Thalidomide-5,6-Cl is the Thalidomide-based cereblon ligand used in the recruitment of CRBN protein. Thalidomide-5,6-Cl can be connected to the ligand for protein by a linker to form PROTACs.
体外研究 (In Vitro)
Thalidomide-5,6-Cl is the Thalidomide-based cereblon ligand used in the recruitment of CRBN protein. Thalidomide-5,6-Cl can be connected to the ligand for protein by a linker to form PROTACs.
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量
327.12
Formula
C13H8Cl2N2O4
CAS 号
2648939-40-4
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献
[1]. Zhang NN, et, al. A Thermostable mRNA Vaccine against COVID-19. Cell. 2020 Sep 3;182(5):1271-1283.e16.
Thalidomide-5-PEG2-Cl is the Thalidomide-based cereblon ligand used in the recruitment of CRBN protein. Thalidomide-5-PEG2-Cl can be connected to the ligand for protein by a linker to form PROTACs[1].
IC50 & Target[1]
Cereblon
体外研究 (In Vitro)
PROTACs contain two different ligands connected by a linker; one is a ligand for an E3 ubiquitin ligase and the other is for the target protein. PROTACs exploit the intracellular ubiquitin-proteasome system to selectively degrade target proteins[1].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量
380.78
Formula
C17H17ClN2O6
CAS 号
2230956-57-5
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献
[1]. Nalawansha DA, et al. PROTACs: An Emerging Therapeutic Modality in Precision Medicine. Cell Chem Biol. 2020;27(8):998-994.
Thalidomide-5,6-Cl is the Thalidomide-based cereblon ligand used in the recruitment of CRBN protein. Thalidomide-5,6-Cl can be connected to the ligand for protein by a linker to form PROTACs.
体外研究 (In Vitro)
Thalidomide-5,6-Cl is the Thalidomide-based cereblon ligand used in the recruitment of CRBN protein. Thalidomide-5,6-Cl can be connected to the ligand for protein by a linker to form PROTACs.
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量
327.12
Formula
C13H8Cl2N2O4
CAS 号
2648939-40-4
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献
[1]. Zhang NN, et, al. A Thermostable mRNA Vaccine against COVID-19. Cell. 2020 Sep 3;182(5):1271-1283.e16.
Thalidomide-5-PEG2-Cl is the Thalidomide-based cereblon ligand used in the recruitment of CRBN protein. Thalidomide-5-PEG2-Cl can be connected to the ligand for protein by a linker to form PROTACs[1].
IC50 & Target[1]
Cereblon
体外研究 (In Vitro)
PROTACs contain two different ligands connected by a linker; one is a ligand for an E3 ubiquitin ligase and the other is for the target protein. PROTACs exploit the intracellular ubiquitin-proteasome system to selectively degrade target proteins[1].
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
分子量
380.78
Formula
C17H17ClN2O6
CAS 号
2230956-57-5
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献
[1]. Nalawansha DA, et al. PROTACs: An Emerging Therapeutic Modality in Precision Medicine. Cell Chem Biol. 2020;27(8):998-994.
Thalidomide-5,6-Cl is the Thalidomide-based cereblon ligand used in the recruitment of CRBN protein. Thalidomide-5,6-Cl can be connected to the ligand for protein by a linker to form PROTACs.
体外研究 (In Vitro)
Thalidomide-5,6-Cl is the Thalidomide-based cereblon ligand used in the recruitment of CRBN protein. Thalidomide-5,6-Cl can be connected to the ligand for protein by a linker to form PROTACs.
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
分子量
327.12
Formula
C13H8Cl2N2O4
CAS 号
2648939-40-4
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献
[1]. Zhang NN, et, al. A Thermostable mRNA Vaccine against COVID-19. Cell. 2020 Sep 3;182(5):1271-1283.e16.
Fludarabine-Cl has inhibition effect on RNA adenosine deaminase 1(ADAR1), and can be used for preventing and/or treating cancer or tumor-related diseases[1].
