hearts were collected BCI promotes heart regeneration by inhibiting Dusp6 Cell Res. 2014 Sep;24(9):1091-107
Nude mice S462.TY cell line xenograft model Intraperitoneal injection 10 mg/kg Once daily, 5x/wk for 27 days Evaluate the effect of BCI on MPNST xenograft model, results showed no significant difference in tumor volume but tumor tissue exhibited necrosis Clin Cancer Res. 2019 Jul 1;25(13):4117-4127.
Zebrafish Transgenic zebrafish embryos Immersion 5 μM From the 1000-cell stage BCI treatment enhanced FGF signaling, leading to increased transcription of several FGF target genes Nat Chem Biol. 2009 Sep;5(9):680-7.
C57BL/6J mice Ovariectomy-induced osteoporosis model Intraperitoneal injection 30 mg/kg Twice a week for 6 weeks To investigate the effect of (E/Z)-BCI on osteoporosis in vivo, results showed that (E/Z)-BCI significantly accelerated the bone loss process. Cell Death Dis. 2021 Sep 2;12(9):825.
NSG mice Orthotopic model of prostate cancer Intraperitoneal injection 10 mg/kg Five consecutive days per week, until experimental endpoint BCI inhibits DUSP6 activity and prevents tumor formation induced by FBXO31 knockout Cell Rep. 2021 Oct 19;37(3):109870
Mice Conventionally-raised wild-type mice and Dusp6-deficient mice Intraperitoneal injection 5 μg/g Once a day during CR period Investigate the role of DUSP6 inhibitor BCI in maintaining cold-adapted microbiota and promoting white adipose tissue browning after cold exposure NPJ Biofilms Microbiomes. 2024 Mar 13;10(1):22
Mice CSF3R-induced leukemia model Intraperitoneal injection 10 mg/kg Twice daily for 8 weeks To evaluate the therapeutic effect of BCI alone or in combination with trametinib on CSF3R-induced leukemia, results showed that the combination of BCI and trametinib successfully cured the leukemia in mice. Blood Adv. 2024 Jun 11;8(11):2765-2776.

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.15mL

0.63mL

0.32mL

15.75mL

3.15mL

1.58mL

31.50mL

6.30mL

3.15mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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