【APExBIO -Proteases系列產品】Z-IETD-FMK/Z-VAD-FMK/TAPI-1-APExBIO台灣銷售
APExBIO –Proteases系列產品 (240+種)
蛋白酶(Proteases)也稱為肽酶(peptidases)或蛋白水解酶(proteolytic enzymes)，由大量催化肽鍵水解(hydrolysis)並隨後導致蛋白質底物(protein substrates)降解為氨基酸(amino acids)的酶組成。蛋白酶(Proteases)與多種人類疾病有關，包括癌症(cancer)、神經退行性疾病(neurodegenerative disorders)、炎症性疾病(inflammatory diseases)和心血管疾病(cardiovascular diseases)。因此，許多蛋白酶抑制劑【小分子(small molecules)和蛋白質】已被鑑定為阻斷蛋白酶的活性(proteases)。蛋白酶抑制劑可以根據它們通過兩種一般機制抑制的蛋白酶類別分為不同的類型，即不可逆的“捕獲(trapping)”反應和可逆(reversible)的緊密結合反應。蛋白酶抑制劑已被用作治療蛋白酶相關疾病的診斷劑(diagnostic)或治療劑(therapeutic agents)。
Z-IETD-FMK | CAS# 210344-98-2 APExBIO 貨號B3232
Product Citation+6
Z-IETD-FMK is an inhibitor of caspase 8 [1].
Z-IETD-FMK 是半胱天冬酶 8 的抑制劑 [1]。Z-IETD-FMK 抑制 PHA 或抗 CD3 加抗 CD28 誘導的 T 細胞增殖，而對resting 的T cells沒有毒性。這種抑制 Z-IETD-FMK 的機制已被證明不是通過對 IL-2 分泌或 IFN-γ 產生的影響，而是通過降低 CD25 表達。實驗表明，在沒有激活信號的情況下，Z-IETD-FMK對正常細胞生長沒有影響。還發現 Z-IETD-FMK 在濃度為 100 μM 時顯著抑制 NF-κB 活化 [1]。除了抑制細胞增殖的能力外，據報導 Z-IETD-FMK 還能抑制 TRAIL 介導的細胞殺傷。它保護 procaspase 9、2 和 3，並在 HCT116 和 SW480 細胞中以相似的程度保護 PARP [2]。
| Storage | Store at -20°C |
| M.Wt | 654.68 |
| Cas No. | 210344-98-2 |
| Formula | C30H43FN4O11 |
| Synonyms | Benzyloxycarbonyl-Ile-Glu(OMe)-Thr-Asp(OMe)-fluoromethylketone, Z-Ile-Glu(OMe)-Thr-Asp(OMe)-FMK |
| Solubility | ≥32.73 mg/mL in DMSO; insoluble in EtOH; insoluble in H2O |
| Chemical Name | methyl 5-[[1-[(5-fluoro-1-methoxy-1,4-dioxopentan-3-yl)amino]-3-hydroxy-1-oxobutan-2-yl]amino]-4-[[3-methyl-2-(phenylmethoxycarbonylamino)pentanoyl]amino]-5-oxopentanoate |
| SDF | Download SDF |
| Canonical SMILES | CCC(C)C(C(=O)NC(CCC(=O)OC)C(=O)NC(C(C)O)C(=O)NC(CC(=O)OC)C(=O)CF)NC(=O)OCC1=CC=CC=C1 |
| Shipping Condition | Ship with blue ice, or upon other requests. |
| General tips | For obtaining a higher solubility, please warm the tube at 37°C and shake it in the ultrasonic bath for a while. We do not recommend long-term storage for the solution, please use it up soon. |
APExBIO台灣代理商
APExBIO提供優質的胜肽和生物分析試劑，廣泛產品線如Protease、Chromatin/Epigenetics表觀遺傳學、MAPK Signal、DNA Damege/DNA repair、細胞凋亡、腫瘤生物學、Stem cell等研究領域， 還提供定制的服務，包括多肽合成，抗體的生產和檢測的發展。產品線DNA/RNA prep kit、Drug Screening panel、Bioactive peptides、Growth factors、Biotinylation Reagents、tag peptides、amino Acids、Growth factors等。APExBIO產品質量都伴隨著證書的分析，高效液相色譜，質譜，和HMNR數據。
- 1. Jiamin Yi, Jiangling Peng, et al. “Degradation of Host Proteins and Apoptosis Induced by Foot-and-Mouth Disease Virus 3C Protease.” Pathogens. 2021 Nov 30;10(12):1566. PMID:34959521