分子量
303.68
Formula
C10H11ClFN5O3
CAS 号
2734853-80-4
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献
[1]. Polysubstituted purine compound and preparation method and application thereof. CN113549076A.
Fludarabine-Cl has inhibition effect on RNA adenosine deaminase 1(ADAR1), and can be used for preventing and/or treating cancer or tumor-related diseases[1].
分子量
303.68
Formula
C10H11ClFN5O3
CAS 号
2734853-80-4
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献
[1]. Polysubstituted purine compound and preparation method and application thereof. CN113549076A.
Fludarabine-Cl has inhibition effect on RNA adenosine deaminase 1(ADAR1), and can be used for preventing and/or treating cancer or tumor-related diseases[1].
分子量
303.68
Formula
C10H11ClFN5O3
CAS 号
2734853-80-4
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献
[1]. Polysubstituted purine compound and preparation method and application thereof. CN113549076A.
Verteporfin (CL 318952) is a photosensitizer for photodynamic therapy to eliminate the abnormal blood vessels in the eye associated with conditions such as age-related macular degeneration. Verteporfin is a YAP inhibitor which disrupts YAP-TEAD interactions. Verteporfin induces cell apoptosis[1]. Verteporfinis an autophagy inhibitor that blocks autophagy at an early stage by inhibiting autophagosome formation[3].
IC50 & Target
IC50: YAP-TEAD interaction
体外研究 (In Vitro)
Verteporfin is specifically selected by PDX-cell screening. The concentrations to cause 50% growth inhibition (GI50) for PhLO, PhLH, and PhLK are 228 nM, 395 nM, and 538 nM, respectively, whereas GI50 for ALL-1, TCC-Y/sr, and NPhA1 are 3.93 µM, 2.11 µM, and 5.61 µM, respectively. GSH significantly reduces the sensitivity of 2 out of 3 PDX cells to verteporfin. Verteporfin reduces the mitochondrial membrane potential in PDX cells[1]. Verteporfin reduces the PTX-resistance on HCT-8/T cells by inhibiting YAP expression and combination therapy with verteporfin and NSC 125973 shows synergism on inhibition of YAP and cytotoxicity to HCT-8/T[2].
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究 (In Vivo)
Verteporfin (10 mg/kg, c.s.c.) and BMS-354825 significantly reduces the leukemia cell ratio, and combined therapy further reduced the number of leukemia cells in the spleen[1].
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
分子量
718.79
Formula
C82H84N8O16
CAS 号
129497-78-5
中文名称
维替泊芬
运输条件
Room temperature in continental US; may vary elsewhere.
Solubility: 2.5 mg/mL (3.48 mM); Suspended solution; Need ultrasonic
7.
请依序添加每种溶剂: 10% DMF 90% corn oil
Solubility: 2.5 mg/mL (3.48 mM); Clear solution; Need ultrasonic
*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献
[1]. Morishita T, et al. The photosensitizer verteporfin has light-independent anti-leukemic activity for Ph-positive acute lymphoblastic leukemia and synergistically works with BMS-354825. Oncotarget. 2016 Aug 2.
[2]. Pan W, et al. Verteporfin can Reverse the NSC 125973 Resistance Induced by YAP Over-Expression in HCT-8/T Cells without Photoactivation through Inhibiting YAP Expression. Cell Physiol Biochem. 2016;39(2):481-90.
[3]. Donohue E, et al. The autophagy inhibitor verteporfin moderately enhances the antitumor activity of gemcitabine in a pancreatic ductal adenocarcinoma model.J Cancer. 2013 Aug 28;4(7):585-96.
Cell Assay [1]
PDX cells co-cultured with S17 cells are treated with 16 combinations of verteporfin (60 nM, 120 nM, 180 nM, and 240 nM) and BMS-354825 (12 nM, 24 nM, 36 nM, and 48 nM). The viabilities of cells treated with each combination are measured after 48 h using FACS Aria flow cytometer. In order to estimate drug interaction between verteporfin and BMS-354825, a normalized isobologram and fraction affectedcombination index (CI) plot are made using CompuSyn software. CI values greater than 1.0 indicated antagonistic effects, equal to 1.0 additive effects, and below 1.0 synergistic effects.
