actin-related

Benproperine phosphate (Pirexyl phosphate) is a cough suppressant.

BRM BRG1 ATP Inhibitor-1 is an allosteric dual Brahma homolog (BRM) SWI SNF related matrix-associated actin-dependent regulator of chromatin subfamily A member 2 (SMARCA2) and BRG1 SMARCA4 ATPase activity inhibitor (IC50s<0.005 μM).

CK-636 (CK-0944636), an Arp2 3 complex inhibitor, can inhibit actin polymerization induced by the human (IC50: 4 μM), fission yeast (IC50: 24 μM) and bovine (IC50: 32 μM) Arp2 3 complex, respectively.

CK-869, an Actin-Related Protein 2 3 (ARP2 3) complex inhibitor with an IC50 of 7 μM, is a valuable tool for investigating the Arp2 3 complex.

CK-666 is a cell-permeable inhibitor of the actin-related protein Arp2 3 complex, binding to and stabilizing its inactive state, thereby preventing the movement of the Arp2 and Arp3 subunits into the activated filament-like (short pitch) configuration.

ALK5-IN-82 is a potent and selective inhibitor of activin receptor-like kinase 5 (ALK5), demonstrating an IC50 value of 9.1 nM. This compound effectively suppresses the expression of α-smooth muscle actin (α-SMA), collagen I, and the proteinases tissue inhibitor of metalloproteinase 1 (TIMP-1) and matrix metalloproteinase 13 (MMP-13) in human umbilical vein endothelial cells induced by transforming growth factor-β. ALK5-IN-82 shows potential for use in research related to cardiac fibrosis.

E0924G is an orally active PPARδ agonist with an EC50 of 2.82 μM. It enhances the upregulation of osteoprotegerin (OPG) expression, with an EC50 of 0.29 μM. E0924G reduces RANKL-induced osteoclast differentiation and inhibits F-actin ring formation in RAW264.7 macrophages. Additionally, E0924G modulates bone density and bone loss in models of ovariectomy (OVX) and age-related osteoporosis.

Wiskostatin is a selective inhibitor of N-WASP, a ubiquitously expressed member of the Wiskott-Aldrich Syndrome protein (WASp) family that regulates actin polymerization.

CK548 is a novel actin-related protein (Arp)2/3 complex inhibitor.

IMM-01 is a novel class of small-molecule agonists of the mammalian Diaphanous (mDia)-related formins, which act downstream of Rho GTPases to assemble actin filaments, and their organization with microfilaments to establish and maintain cell polarity during migration and asymmetric division. GTP-bound Rho activates mDia family members by disrupting the interaction between the DID and DAD autoregulatory domains, which releases the FH2 domain to modulate actin and microtubule dynamics[1].

1. Cucurbitacin IIA (Dihydrocucurbitacin Q1) can induce apoptosis and enhance autophagy , contributes to the anti-inflammatory activity of Cucurbitacin IIA against inflammation-related diseases. 2. Cucurbitacin IIA is a novel class of anti-cancer drug in suppression of cancer cell expansion by disrupting the actin cytoskeleton and directing the cell to undergo PARP-mediated apoptosis through the inhibition of survivin downstream of JAK2 STAT3.

CCG-222740 is an inhibitor of Rho MRTF pathway