Protein-Arginine-Deiminase-Inhibitors-Modulators-MCE

1、 HYPERLINK https:/www.MedChemE/Targets/Protein Arginine Deiminase.html Protein HYPERLINK https:/www.MedChemE/Targets/Protein Arginine Deiminase.html HYPERLINK https:/www.MedChemE/Targets/Protein Arginine Deiminase.html Arginine HYPERLINK https:/www.MedChemE/Targets/Protein Arginine Deiminase.html HY

2、PERLINK https:/www.MedChemE/Targets/Protein Arginine Deiminase.html DeiminasePeptidylarginine DeiminaseProtein arginine deiminase (PAD), is a group of calcium-dependent enzymes, which play crucial roles in citrullination, and cancatalyze arginine residues into citrulline. his chemical reaction induc

3、es citrullinated proteins formation with altered structure andfunction, leading to numerous pathological diseases, including inflammation and autoimmune diseases. These pathologiesestablished the PADs as therapeutic targets and multiple PAD inhibitors are known.Humans encode five PADs, designated PA

4、Ds 1-4 and PAD6. Of the five PAD isozymes (PAD1, 2, 3, 4 and 6), only four (PADs1-4) arecatalytically active. PAD activity is tightly regulated by Ca2+ and PADs contain 4 (PAD1), 5 (PAD3, 4) or 6 (PAD2) Ca2+-binding sites.Dysregulated PAD activity, most notably PAD2 and PAD4, is associated with mult

5、iple inflammatory diseases (e.g., rheumatoidarthritis) as well as cancer, and PAD inhibitors, such as Cl-amidine and BB-Cl-amidine, show efficacy in multiple preclinical animalmodels of disease.www.MedChemE 1 HYPERLINK https:/www.MedChemE/Targets/Protein Arginine Deiminase.html Protein HYPERLINK htt

6、ps:/www.MedChemE/Targets/Protein Arginine Deiminase.html HYPERLINK https:/www.MedChemE/Targets/Protein Arginine Deiminase.html Arginine HYPERLINK https:/www.MedChemE/Targets/Protein Arginine Deiminase.html HYPERLINK https:/www.MedChemE/Targets/Protein Arginine Deiminase.html Deiminase HYPERLINK http

7、s:/www.MedChemE/Targets/Protein Arginine Deiminase.html HYPERLINK https:/www.MedChemE/Targets/Protein Arginine Deiminase.html Inhibitors HYPERLINK https:/www.MedChemE/Targets/Protein Arginine Deiminase.html HYPERLINK https:/www.MedChemE/Targets/Protein Arginine Deiminase.html & HYPERLINK https:/www.

8、MedChemE/Targets/Protein Arginine Deiminase.html HYPERLINK https:/www.MedChemE/Targets/Protein Arginine Deiminase.html Activators HYPERLINK https:/www.MedChemE/Acefylline.html Acefylline(Theophyllineacetic acid; Theophylline-7-acetic acid) Cat. No.: HY-B1505 HYPERLINK https:/www.MedChemE/BB-Cl-Amidi

9、ne.html BB-Cl-AmidineCat. No.: HY-111347Acefylline (Theophyllineacetic acid), a xanthinederivative, is an adenosine receptor antagonist.Acefylline is a peptidylarginine deiminase (PAD)activator. Acefylline is also a bronchodilator,which inhibits rat lung cAMP phosphodiesteraseisoenzymes.BB-Cl-Amidin

10、e is a peptidylarginine deminase(PAD) inhibitor.Purity: 99.89%Clinical Data: LaunchedSize: 10 mM 1 mL, 100 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/bb-cl-amidine-hydrochloride.html BB-Cl-Amidine HYPERLINK https:/www.MedChemE/bb-cl-amidine-hydr

11、ochloride.html HYPERLINK https:/www.MedChemE/bb-cl-amidine-hydrochloride.html hydrochloride HYPERLINK https:/www.MedChemE/bb-cl-amidine-hydrochloride.html HYPERLINK https:/www.MedChemE/bms-p5.html BMS-P5Cat. No.: HY-111347A Cat. No.: HY-137655BB-Cl-Amidine hydrochloride is a peptidylargininedeminase

12、 (PAD) inhibitor.BMS-P5 is a specific and orally activepeptidylarginine deiminase 4 (PAD4) inhibitor.BMS-P5 blocks MM-induced NET formation and delaysprogression of MM in a syngeneic mouse model.Purity: 99.78%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mgPurity: 98%Clinic

13、al Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/bms-p5-free-base.html BMS-P5 HYPERLINK https:/www.MedChemE/bms-p5-free-base.html HYPERLINK https:/www.MedChemE/bms-p5-free-base.html free HYPERLINK https:/www.MedChemE/bms-p5-free-base.html HYPERLINK https:/www.MedChemE/b