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration [1]
Mice: PhLO cells (1.0×107/mouse) are injected intravenously into 6-week-old male NOG mice, which are then treated with vehicle, verteporfin (140 mg/kg/day), BMS-354825 (20 mg/kg/day), and a combination of these drugs from days 22 to 28. Verteporfin is administered by continuous subcutaneous infusion (c.s.c.) using Alzet osmotic pumps. An intraperitoneal injection (i.p.) is performed for BMS-354825. All mice are sacrificed on day 28 and the chimerism of leukemia cells is investigated by flow cytometer using an anti-human CD19 antibody and antimouse CD45 antibody. Blood concentrations of verteporfin are calculated by LCMS-2020.
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献
[1]. Morishita T, et al. The photosensitizer verteporfin has light-independent anti-leukemic activity for Ph-positive acute lymphoblastic leukemia and synergistically works with BMS-354825. Oncotarget. 2016 Aug 2.
[2]. Pan W, et al. Verteporfin can Reverse the NSC 125973 Resistance Induced by YAP Over-Expression in HCT-8/T Cells without Photoactivation through Inhibiting YAP Expression. Cell Physiol Biochem. 2016;39(2):481-90.
[3]. Donohue E, et al. The autophagy inhibitor verteporfin moderately enhances the antitumor activity of gemcitabine in a pancreatic ductal adenocarcinoma model.J Cancer. 2013 Aug 28;4(7):585-96.
Cl-amidine is an orally active peptidylarginine deminase (PAD) inhibitor, with IC50 values of 0.8 μM, 6.2 μM and 5.9 μM for PAD1, PAD3, and PAD4, respectively. Cl-amidine induces apoptosis in cancer cells. Cl-amidine induces microRNA (miR)-16 (miRNA-16, microRNA-16) expression and causes cell cycle arrest. Cl-Amidine prevents histone 3 citrullination and neutrophil extracellular trap formation, and improves survival in a murine sepsis model[1][2][3][4][5].
Cl-amidine is a bioavailable haloacetamidine-based compound that inhibits all the active PAD isozymes with near equal potency (kinact/KI=13,000 M-1•min-1 for PAD4)[1]. Cl-amidine (0, 5, 10, 15, 20, 25, 50 μg/mL, 24 hours) induces apoptosis in TK6 lymphoblastoid cells and HT29 colon cancer cells in a dose-dependent manner. Interestingly, the colon cancer cell line (HT29) is relatively resistant to apoptosis caused by Cl-amidine[2]. Cl-amidine irreversibly inactivates PADs by covalently modifying an active site cysteine that is important for its catalytic activity[4].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
Apoptosis Analysis[2].
Cell Line:
TK6 lymphoblastoid cells and HT29 colon cancer cells.
Concentration:
0, 5, 10, 15, 20, 25, 50 μg/mL.
Incubation Time:
24 h.
Result:
Induced apoptosis dose-dependently.
体内研究 (In Vivo)
Cl-amidine (75 mg/kg, ip once daily) suppresses and treats DSS-induced colitis in mice[2]. Cl-amidine (5, 25, 75 mg/kg, oral gavage, once daily) leads to significant reductions in the histology scores dose-dependently[2].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model:
C57BL/6 mice (8-12 wk old, DSS mouse model of colitis)[2].
Dosage:
75 mg/kg.
Administration:
IP once daily.
Result:
Suppressed PAD activity, protein citrullination, and PAD levels in the colon in vivo.
Animal Model:
C57BL/6 mice (8-12 wk old, DSS mouse model of colitis)[2].
Dosage:
5, 25, 75 mg/kg.
Administration:
Oral gavage once daily.
Result:
Led to significant reductions in the histology scores.
分子量
310.78
Formula
C14H19ClN4O2
CAS 号
913723-61-2
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献
[1]. Yuan Luo, et al. Inhibitors and Inactivators of Protein Arginine Deiminase 4: Functional and Structural Characterization. Biochemistry. 2006 Oct 3; 45(39): 11727–11736.
