WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 555855
CAS#: 1245792-51-1
Description: BCI is an allosteric inhibitor of dual specificity phosphatase (DUSP). BCI specifically inhibits DUSP6 and DUSP1 with EC50s of 13.3 and 8.0 μM in cells, respectively.
MedKoo Cat#: 555855
Name: BCI inhibitor
CAS#: 1245792-51-1
Chemical Formula: C22H23NO
Exact Mass: 317.178
Molecular Weight: 317.432
Elemental Analysis: C, 83.24; H, 7.30; N, 4.41; O, 5.04
Synonym: BCI; (E)-BCI, BCI inhibitor;
IUPAC/Chemical Name: (E)-2-benzylidene-3-(cyclohexylamino)-2,3-dihydro-1H-inden-1-one
InChi Key: XJDKPLZUXCIMIS-HMMYKYKNSA-N
InChi Code: InChI=1S/C22H23NO/c24-22-19-14-8-7-13-18(19)21(23-17-11-5-2-6-12-17)20(22)15-16-9-3-1-4-10-16/h1,3-4,7-10,13-15,17,21,23H,2,5-6,11-12H2/b20-15+
SMILES Code: O=C1/C(C(C2=C1C=CC=C2)NC3CCCCC3)=C/C4=CC=CC=C4
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO
Shelf Life: >3 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
| Biological target: | BCI is an inhibitor of dual specificity phosphatase (DUSP) which inhibits DUSP6 and DUSP1 with EC50s of 13.3 and 8.0 μM, respectively. |
| In vitro activity: | BCI hydrochloride (BCI), a DUSP6 small molecule inhibitor, increased the activity of ERK but interestingly decreased the expression of ERK response genes in BGC823, SGC7901 and CDDP-resistant SGC7901/DDP cells. BCI also caused cell death through the DNA damage response (DDR) pathway. Moreover, BCI inhibited cell proliferation, migration and invasion in a receptor-independent manner and enhanced CDDP cytotoxicity at pharmacological concentrations in the gastric cancer (GC) cells. Reference: Cancer Lett. 2018 Jan 1;412:243-255. https://www.sciencedirect.com/science/article/pii/S0304383517306316?via%3Dihub |
| In vivo activity: | In vivo experiments showed that BCI enhances the antitumor effects of CDDP (cisplatin) in cell-based xenografts and PDX models. Reference: Cancer Lett. 2018 Jan 1;412:243-255. https://www.sciencedirect.com/science/article/pii/S0304383517306316?via%3Dihub |
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 125.0 | 393.79 |
The following data is based on the product molecular weight 317.432 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
| Formulation protocol: | 1. Wu QN, Liao YF, Lu YX, Wang Y, Lu JH, Zeng ZL, Huang QT, Sheng H, Yun JP, Xie D, Ju HQ, Xu RH. Pharmacological inhibition of DUSP6 suppresses gastric cancer growth and metastasis and overcomes cisplatin resistance. Cancer Lett. 2018 Jan 1;412:243-255. doi: 10.1016/j.canlet.2017.10.007. Epub 2017 Oct 16. PMID: 29050982. 2. Zhang F, Tang B, Zhang Z, Xu D, Ma G. DUSP6 Inhibitor (E/Z)-BCI Hydrochloride Attenuates Lipopolysaccharide-Induced Inflammatory Responses in Murine Macrophage Cells via Activating the Nrf2 Signaling Axis and Inhibiting the NF-κB Pathway. Inflammation. 2019 Apr;42(2):672-681. doi: 10.1007/s10753-018-0924-2. PMID: 30506106. |
| In vitro protocol: | 1. Wu QN, Liao YF, Lu YX, Wang Y, Lu JH, Zeng ZL, Huang QT, Sheng H, Yun JP, Xie D, Ju HQ, Xu RH. Pharmacological inhibition of DUSP6 suppresses gastric cancer growth and metastasis and overcomes cisplatin resistance. Cancer Lett. 2018 Jan 1;412:243-255. doi: 10.1016/j.canlet.2017.10.007. Epub 2017 Oct 16. PMID: 29050982. 2. Zhang F, Tang B, Zhang Z, Xu D, Ma G. DUSP6 Inhibitor (E/Z)-BCI Hydrochloride Attenuates Lipopolysaccharide-Induced Inflammatory Responses in Murine Macrophage Cells via Activating the Nrf2 Signaling Axis and Inhibiting the NF-κB Pathway. Inflammation. 2019 Apr;42(2):672-681. doi: 10.1007/s10753-018-0924-2. PMID: 30506106. |
| In vivo protocol: | 1. Wu QN, Liao YF, Lu YX, Wang Y, Lu JH, Zeng ZL, Huang QT, Sheng H, Yun JP, Xie D, Ju HQ, Xu RH. Pharmacological inhibition of DUSP6 suppresses gastric cancer growth and metastasis and overcomes cisplatin resistance. Cancer Lett. 2018 Jan 1;412:243-255. doi: 10.1016/j.canlet.2017.10.007. Epub 2017 Oct 16. PMID: 29050982. |
[1]. Korotchenko VN, et al. In vivo structure-activity relationship studies support allosteric targeting of a dual specificity phosphatase. Chembiochem. 2014 Jul 7;15(10):1436-45.
Dual specificity phosphatase 6 (DUSP6) functions as a feedback attenuator of fibroblast growth factor signaling during development.
