BCI (Synonyms: (E)-BCI) |
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Catalog No.GC38646
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BCI, as a selective dual-specificity phosphatase 6 (DUSP6) inhibitor, can inhibit tumor growth and macrophage inflammation.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1245792-51-1
Sample solution is provided at 25 µL, 10mM.
BCI, as a selective dual-specificity phosphatase 6 (DUSP6) inhibitor, can inhibit tumor growth and macrophage inflammation.[1].
In vitro, BCI (1-4μM; 24-72h) showed no cytotoxic effects on RAW264.7 cells and BMMs, respectively[1]. BCI (2-4μM; 72h) had no obvious effect on cell cycle progression or apoptosis in BMMs[1]. BCI (0-4μM; 6d) decreased the cell viability of Neuroblastoma (NB) cell lines SK-N-AS, KELLY, IMR-32 and LAN-1 in a dose-dependent manner[2]. BCI (4μM; 24h) significantly increased the proportion of cells expressing cleaved caspase-3, indicating the activation of apoptosis in KELLY cells[2]. BCI (5μM; 6h) markedly increased ERK1/2 phosphorylation and decreased total NCC and NCC surface expression in mDCT cells[4].
In vivo, BCI (10mg/kg/d; i.p.; 5d) suppressed AKT activation and prevents tumor formation in mouse prostate[3]. BCI (50, 100, and 200mg/kg/d; p.o.; 1 month) obviously increased the number of pNrf2-positive cells in periodontal tissue and mitigated the alveolar bone loss in rats with chronic periodontitis and diabetes mellitus (CPDM)[5].
References:
[1] Cai C, et al. BCI Suppresses RANKL-Mediated Osteoclastogenesis and Alleviates Ovariectomy-Induced Bone Loss. Front Pharmacol. 2021 Nov 1;12:772540.
[2] Thompson EM, et al. The cytotoxic action of BCI is not dependent on its stated DUSP1 or DUSP6 targets in neuroblastoma cells. FEBS Open Bio. 2022 Jul;12(7):1388-1405.
[3] Duan S, et al. Loss of FBXO31-mediated degradation of DUSP6 dysregulates ERK and PI3K-AKT signaling and promotes prostate tumorigenesis. Cell Rep. 2021 Oct 19;37(3):109870.
[4] Feng X, et al. Aldosterone modulates thiazide-sensitive sodium chloride cotransporter abundance via DUSP6-mediated ERK1/2 signaling pathway. Am J Physiol Renal Physiol. 2015 May 15;308(10):F1119-27.
[5] Zhu C, et al. The therapeutic role of baicalein in combating experimental periodontitis with diabetes via Nrf2 antioxidant signaling pathway. J Periodontal Res. 2020 Jun;55(3):381-391.
| Cell experiment [1]: | |
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Cell lines |
MPNST cells |
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Preparation Method |
MPNST cells were starved overnight, incubated with BCI (2μM) for 60mins then stimulated with DMEM and 10% FBS for 1hr. Immunoblot analysis of TP53, p-RB and p-ATM and PARP cleavage and CC3 in ST8814 and S462.TY MPNST cells 24h after treatment with BCI (2μM). |
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Reaction Conditions |
2μM; 60 mins |
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Applications |
After 1hr, p-ERK, p-JNK, p-c-jun and total c-jun were elevated in the BCI-treated MPNST cell lines ST8814 and S462.TY but did not change in iHSC-1λ. Within 24 hours, BCI decreased total PARP and increased cleaved PARP and CC3, indicative of apoptotic cell death in NF1 deficient ST8814 and S462.TY cells. |
| Animal experiment [2]: | |
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Animal models |
Female C57BL/6 mice (8-weeks old) |
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Dosage form |
15mg/kg or 30mg/kg; i.p.; 8 weeks |
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Preparation method |
Low- or high-concentration (15mg/kg or 30mg/kg) BCI was injected intraperitoneally for 8 weeks, and bone loss was evaluated by micro-CT. |
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Applications |
Bone loss was prevented in both the low- and high-concentration BCI groups. Moreover, quantitative results indicated obvious increases in bone volume/total tissue volume (BV/TV), trabecular number (Tb.N), bone mineral density (BMD), and bone surface density (BS/TV) in both BCI-treated groups relative to the OVX group. |
References: | |
| Cas No. | 1245792-51-1 | SDF | |
| Synonyms | (E)-BCI | ||
| Canonical SMILES | O=C1/C(C(NC2CCCCC2)C3=C1C=CC=C3)=C/C4=CC=CC=C4 | ||
| Formula | C22H23NO | M.Wt | 317.42 |
| Solubility | DMSO: 125 mg/mL (393.80 mM) | Storage | Store at -20°C |
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.1504 mL | 15.752 mL | 31.504 mL |
| 5 mM | 630.1 μL | 3.1504 mL | 6.3008 mL |
| 10 mM | 315 μL | 1.5752 mL | 3.1504 mL |
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- Purity: >98.00% Appearance: A solid
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Average Rating: 5 (Based on Reviews and 7 reference(s) in Google Scholar.)