CK-636 CK-636;N-[2-(2-Methyl-1H-indol-3-yl)ethyl]-2-thiophenecarboxamide;CK-0944636;CK-636 N-[2-(2-Methyl-1H-indol-3-yl)ethyl]-2-thiophenecarboxamide;N-[2-(2-Methyl-1H-indol-3-yl)ethyl]-2-thiophenecarboxamid 442632-72-6
CK-636(CK-0944636) is a small molecule inhibitor of Arp2/3 complex; Inhibitor of actin polymerization; Cell permeable inhibitor of human (IC50=4μM), fission yeast (IC50=24μM) and bovine (IC50=32μM) Arp2/3 complex between Arp2 and Arp3. Inhibits actin polymerization (IC50=22μM).
IC50 value: 4/24/32 uM (Human/fission yeast/bovine Arp2/3) [1]
Target: Arp2/3 complex; actin polymerization
CK-636 binds between Arp2 and Arp3, where it appears to block movement of Arp2 and Arp3 into their active conformation. CK-636 inserts into the hydrophobic core of Arp3 and alters its conformation. Both classes of compounds inhibit formation of actin filament comet tails by Listeria and podosomes by monocytes.
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