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BCI hydrochloride Sale

(Synonyms: (E)-BCI hydrochloride) 目录号 : GC65025

An inhibitor of DUSP6 and DUSP1

BCI hydrochloride Chemical Structure

Cas No.:95130-23-7

规格 价格 库存 购买数量
10mM (in 1mL DMSO)
¥878.00
现货
1mg
¥450.00
现货
5mg
¥1,350.00
现货
10mg
¥1,980.00
现货

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Sample solution is provided at 25 µL, 10mM.

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产品描述

BCI is an inhibitor of dual specificity phosphatase 6 (DUSP6) and DUSP1.1,2 (E/Z)-BCI (0.5-2 ?M) inhibits LPS-induced expression of Dusp6 in a concentration-dependent manner and increases nuclear protein levels of Nrf2 in RAW 264.7 macrophages. It also inhibits LPS-induced increases in the production of IL-1β, IL-6, and reactive oxygen species (ROS) in RAW 264.7 and isolated mouse peritoneal macrophages in an ERK-independent manner. (E/Z)-BCI inhibits proliferation, migration, and invasion of gastric cancer cells in an ERK-dependent manner and induces cell death in part via the DNA damage response pathway.2 It reduces tumor growth in a gastric cancer patient-derived xenograft (PDX) mouse model when administered at a dose of 35 mg/kg every seven days and has an additive effect when used in combination with CDDP . The (E) isomer of BCI inhibits DUSP6 and DUSP1 in HeLa cells (IC50s = 12.3 and 11.5 ?M, respectively, for the human recombinant enzymes) and prevents pERK2 dephosphorylation induced by DUSP6 in vitro.3 It is selective for DUSP6 and DUSP1 over DUSP3/VHR, Cdc25B, and PTP1B, for which it has no activity. (E)-BCI induces expansion of the cardiac progenitor cell pool and increases heart size in zebrafish embryos. This product is a mixture of the (E) and (Z) isomers of BCI.2

1.Zhang, F., Tang, B., Zhang, Z., et al.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 pathwayInflammation42(2)672-681(2019) 2.Wu, Q.-N., Liao, Y.-F., Lu, Y.-X., et al.Pharmacological inhibition of DUSP6 suppresses gastric cancer growth and metastasis and overcomes cisplatin resistanceCancer Lett.412243-255(2018) 3.Molina, G., Vogt, A., Bakan, A., et al.Zebrafish chemical screening reveals an inhibitor of Dusp6 that expands cardiac cell lineagesNat. Chem. Biol.5(9)680-687(2009)

Chemical Properties

Cas No. 95130-23-7 SDF Download SDF
别名 (E)-BCI hydrochloride
分子式 C22H24ClNO 分子量 353.89
溶解度 DMSO : 15.62 mg/mL (44.14 mM; Need ultrasonic) 储存条件 -20°C, away from moisture
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储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。
Shipping Condition 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。

溶解性数据

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1 mg 5 mg 10 mg
1 mM 2.8257 mL 14.1287 mL 28.2574 mL
5 mM 0.5651 mL 2.8257 mL 5.6515 mL
10 mM 0.2826 mL 1.4129 mL 2.8257 mL
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Research Update

BCI Suppresses RANKL-Mediated Osteoclastogenesis and Alleviates Ovariectomy-Induced Bone Loss

Front Pharmacol 2021 Nov 1;12:772540.PMID:34803714DOI:10.3389/fphar.2021.772540.

Osteoporosis is a common aging-related metabolic disease that mainly occurs in older adults and postmenopausal women. Despite advances in anti-osteoporosis treatment, outcomes remain unsatisfactory due to detrimental side effects. BCI hydrochloride (BCI), a selective dual-specificity phosphatase 6 (DUSP6) inhibitor, is associated with multiple cellular functions, including inhibiting tumor growth and macrophage inflammation; however, its role in regulating osteoclast differentiation remains unknown. Here, we revealed that treatment with BCI attenuated RANKL-mediated osteoclast differentiation in vitro and alleviated ovariectomy-induced osteoporosis without obvious toxicity. Specifically, BCI disrupted F-actin ring formation and bone-resorption activity and decreased osteoclast-specific gene and protein levels in a dose-dependent manner. KEGG pathway analysis, GSEA based on transcriptome sequencing, and western blot results suggested that BCI inhibited RANKL-induced osteoclastogenesis by restraining STAT3 and NF-κB signaling and attenuating NF-κB/p65 interaction with NFATc1. These results revealed that BCI treatment prevented postmenopausal osteoporosis and might represent an effective approach for treating osteoporosis.