Z-FA-FMK
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
Z-FA-FMK是一种对照多肽氟甲基酮(boc-Thr-CH2F),是钙蛋白酶(Ac-Leu-Leu-norleucinal)、组织蛋白酶B(Z-Phe-Ala-CH2F)以及CPP32样蛋白酶(Z-Phe-Ala-CH2F)的抑制剂 [1]。在包括人类肿瘤的多种组织中,多肽氟甲基酮是引起组织蛋白酶B同工酶失活的有效化合物,以时间依赖性的方式发挥作用[2]。组织蛋白酶B和L的抑制剂Z-FA-FMK阻断选择性RRMs诱导的DEVDase活性、DNA片段化和磷脂酰丝氨酸外化。Z-FA-FMK可以抑制体外caspase活性,选择性的抑制重组效应子caspases-2、-3、-6和-7。相比之下,纯化的起始caspases 8和10不受影响,而凋亡体相关的caspase 9仅部分被抑制[3]。
Z-FA-FMK是半胱氨酸蛋白酶的抑制剂,如组织蛋白酶B,不需要P1 Asp残基。它可被用作FMK P1 Asp caspase抑制剂的阴性对照抑制剂。
参考文献:
1. Inhibition of the interleukin-1 beta converting enzyme family rescues neurons from apoptotic death.Lynch, T., Vasilakos, J.P., Raser, K., Keane, K.M., Shivers, B.D.Mol. Psychiatry(1997)
2. Visualization of time-dependent inactivation of human tumor cathepsin B isozymes by a peptidyl fluoromethyl ketone using a fluorescent print technique.Smith, R.E., Rasnick, D., Burdick, C.O., Cho, K.J., Rose, J.C., Vahratian, A.Anticancer Res.(1988)
3. Lopez-Hernandez, F. J., Ortiz, M. A., Bayon, Y., & Piedrafita, F. J. (2003). Z-FA-fmk Inhibits Effector Caspases but not Initiator Caspases 8 and 10, and Demonstrates That Novel Anticancer Retinoid-related Molecules Induce Apoptosis via the Intrinsic Pathway1.Molecular cancer therapeutics, 2(3), 255-263.
- 1. Zhijun Liu, Himani Nailwal, et al. "A class of viral inducer of degradation of the necroptosis adaptor RIPK3 regulates virus-induced inflammation." Immunity. 2021 Feb 9;54(2):247-258.e7. PMID: 33444549
- 2. Mohammed Mohasin, Katharin Balbirnie-Cumming, et al. "Macrophages utilize mitochondrial fission to enhance mROS production during responses to Streptococcus pneumoniae." bioRxiv. 2019 August 02.
- 3. Hodges AL, Kempen CG, et al. "TNF Family Cytokines Induce Distinct Cell Death Modalities in the A549 Human Lung Epithelial Cell Line when Administered in Combination with Ricin Toxin." Toxins (Basel). 2019 Aug 1;11(8). pii: E450. PMID: 31374990
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 386.42 |
Cas No. | 105637-38-5;197855-65-5 |
Formula | C21H23N2O4F |
Synonyms | Z-FA-FMK, Z-Phe-Ala-fluoromethyl ketone, Z-Phe-Ala-FMK, Zfa-FMK, Z-Phe-Ala-CH2F, Cathepsin B, Caspase Inhibitor |
Solubility | insoluble in H2O; ≥13.45 mg/mL in DMSO; ≥3.57 mg/mL in EtOH with ultrasonic |
Chemical Name | benzyl N-[1-[(4-fluoro-3-oxobutan-2-yl)amino]-1-oxo-3-phenylpropan-2-yl]carbamate |
SDF | Download SDF |
Canonical SMILES | CC(C(=O)CF)NC(=O)C(CC1=CC=CC=C1)NC(=O)OCC2=CC=CC=C2 |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |
Cell experiment:[1] | |
Cell lines |
Jurkat T cells |
Reaction Conditions |
5, 30, or 100 μM Z-FA-FMK for 1 h preincubation |
Applications |
Increasing concentrations of Z-FA-FMK prevented retinoid-related molecule (RRM)-induced DNA fragmentation and DEVDase activity. Similarly, preincubation with a high concentration of Z-FA-FMK (100 μM) significantly inhibited the externalization of phosphatidylserine induced by RRMs. Z-FA-FMK, as an inhibitor of cathepsins B and L, has been used to explore the molecular mechanism underlying the anticancer activity of RRMs. |
Animal experiment:[2] | |
Animal models |
SCID mice xenografted with Ras oncogenic HT1080 cells |
Dosage form |
0.02 mg Administered intratumorally, everyday up to 7 days post-viral injection and every 2 days until completion of the experiment. |
Applications |
Z-FA-FMK effectively blocked the replication activity of respiratory enteric orphan (reo)virus in both tumor and hear tissues. Therefore, Z-FA-FMK could serve as a potential viral inhibitor which prevents reovirus-mediated myocarditis and oncolysis in vivo. |
Note |
The technical data provided above is for reference only. |
References: 1. Lopez-Hernandez FJ, Ortiz MA, Bayon Y, et al. Z-FA-fmk inhibits effector caspases but not initiator caspases 8 and 10, and demonstrates that novel anticancer retinoid-related molecules induce apoptosis via the intrinsic pathway. Molecular Cancer Therapeutics, 2003, 2(3): 255-263. 2. Kim M, Hansen KK, Davis L, et al. Z-FA-FMK as a novel potent inhibitor of reovirus pathogenesis and oncolysis in vivo. Antiviral Therapy, 2010, 15(6): 897-905. |
Description | Z-FA-FMK是半胱氨酸蛋白酶的不可逆抑制剂 | |||||
靶点 | cysteine protease | |||||
IC50 |
质量控制和MSDS
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