- 2. Jiangqi Zhao, Xuyan Huang, et al. “Toll-like receptor 3 is an endogenous sensor of cell death and a potential target for induction of long-term cardiac transplant survival.” Am J Transplant. 2021 Oct;21(10):3268-3279. PMID:33784431
- 3. Melissa S Phuong, Rafael E Hernandez, et al. “Impairment in inflammasome signaling by the chronic Pseudomonas aeruginosa isolates from cystic fibrosis patients results in an increase in inflammatory response.” Cell Death Dis. 2021 Mar 4;12(3):241. PMID:33664232
- 4. Yang Pan, Yu-miao Pan, et al. “MicroRNA-98 ameliorates doxorubicin-induced cardiotoxicity via regulating caspase-8 dependent Fas/RIP3 pathway.” Environ Toxicol Pharmacol. 2021 Jul;85:103624. PMID:33617954
- 5. Chen Z, Xu G, et al. “Lobaplatin induces pyroptosis through regulating cIAP1/2, Ripoptosome and ROS in nasopharyngeal carcinoma.” Biochem Pharmacol. 2020;177:114023. PMID:32413426
- 6. Zhao M, Duan X, et al. “A Novel Role for PX, a Structural Protein of Fowl Adenovirus Serotype 4 (FAdV4), as an Apoptosis-Inducer in Leghorn Male Hepatocellular Cell.” Cell. Viruses. 2020;12(2):E228. PMID:32085479
Z-VAD-FMK | CAS# 187389-52-2 APExBIO 貨號 A1902
Product Citation+6
Z-VAD-FMK 是一種 ICE 樣蛋白酶抑制劑(ICE-like proteases)，可抑制由多種刺激物誘導的 THP.1 細胞凋亡(apoptosis)和 Fas 抗原誘導的 Jurkat T 細胞凋亡(apoptosis)。它通過阻止 proCPP32 活化為其活性形式來抑制細胞凋亡(apoptosis)，而不是通過直接阻止 CPP32 的蛋白水解作用來抑制細胞凋亡(apoptosis)。Z-VAD-FMK almost completely inhibited the formation of large kilobasepair induced by all four stimuli. Similarly Z-VAD-FMK almost completely inhibited the enhanced formation of large kilobasepair fragments induced by thapsigargin or cycloheximide in the presence of TLCK, in good agreement with its ability to inhibit apoptosis induced by these treatments. These stimuli also induced internucleosomal cleavage of DNA, which was inhibited by Z-VAD-FMK. These results suggested that an ICE-like protease(s) acts at a stage prior to the formation of large kilobasepair fragments of DNA3.
- 1. Jingchun Du, Yougui Xiang, et al. “RIPK1 dephosphorylation and kinase activation by PPP1R3G/PP1γ promote apoptosis and necroptosis.” Nat Commun. 2021 Dec 3;12(1):7067. PMID:34862394
- 2. Xinxin Ren, Xiang Wang, et al. “Significance of TEAD Family in Diagnosis, Prognosis and Immune Response for Ovarian Serous Carcinoma.” Int J Gen Med. 2021 Oct 27;14:7133-7143. PMID:34737608
- 3. Du Yu, Yundi Zhao, et al. “C19orf66 Inhibits Japanese Encephalitis Virus Replication by Targeting -1 PRF and the NS3 Protein.” Virol Sin. 2021 Dec;36(6):1443-1455. PMID:34309824
