Arp2-3-Complex-Inhibitors-Modulators-MCE

1、 HYPERLINK https:/www.MedChemE/Targets/Arp2_3 Complex.html Arp2/3 HYPERLINK https:/www.MedChemE/Targets/Arp2_3 Complex.html HYPERLINK https:/www.MedChemE/Targets/Arp2_3 Complex.html ComplexActin-related protein 2/3 complexThe Arp2/3 complex is originally identified in Acanthamoeba and consists of se

2、ven proteins (actin-related proteins; Arp2 and Arp3,and Arp2/3 complex subunits; ARPC1-5) that are conserved in all eukaryotes, with the exception of some algae, microsporidia andprotists. The complex plays an essential role in a wide variety of cellular processes including lamellipodia-mediated cel

3、l migration,endocytosis and phagocytosis, by virtue of its ability to generate branched actin filament networks.Activation of Arp2/3 requires interaction with actin nucleation-promoting factors (NPFs). Regulation of Arp2/3 activity is achievedby endogenous inhibitory proteins through direct binding

4、to Arp2/3 and competition with NPFs or by binding to Arp2/3-inducedactin filaments and disassembly of branched actin networks. Arp2/3 inhibition has recently garnered more attention as it has beenassociated with attenuation of cancer progression, neurotoxic effects during drug abuse, and pathogen in

5、vasion of host cells.www.MedChemE 1 HYPERLINK https:/www.MedChemE/Targets/Arp2/3 Complex.html Arp2/3 HYPERLINK https:/www.MedChemE/Targets/Arp2/3 Complex.html HYPERLINK https:/www.MedChemE/Targets/Arp2/3 Complex.html Complex HYPERLINK https:/www.MedChemE/Targets/Arp2/3 Complex.html HYPERLINK https:/

6、www.MedChemE/Targets/Arp2/3 Complex.html Inhibitors, HYPERLINK https:/www.MedChemE/Targets/Arp2/3 Complex.html HYPERLINK https:/www.MedChemE/Targets/Arp2/3 Complex.html Activators HYPERLINK https:/www.MedChemE/Targets/Arp2/3 Complex.html HYPERLINK https:/www.MedChemE/Targets/Arp2/3 Complex.html & HY

7、PERLINK https:/www.MedChemE/Targets/Arp2/3 Complex.html HYPERLINK https:/www.MedChemE/Targets/Arp2/3 Complex.html Chemicals HYPERLINK https:/www.MedChemE/187-1-n-wasp-inhibitor.html 187-1, HYPERLINK https:/www.MedChemE/187-1-n-wasp-inhibitor.html HYPERLINK https:/www.MedChemE/187-1-n-wasp-inhibitor.

8、html N-WASP HYPERLINK https:/www.MedChemE/187-1-n-wasp-inhibitor.html HYPERLINK https:/www.MedChemE/187-1-n-wasp-inhibitor.html inhibitor HYPERLINK https:/www.MedChemE/187-1-n-wasp-inhibitor.html HYPERLINK https:/www.MedChemE/187-1-n-wasp-inhibitor-tfa.html 187-1, HYPERLINK https:/www.MedChemE/187-1

9、-n-wasp-inhibitor-tfa.html HYPERLINK https:/www.MedChemE/187-1-n-wasp-inhibitor-tfa.html N-WASP HYPERLINK https:/www.MedChemE/187-1-n-wasp-inhibitor-tfa.html HYPERLINK https:/www.MedChemE/187-1-n-wasp-inhibitor-tfa.html inhibitor HYPERLINK https:/www.MedChemE/187-1-n-wasp-inhibitor-tfa.html HYPERLIN

10、K https:/www.MedChemE/187-1-n-wasp-inhibitor-tfa.html TFACat. No.: HY-P1045 Cat. No.: HY-P1045A187-1, N-WASP inhibitor, a 14-aa cyclic peptide,is an allosteric neural Wiskott-Aldrich syndromeprotein (N-WASP) inhibitor. 187-1, N-WASPinhibitor potently inhibits actin assembly inducedby phosphatidylino

11、sitol 4,5-bisphosphate (PIP2)with an IC of 2 M.50Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg187-1, N-WASP inhibitor TFA, a 14-aa cyclicpeptide, is an allosteric neural Wiskott-Aldrichsyndrome protein (N-WASP) inhibitor.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg

12、, 5 mg HYPERLINK https:/www.MedChemE/benproperine-phosphate.html Benproperine HYPERLINK https:/www.MedChemE/benproperine-phosphate.html HYPERLINK https:/www.MedChemE/benproperine-phosphate.html phosphateCat. No.: HY-114657A HYPERLINK https:/www.MedChemE/CK-636.html CK-636(CK-0944636) Cat. No.: HY-15