[2]. Chumanevich AA, et al. Suppression of colitis in mice by Cl-amidine: a novel peptidylarginine deiminase inhibitor. Am J Physiol Gastrointest Liver Physiol. 2011 Jun;300(6):G929-38.
[3]. Witalison EE, et al. Molecular targeting of protein arginine deiminases to suppress colitis and prevent colon cancer. Oncotarget. 2015 Nov 3;6(34):36053-62.
[4]. Biron BM, et al., Cl-Amidine Prevents Histone 3 Citrullination and Neutrophil Extracellular Trap Formation, and Improves Survival in a Murine Sepsis Model. J Innate Immun. 2017;9(1):22-32.
[5]. Bryan Knuckley, et al. Substrate Specificity and Kinetic Studies of PADs 1, 3, and 4 Identify Potent and Selective Inhibitors of Protein Arginine Deiminase 3. Biochemistry. 2010 Jun 15;49(23):4852-63.
CL2-SN-38 是 (ADC) 的一部分,能与抗 trop -2人源化抗体 hRS7 结合。SN-38 是一种 DNA 拓扑异构酶 I 抑制剂。抗体药物偶联物 anti-Trop-2 hRS7-CL2A-SN-38 对多种人体实体肿瘤具有显著的特异性的抗肿瘤作用。
CL2-SN-38 Chemical Structure
CAS No. : 1036969-20-6
规格
价格
是否有货
数量
5 mg
¥2300
In-stock
10 mg
¥3500
In-stock
25 mg
¥5800
In-stock
50 mg
¥10000
In-stock
100 mg
¥18000
In-stock
200 mg
询价
500 mg
询价
* Please select Quantity before adding items.
生物活性
CL2-SN-38 is a part of the antibody drug conjugate (ADC), can conjugate with the anti-Trop-2-humanized antibody hRS7. SN-38 is a DNA topoisomerase I inhibitor. The anti-Trop-2 hRS7-CL2A-SN-38 ADC provides significant and specific antitumor effects against a range of human solid tumor types[1].
IC50 & Target
Camptothecins
分子量
1627.79
Formula
C82H106N12O23
CAS 号
1036969-20-6
运输条件
Room temperature in continental US; may vary elsewhere.
[1]. Cardillo TM, et al. Humanized anti-Trop-2 IgG-SN-38 conjugate for effective treatment of diverse epithelial cancers: preclinical studies in human cancer xenograft models and monkeys. Clin Cancer Res. 2011 May 15;17(10):3157-69.
Cl-amidine hydrochloride is an orally active peptidylarginine deminase (PAD) inhibitor, with IC50 values of 0.8 μM, 6.2 μM and 5.9 μM for PAD1, PAD3, and PAD4, respectively. Cl-amidine hydrochloride induces apoptosis in cancer cells. Cl-amidine hydrochloride induces microRNA (miR)-16 (miRNA-16, microRNA-16) expression and causes cell cycle arrest. Cl-Amidine hydrochloride prevents histone 3 citrullination and neutrophil extracellular trap formation, and improves survival in a murine sepsis model[1][2][3][4][5].
Cl-amidine is a bioavailable haloacetamidine-based compound that inhibits all the active PAD isozymes with near equal potency (kinact/KI=13,000 M-1•min-1 for PAD4)[1]. Cl-amidine (0, 5, 10, 15, 20, 25, 50 μg/mL, 24 hours) induces apoptosis in TK6 lymphoblastoid cells and HT29 colon cancer cells in a dose-dependent manner. Interestingly, the colon cancer cell line (HT29) is relatively resistant to apoptosis caused by Cl-amidine[2]. Cl-Amidine prevents histone 3 citrullination and neutrophil extracellular trap formation, and improves survival in a murine sepsis model[4].
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Apoptosis Analysis[2].
Cell Line:
TK6 lymphoblastoid cells and HT29 colon cancer cells.
Concentration:
0, 5, 10, 15, 20, 25, 50 μg/mL.