- 4. Chunhua Shu, Rui Wang, et al. “The “Dextran-Magnetic Layered Double Hydroxide-Fluorouracil” Drug Delivery System Exerts Its Anti-tumor Effect by Inducing Lysosomal Membrane Permeability in the Process of Cell Death.” Biol Pharm Bull. 2021 Oct 1;44(10):1473-1483. PMID:34305072
- 5. Qionghui Zhan, Jaepyo Jeon, et al. “CAMK2/CaMKII activates MLKL in short-term starvation to facilitate autophagic flux.” Autophagy. 2022 Apr;18(4):726-744. PMID:34282994
- 6. Jia-yuan Zhang, Bo Zhou, et al. “The metabolite α-KG induces GSDMC-dependent pyroptosis through death receptor 6-activated caspase-8.” Cell Res. 2021 Sep;31(9):980-997. PMID:34012073
| Storage | Store at -20°C |
| M.Wt | 467.49 |
| Cas No. | 187389-52-2 |
| Formula | C22H30FN3O7 |
| Synonyms | Benzyloxycarbonyl-Val-Ala-Asp(OMe)-fluoromethylketone,Z-Val-Ala-Asp(OMe)-FMK |
| Solubility | ≥23.37 mg/mL in DMSO; insoluble in EtOH; insoluble in H2O |
| Chemical Name | methyl (3S)-5-fluoro-3-[[(2S)-2-[[(2S)-3-methyl-2-(phenylmethoxycarbonylamino)butanoyl]amino]propanoyl]amino]-4-oxopentanoate |
| SDF | Download SDF |
| Canonical SMILES | CC(C)C(C(=O)NC(C)C(=O)NC(CC(=O)OC)C(=O)CF)NC(=O)OCC1=CC=CC=C1 |
| Shipping Condition | Ship with blue ice, or upon other requests. |
| General tips | For obtaining a higher solubility, please warm the tube at 37°C and shake it in the ultrasonic bath for a while. We do not recommend long-term storage for the solution, please use it up soon. |
Talabostat mesylate | CAS# 150080-09-4 APExBIO 貨號B3941
Product Citation+6
Talabostat mesilate (PT-100; Val-boroPro) 是一種具有口服活性的 DPP4 二肽基肽酶特異性抑制劑，包括腫瘤相關成纖維細胞活化蛋白 (Fibroblast activation protein , FAP)。成纖維細胞活化蛋白- (Fibroblast activation protein , FAP)，作為一種完整的膜絲氨酸蛋白酶(integral membrane serine protease)和後脯氨酰肽酶家族(post-prolyl peptidase family)的成員，與二肽基肽酶 IV (dipeptidyl peptidase IV ,DPPIV) 密切相關，並顯示具有特徵性 I-水解酶(characteristic)和八葉螺旋槳的 DPPIV 樣折疊域(DPPIV-like fold )。體外(In vitro) 通過切割 N 端 Xaa-Pro 或 Xaa-Ala 殘基，talabostat 阻斷二肽基肽酶(dipeptidyl peptidases)，例如成纖維細胞活化蛋白 (fibroblast activation protein , FAP)，從而誘導細胞因子(cytokine)和趨化因子的產生（除了特異性 T 細胞免疫和T 細胞依賴性活性）。該藥劑還可以誘導集落刺激因子的產生，例如粒細胞集落刺激因子（G-CSF），從而誘導造血。二肽基肽酶是指多肽激素和趨化因子的活化。Talabostat 略微降低了表達 FAP 的腫瘤的生長速率，但由於 PT-630 和 LAF-237 沒有，因此生長阻斷可能與抑制 FAP 或相關的脯氨酰肽酶後二肽基肽酶 IV 無關。 體內：到目前為止，還沒有進行體內研究。臨床試驗：已進行臨床研究。
- Andreas Linder, Stefan Bauernfried, et al. “CARD8 inflammasome activation triggers pyroptosis in human T cells.” EMBO J 2020 Aug 25;e105071.PMID:32840892
- Chen M, Lei X, et al. “Pericyte-targeting prodrug overcomes tumor resistance to vascular disrupting agents.” J Clin Invest. 2017 Oct 2;127(10):3689-3701.PMID:28846068