13、892Benproperine phosphate is an orally active, potentactin-related protein 2/3 complex subunit 2(ARPC2) inhibitor. Benproperine phosphateattenuates the actin polymerization rate of actionpolymerization nucleation by impairing Arp2/3function.CK-636 is a cell permeable inhibitor of Arp2/3complex, that

14、 could inhibit actinpolymerization, with IC values of 4 M, 24 M50and 32 M for human, fission yeast and bovine,respectively.Purity: 99.23%Clinical Data: LaunchedSize: 10 mM 1 mL, 100 mgPurity: 98.43%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 10 mg, 50 mg, 100 mg HYPERLINK https:/www.MedC

15、hemE/ck-666.html CK-666 HYPERLINK https:/www.MedChemE/ck-666.html HYPERLINK https:/www.MedChemE/CK-869.html CK-869Cat. No.: HY-16926 Cat. No.: HY-16927CK-666 is a cell-permeable actin-related proteinArp2/3 complex inhibitor (IC =12 M). CK-66650binds to Arp2/3 complex, stabilizes the inactivestate of

16、 the complex, blocking movement of theArp2 and Arp3 subunits into the activatedfilament-like (short pitch) conformation.CK-869 is an Actin-Related Protein 2/3 (ARP2/3)complex inhibitor, with an IC of 7 M.50Purity: 99.79%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mgPurity

17、: 99.74%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/Cytochalasin_B.html Cytochalasin HYPERLINK https:/www.MedChemE/Cytochalasin_B.html HYPERLINK https:/www.MedChemE/Cytochalasin_B.html B HYPERLINK https:/www.MedChemE/Cytocha

18、lasin_B.html HYPERLINK https:/www.MedChemE/cytochalasin-d.html Cytochalasin HYPERLINK https:/www.MedChemE/cytochalasin-d.html HYPERLINK https:/www.MedChemE/cytochalasin-d.html D(Phomin) Cat. No.: HY-16928 (Zygosporin A; NSC 209835) Cat. No.: HY-N6682Cytochalasin B is a cell-permeable mycotoxinbindin

19、g to the barbed end of actin filaments,disrupting the formation of actin polymers, withK value of 1.4-2.2 nM for F-actin.dCytochalasin D (Zygosporin A; NSC 209835) is apotent and cell-permeable inhibitor of actinpolymerization derived from fungus, inhibits theG-actincofilin interaction by binding to

20、 G-actin.Purity: 99.84%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 1 mg, 5 mg, 10 mgPurity: 99.75%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 1 mg, 5 mg, 10 mg HYPERLINK https:/www.MedChemE/dihydrocytochalasin-b.html Dihydrocytochalasin HYPERLINK https:/www.MedChemE/dihydrocy

21、tochalasin-b.html HYPERLINK https:/www.MedChemE/dihydrocytochalasin-b.html B HYPERLINK https:/www.MedChemE/dihydrocytochalasin-b.html HYPERLINK https:/www.MedChemE/jasplakinolide.html JasplakinolideCat. No.: HY-N6701 Cat. No.: HY-P0027Dihydrocytochalasin B (H2CB) is a Cytokinesisinhibitor and change

22、s the morphology of the cells,similar to that of cytochalasin B; does notinhibit glucose transport.Jasplakinolide is a potent actin polymerizationinducer and stabilizes pre-existing actinfilaments. Jasplakinolide binds to F-actincompetitively with phalloidin with a K of 15dnM.Purity: 98%Clinical Dat

23、a: No Development ReportedSize: 1 mg, 5 mgPurity: 98.0%Clinical Data: No Development ReportedSize: 100 g2 Tel: 609-228-6898 Fax: 609-228-5909 Email: salesMedChemE HYPERLINK https:/www.MedChemE/latrunculin-a.html Latrunculin HYPERLINK https:/www.MedChemE/latrunculin-a.html HYPERLINK https:/www.MedChe

24、mE/latrunculin-a.html A(LAT-A) Cat. No.: HY-16929 HYPERLINK https:/www.MedChemE/phalloidin-tritc.html Phalloidin-TRITCCat. No.: HY-P2270Latrunculin A (LAT-A) is a toxin isolated from thered sea sponge Latrunculia magnifica, binds toactin monomers, inhibits polymerization of actin,with K s of 0.1, 0.

25、4, 4.7 M and 0.19 M fordATP-actin, ADP-Pi-actin, ADP-actin and G-actin,respectively.Phalloidin-TRITC is a TRITC labeled, redfluorescence probe for F-actin. Phalloidin, boundto actin filaments, reacts covalently with aminoacids Glu-llT, Met-ll9, and Met355, which are veryclose to the nucleotide binding site.Purity: