| 包装 | 价格(元) |
| 10mM (in 1mL DMSO) | 电议 |
| 1mg | 电议 |
| 5mg | 电议 |
| 10mg | 电议 |
| 25mg | 电议 |
Cell lines | MCF10DCIS cells |
Preparation Method | MCF10DCIS cells were grown in soft agar at different concentrations of BB-CL-AMIDINE (0 μM (DMSO), or 1 μM BB-CL-AMIDINE). After 2.5 weeks, individual colonies larger than 70 μm were counted. |
Reaction Conditions | 0 μM or 1 μM; 2.5 weeks |
Applications | There was an average of 3,536 colonies in the DMSO control whereas only 1,967 colonies were seen in the BB-CL-AMIDINE treated group after 2.5 weeks of soft agar culture. This represents a 44% decrease in the average colony formation in the presence of 1 μM BB-CL-AMIDINE, indicating a significant tumorigenic inhibition of breast cancer cells (MCF10DCIS cells) by the PADI inhibitor. |
Animal models | Eight-week-old female NOD mice |
Dosage form | 1 μg/g; s.c. |
Preparation method | Eight-week-old female NOD mice were used. Treatments involved subcutaneous injections with BB-Cl-amidine (1 μg/g body weight) or vehicle (25% DMSO in PBS) six times per week until 25 weeks of age for diabetes incidence or until 13 weeks of age for mechanistic studies |
Applications | BB-Cl-amidine treatment fully prevented diabetes development, with all mice free of diabetes until 25 weeks of age, against 44% diabetes free in DMSO-treated mice. |
| 产品描述 | BB-Cl-Amidine, a peptidylarginine deminase (PAD) inhibitor, is frequently used to study PAD function.[1] In vitro experiment it shown that after 48 h of treatment with 0 to 20 μM BB-Cl-Amidine caused a dose-dependent decrease in cell viability in canine and feline mammary tumor cells.[1]In vitro, Cl-amidine and BB-Cl-Amidine show similar potencies and selectivities in U2OS cells, the cellular potency of BB-Cl-Amidine is increased by more than 20-fold, with EC50 values of 8.8±0.6 μM in U2OS osteosarcoma cells.[5] In vivo efficacy test it exhibited that treatment with 1 μg/ml BB-Cl-Amidine intraperitoneally for two weeks in xenograft mice, BB-Cl-Amidine-treated tumors became crusty and the surrounding skin showed hair loss. There was an or a slight increase in apoptotic cells in the BB-Cl-Amidine-treated canine or feline xenograft tumors.[1]In vitro, at concentrations around 15-20 μM and 4 μM, respectively, BB-Cl-Amidine inhibited both PAD isoforms in a dose-dependent manner with 90% inhibition of PAD2 and PAD4.[2] In vivo, arthritic mice were treated with 10 mg/kg BB-Cl-Amidine, there was a reduction in inflammation and joint destruction.[3]In vivo, treatment with 1 mg/kg BB-Cl-Amidine intraperitoneally and Ac-YVAD-cmk (a pyroptosis inhibitor) attenuated NET levels in BALF and neutrophil infiltration in alveoli.[4]In vivo, treatment with 1 mg/kg BB-Cl-Amidine subcutaneously obviously reduced splenomegaly in MRL/lpr mice and improved endothelium-dependent vasorelaxation.[5] References: |
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