Incubation Time:
24 h.
Result:
Induced apoptosis dose-dependently.
体内研究 (In Vivo)
Cl-amidine (75 mg/kg, ip once daily) suppresses and treats DSS-induced colitis in mice[2]. Cl-amidine (5, 25, 75 mg/kg, oral gavage, once daily) leads to significant reductions in the histology scores dose-dependently[2].
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model:
C57BL/6 mice (8-12 wk old, DSS mouse model of colitis)[2].
Dosage:
75 mg/kg.
Administration:
IP once daily.
Result:
Suppressed PAD activity, protein citrullination, and PAD levels in the colon in vivo.
Animal Model:
C57BL/6 mice (8-12 wk old, DSS mouse model of colitis)[2].
Dosage:
5, 25, 75 mg/kg.
Administration:
Oral gavage once daily.
Result:
Led to significant reductions in the histology scores.
分子量
347.24
Formula
C14H20Cl2N4O2
CAS 号
1373232-26-8
运输条件
Room temperature in continental US; may vary elsewhere.
Solubility: 5.5 mg/mL (15.84 mM); Clear solution; Need ultrasonic
*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献
[1]. Yuan Luo, et al. Inhibitors and Inactivators of Protein Arginine Deiminase 4: Functional and Structural Characterization. Biochemistry. 2006 Oct 3; 45(39): 11727–11736.
[2]. Chumanevich AA, et al. Suppression of colitis in mice by Cl-amidine: a novel peptidylarginine deiminase inhibitor. Am J Physiol Gastrointest Liver Physiol. 2011 Jun;300(6):G929-38.
[3]. Witalison EE, et al. Molecular targeting of protein arginine deiminases to suppress colitis and prevent colon cancer. Oncotarget. 2015 Nov 3;6(34):36053-62.
[4]. Biron BM, et al., Cl-Amidine Prevents Histone 3 Citrullination and Neutrophil Extracellular Trap Formation, and Improves Survival in a Murine Sepsis Model. J Innate Immun. 2017;9(1):22-32.
Cl-C6-PEG4-O-CH2COOH (PROTAC Linker 4) is a PEG-based PROTAC linker can be used in the synthesis of chloroalkane-containing PROTACs (HaloPROTACs)[1].
IC50 & Target
PEGs
体外研究 (In Vitro)
PROTACs contain two different ligands connected by a linker; one is a ligand for an E3 ubiquitin ligase and the other is for the target protein. PROTACs exploit the intracellular ubiquitin-proteasome system to selectively degrade target proteins[1].
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
分子量
370.87
Formula
C16H31ClO7
CAS 号
1799506-30-1
运输条件
Room temperature in continental US; may vary elsewhere.
[1]. Buckley DL, et al. HaloPROTACS: Use of Small Molecule PROTACs to Induce Degradation of HaloTag Fusion Proteins. ACS Chem Biol. 2015 Aug 21;10(8):1831-7.
D-Cl-amidine is a potent and highly selective PAD1 inhibitor. D-Cl-amidine is well-torelated with no significant toxicity[1].
体外研究 (In Vitro)
D-Cl-amidine (200-400 μM) is effective in significantly decreasing cell viability in MDA-MB-231 cells[1]. D-Cl-amidine increase caspase 3 activity, indicating that inhibition of PAD1 leads to an increase in apoptosis[1].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究 (In Vivo)
D-Cl-amidine, administered by iv at a dose of 2.5 mg/kg, is still detected after 2 h in serum at a concentration of ~21 nM and at 4 h at ~10 nM. D-Cl-amidine is still observed in the blood serum at a concentration of ∼10 nM at 4 h when administered by ip at a dose of 10 mg/kg[1].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量
310.78
Formula
C14H19ClN4O2
CAS 号
1404060-15-6
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献
[1]. Bicker KL, et al. D-amino acid based protein arginine deiminase inhibitors: Synthesis, pharmacokinetics, and in cellulo efficacy. ACS Med Chem Lett. 2012 Oct 26;3(12):1081-1085.