- Feng X, Wang Q, et al. “A synthetic urinary probe-coated nanoparticles sensitive to fibroblast activation protein α for solid tumor diagnosis.” Int J Nanomedicine. 2017 Jul 27;12:5359-5372.PMID:28794628
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 310.18 |
| Cas No. | 150080-09-4 |
| Formula | C10H23BN2O6S |
| Solubility | ≥11.45 mg/mL in DMSO; ≥31 mg/mL in H2O; ≥8.2 mg/mL in EtOH with ultrasonic |
| SDF | Download SDF |
| Canonical SMILES | OS(=O)(C)=O.O=C([C@H](C(C)C)N)N1[C@H](B(O)O)CCC1 |
| Shipping Condition | Ship with blue ice, or upon other requests. |
| General tips | For obtaining a higher solubility, please warm the tube at 37°C and shake it in the ultrasonic bath for a while. We do not recommend long-term storage for the solution, please use it up soon. |
Cisplatin | CAS# 15663-27-1 APExBIO 貨號A8321
Product Citation+12
一種高效、廣譜的化療藥物[1]。
Cisplatin是一種具有一些副作用的抗癌劑(chemotherapeutic agent)。據信它通過幾種機制誘導細胞凋亡(apoptosis)。傳統的機制是Cisplatin進入細胞，與DNA鳥嘌呤鹼基(DNA guanine bases)相互作用，形成鏈間(inter-)或鏈內交聯(intra-strand chain cross-linking)，從而阻止DNA的複雜(replication)。這種形成還可以通過激活 p53 來誘導細胞凋亡(apoptosis)。還發現Cisplatin會導致 ROS 產生並增加脂質過氧化(lipid peroxidation)，從而導致細胞進入凋亡途徑(apoptotic pathway)。此外，Cisplatin通過半胱天冬酶依賴性途徑(caspase-dependent pathway)誘導細胞凋亡(apoptosis)。在耳蝸細胞(cochlear cells)中，Cisplatin治療導致 caspase-3 和 -9 增加，並引起耳蝸(cochlear damage)損傷副作用 [1]。
- JING CHU, JINGHAI GAO, et al. “Mechanism of hydrogen on cervical cancer suppression revealed by high‑throughput RNA sequencing.” Oncol Rep. 2021 Jul;46(1):141.PMID:34080660
- Gang Wang, Qikai Sun, et al. “The stabilization of yes-associated protein by TGFβ-activated kinase 1 regulates the self-renewal and oncogenesis of gastric cancer stem cells.” J Cell Mol Med. 2021 Jul;25(14):6584-6601.PMID:34075691
- Cheng-Wei Chou, Ri-Yao Yang, et al. “The stabilization of PD-L1 by the endoplasmic reticulum stress protein GRP78 in triple-negative breast cancer.” Am J Cancer Res 2020 Aug 1;10(8):2621-2634.PMID:32905506
- Guo J, Xu G, et al. “Low Expression of Smurf1 Enhances the Chemosensitivity of Human Colorectal Cancer to Gemcitabine and Cisplatin in Patient-Derived Xenograft Models.” Transl Oncol. 2020;13(9):100804.PMID:32512228
- Li A, Cao W, et al. “Gefitinib sensitization of cisplatin-resistant wild-type EGFR non-small cell lung cancer cells.” J Cancer Res Clin Oncol. 2020;146(7):1737-1749.PMID:32342201
- Mikhail Chesnokov, Imran Khan, et al. “The MEK1/2 pathway as a therapeutic target in high-grade serous ovarian carcinoma.” bioRxiv. 2019 September 16.