14、ms-p5-free-base.html base HYPERLINK https:/www.MedChemE/bms-p5-free-base.html HYPERLINK https:/www.MedChemE/Cl-amidine.html Cl-amidineCat. No.: HY-137655A Cat. No.: HY-100574BMS-P5 free base is a specific and orally activepeptidylarginine deiminase 4 (PAD4) inhibitor.BMS-P5 free base blocks MM-induc

15、ed NET formationand delays progression of MM in a syngeneic mousemodel.Cl-amidine is an orally active peptidylargininedeminase (PAD) inhibitor, with IC values of 0.850M, 6.2 M and 5.9 M for PAD1, PAD3, and PAD4,respectively. Cl-amidine induces apoptosis incancer cells.Purity: 99.96%Clinical Data: No

16、 Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/Cl-amidine_hydrochloride.html Cl-amidine HYPERLINK https:/www.MedChemE/Cl-amidine_hydrochloride.html HYPERLINK https:/www.MedChemE/Cl-amidin

17、e_hydrochloride.html hydrochloride HYPERLINK https:/www.MedChemE/Cl-amidine_hydrochloride.html HYPERLINK https:/www.MedChemE/cl-amidine-tfa.html Cl-amidine HYPERLINK https:/www.MedChemE/cl-amidine-tfa.html HYPERLINK https:/www.MedChemE/cl-amidine-tfa.html TFACat. No.: HY-100574A Cat. No.: HY-100574B

18、Cl-amidine hydrochloride is an orally activepeptidylarginine deminase (PAD) inhibitor, withIC values of 0.8 M, 6.2 M and 5.9 M for PAD1,50PAD3, and PAD4, respectively. Cl-amidinehydrochloride induces apoptosis in cancer cells.Cl-amidine TFA is an orally active peptidylargininedeminase (PAD) inhibito

19、r, with IC values of 0.850M, 6.2 M and 5.9 M for PAD1, PAD3, and PAD4,respectively. Cl-amidine TFA induces apoptosis incancer cells.Purity: 99.10%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg

20、 HYPERLINK https:/www.MedChemE/d-cl-amidine.html D-Cl-amidine HYPERLINK https:/www.MedChemE/d-cl-amidine.html HYPERLINK https:/www.MedChemE/d-cl-amidine-hydrochloride.html D-Cl-amidine HYPERLINK https:/www.MedChemE/d-cl-amidine-hydrochloride.html HYPERLINK https:/www.MedChemE/d-cl-amidine-hydrochlor

21、ide.html hydrochlorideCat. No.: HY-100574C Cat. No.: HY-100574DD-Cl-amidine is a potent and highly selectivePAD1 inhibitor. D-Cl-amidine is well-torelatedwith no significant toxicity.D-Cl-amidine hydrochloride is a potent and highlyselective PAD1 inhibitor. D-Cl-amidine iswell-torelated with no sign

22、ificant toxicity.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 99.40%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mg, 50 mg, 100 mg2 Tel: 609-228-6898 Fax: 609-228-5909 Email: salesMedChemE HYPERLINK https:/www.MedChemE/gsk106.html GSK106 HYPERLINK https:/ww

23、w.MedChemE/gsk106.html HYPERLINK https:/www.MedChemE/gsk121.html GSK121Cat. No.: HY-120343 Cat. No.: HY-117777GSK106 is an inactive control for the selectivePAD4 inhibitors, GSK484 and GSK199.GSK-121 Trifluoroacetates a selective PAD4inhibitor.Purity: 98%Clinical Data: No Development ReportedSize: 1

24、 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/gsk199.html GSK199 HYPERLINK https:/www.MedChemE/gsk199.html HYPERLINK https:/www.MedChemE/GSK484.html GSK484 HYPERLINK https:/www.MedChemE/GSK484.html HYPERLINK https:/www.MedChemE/GSK484.html h

25、ydrochlorideCat. No.: HY-103058 Cat. No.: HY-100514GSK199 is a reversible and selective PAD4inhibitor with an IC of 200 nM in the absence of50calcium.GSK484 hydrochloride is a selective and reversiblepeptidylarginine deiminase 4 (PAD4) inhibitor.GSK484 hydrochloride demonstrates high affinitybinding

26、 to PAD4 with IC s of 50 nM in the absence50of Calcium. In the presence of 2 mM Calcium,notably lower potency (250 nM) is observed.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98.76%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/pad2-in-1.html PAD2-IN-1 HYPERLINK https:/www.MedChemE/pad2-in-1.html HYPERLINK https:/www.MedChemE/pad2-in-2.html PAD2-IN-2Cat. No.: HY-136557 Cat. No.: HY-125099PAD2-IN-1