Cl-amidine TFA is an orally active peptidylarginine deminase (PAD) inhibitor, with IC50 values of 0.8 μM, 6.2 μM and 5.9 μM for PAD1, PAD3, and PAD4, respectively. Cl-amidine TFA induces apoptosis in cancer cells. Cl-amidine TFA induces microRNA (miR)-16 (miRNA-16, microRNA-16) expression and causes cell cycle arrest. Cl-Amidine TFA prevents histone 3 citrullination and neutrophil extracellular trap formation, and improves survival in a murine sepsis model[1][2][3][4][5].
Cl-amidine is a bioavailable haloacetamidine-based compound that inhibits all the active PAD isozymes with near equal potency (kinact/KI=13,000 M-1•min-1 for PAD4)[1]. Cl-amidine (0, 5, 10, 15, 20, 25, 50 μg/mL, 24 hours) induces apoptosis in TK6 lymphoblastoid cells and HT29 colon cancer cells in a dose-dependent manner. Interestingly, the colon cancer cell line (HT29) is relatively resistant to apoptosis caused by Cl-amidine[2]. Cl-amidine irreversibly inactivates PADs by covalently modifying an active site cysteine that is important for its catalytic activity[4].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
Apoptosis Analysis[2].
Cell Line:
TK6 lymphoblastoid cells and HT29 colon cancer cells.
Concentration:
0, 5, 10, 15, 20, 25, 50 μg/mL.
Incubation Time:
24 h.
Result:
Induced apoptosis dose-dependently.
体内研究 (In Vivo)
Cl-amidine (75 mg/kg, ip once daily) suppresses and treats DSS-induced colitis in mice[2]. Cl-amidine (5, 25, 75 mg/kg, oral gavage, once daily) leads to significant reductions in the histology scores dose-dependently[2].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model:
C57BL/6 mice (8-12 wk old, DSS mouse model of colitis)[2].
Dosage:
75 mg/kg.
Administration:
IP once daily.
Result:
Suppressed PAD activity, protein citrullination, and PAD levels in the colon in vivo.
Animal Model:
C57BL/6 mice (8-12 wk old, DSS mouse model of colitis)[2].
Dosage:
5, 25, 75 mg/kg.
Administration:
Oral gavage once daily.
Result:
Led to significant reductions in the histology scores.
分子量
424.80
Formula
C16H20ClF3N4O4
CAS 号
1043444-18-3
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献
[1]. Yuan Luo, et al. Inhibitors and Inactivators of Protein Arginine Deiminase 4: Functional and Structural Characterization. Biochemistry. 2006 Oct 3; 45(39): 11727–11736.
[2]. Chumanevich AA, et al. Suppression of colitis in mice by Cl-amidine: a novel peptidylarginine deiminase inhibitor. Am J Physiol Gastrointest Liver Physiol. 2011 Jun;300(6):G929-38.
[3]. Witalison EE, et al. Molecular targeting of protein arginine deiminases to suppress colitis and prevent colon cancer. Oncotarget. 2015 Nov 3;6(34):36053-62.
[4]. Biron BM, et al., Cl-Amidine Prevents Histone 3 Citrullination and Neutrophil Extracellular Trap Formation, and Improves Survival in a Murine Sepsis Model. J Innate Immun. 2017;9(1):22-32.
[5]. Bryan Knuckley, et al. Substrate Specificity and Kinetic Studies of PADs 1, 3, and 4 Identify Potent and Selective Inhibitors of Protein Arginine Deiminase 3. Biochemistry. 2010 Jun 15;49(23):4852-63.
Fmoc-L-Tyr(2,6-Cl2-Bzl)-OH is an Fmoc protected tyrosine derivative that is potentially useful for proteomics studies and solid phase peptide synthesis techniques. Tyrosine is a very important amino acid – one of the few amino acids which is phosphorylated to vary the physical properties of the peptides, and is a precursor for the formation of iodinated thyroid hormones. The Fmoc group is typically removed with a base such as pyridine – an orthogonal de-protection strategy to the acid labilie Boc group.