| Physical Appearance | A solid |
| Storage | Store at RT It is recommended to store in the form of powder in the dark, the solution is very unstable (Prepare Solution fresh and use at room temperature), DMF is recommended, DMSO can inactivate Cisplatin’s activity. |
| M.Wt | 300.05 |
| Cas No. | 15663-27-1 |
| Formula | Cl2H6N2Pt |
| Synonyms | CDDP |
| Solubility | insoluble in EtOH; insoluble in H2O; ≥12.5 mg/mL in DMF |
| Chemical Name | azane;dichloroplatinum(2+) |
| SDF | Download SDF |
| Canonical SMILES | N.N.Cl[Pt+2]Cl |
| Shipping Condition | Ship with blue ice, or upon other requests. |
| General tips | For obtaining a higher solubility, please warm the tube at 37°C and shake it in the ultrasonic bath for a while. We do not recommend long-term storage for the solution, please use it up soon. |
17-DMAG (Alvespimycin) HCl | CAS#467214-21-7 APExBIO 貨號A2213
Product Citation+3
Hsp90 inhibitor
17-DMAG 是 Hsp90 的抑制劑，IC50 值為 62±29nM [1]。17-DMAG 可以與 Hsp90 的 ATP 結合基序結合，抑制 Hsp90 的蛋白chaperoning活性。它將導致 Hsp90 的client proteins（如 EGFR、AKT、突變 p53 和 IKK）的錯誤折疊(misfolding)和隨後的降解(degradation) 。由於腫瘤細胞中 17-DMAG 結合所需的 Hsp90 具有更特異性的conformation，並且 Hsp90 的許多client proteins有助於腫瘤細胞的生長，因此 17-DMAG 對腫瘤細胞的毒性通常比對正常細胞的毒性更大 [2]。據報導，17-DMAG 是一種抗腫瘤劑(ntitumor agent)，在體外和初始體內試驗中具有更廣泛的可利用活性和藥學上更易於處理的特徵。 17-DMAG在處理NCI 60細胞株時可影響細胞生長，平均GI50為0.053mM。 17-DMAG 的體內活性在四個黑色素瘤模型中使用 Freiburg 人類腫瘤異種移植組和兩個肺異種移植(lung xenografts)進行了測試。它表明 17-DMAG 在兩個肺異種移植物和四個黑色素瘤模型中的兩個中具有高活性，但在另外兩個 MEXF 462 和 MEXF 514 中沒有 [3]。
- Peng Zhou, Becky K.C. Chan, et al. “A Three-Way Combinatorial CRISPR Screen for Analyzing Interactions among Druggable Targets.” Cell Rep. 2020 Aug 11;32(6):108020.PMID:32783942
- Bhola PD, Ahmed E, et al. “High-throughput dynamic BH3 profiling may quickly and accurately predict effective therapies in solid tumors.” Sci Signal. 2020;13(636):eaay1451.PMID:32546544
- Katayama K, Noguchi K, et al. “Heat shock protein 90 inhibitors overcome the resistance to Fms-like tyrosine kinase 3 inhibitors in acute myeloid leukemia.” Oncotarget. 2018 Sep 28;9(76):34240-34258.PMID:30344940
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 653.21 |
| Cas No. | 467214-21-7 |
| Formula | C32H48N4O8·HCl |
| Solubility | ≥26.2 mg/mL in DMSO; insoluble in EtOH; ≥3.04 mg/mL in H2O |
| Chemical Name | [(3R,5S,6R,7S,8E,10S,11S,12Z,14E)-21-[2-(dimethylamino)ethylamino]-6-hydroxy-5,11-dimethoxy-3,7,9,15-tetramethyl-16,20,22-trioxo-17-azabicyclo[16.3.1]docosa-1(21),8,12,14,18-pentaen-10-yl] carbamate;hydrochloride |
| SDF | Download SDF |
| Canonical SMILES | CC1CC(C(C(C=C(C(C(C=CC=C(C(=O)NC2=CC(=O)C(=C(C1)C2=O)NCCN(C)C)C)OC)OC(=O)N)C)C)O)OC.Cl |
| Shipping Condition | Ship with blue ice, or upon other requests. |
| General tips | For obtaining a higher solubility, please warm the tube at 37°C and shake it in the ultrasonic bath for a while. We do not recommend long-term storage for the solution, please use it up soon. |
| 品項 | CAS# | #貨號 | 應用 |
| Z-VAD-FMK | CAS# 187389-52-2 | 貨號 A1902 |
Proteases ICE-like proteases |
| TAPI-1 | CAS#171235-71-5 | 貨號 B4686 |
Proteases TACE/ADAM17 inhibitor Product Citation+3 |
| Talabostat mesylate | CAS# 150080-09-4 | 貨號B3941 |
Proteases DPP4 二肽基肽酶特異性抑制劑 |
| Z-IETD-FMK | CAS# 210344-98-2 | 貨號B3232 | inhibitor of caspase 8 |
| Cisplatin | CAS# 15663-27-1 | 貨號A8321 | 高效、廣譜的化療藥物 |
| 17-DMAG (Alvespimycin) HCl | CAS#467214-21-7 | 貨號A2213 | Hsp90 inhibitor |
| CA-074 Me | CAS# 147859-80-1 | 貨號A8239 | Cathepsin B inhibitor |
| VX-765 | CAS# 273404-37-8 | 貨號A8238 | Caspase-1 inhibitor |