filaments

NP-G2-044 is an orally active fascin inhibitor, with an IC50 of ~2 μM. It blocks tumor metastasis and increases antitumor immune response.

Jasplakinolide(Jaspamide), a naturally occurring cyclic peptide from marine sponges, is a potent inducer of actin polymerization.Jasplakinolide exhibits antifungal and antitumor activity and stabilizes pre-existing actin filaments. Jasplakinolide competitively binds to F-actin with the ghost pen cyclic peptide and has a Kd value of 15 nM for F-actin.

Cytochalasin E is a potent actin depolymerization agent and an epoxide containing Aspergillus-derived fungal metabolite. Cytochalasin E also inhibits angiogenesis and tumor growth. It binds and caps the barbed end of actin filaments to prevent actin elong

Troponin modulator 1 (compound 7) enhances the function of mutated myocardial thin filaments. By phosphorylation, it increases Ca2+ sensitivity, with an EC50 of 67 μM.

TR-100 is a small-molecule inhibitor that targets tumor-associated tropomyosin; it specifically binds to the C-terminus of tropomyosin 3.1, thereby disrupting its interaction with actin filaments and compromising cytoskeletal stability. TR-100 selectively affects Tpm3.1-dependent actin filament function in cancer cells while having minimal impact on normal tissues (such as cardiac muscle). It is primarily used to study mechanisms related to tumor cell proliferation, migration, and survival. Additionally, TR-100 inhibits Dynamin-1 with an IC50 value of 10.8 µM.

DHI1 is an anti-leukemia agent with high selectivity towards Jurkat (IC50= 21.83 μM) and HL-60 (IC50= 19.14 μM) leukemia cells, while exhibiting low toxicity to non-cancerous cells. It induces G2/M cell cycle arrest in both Jurkat and HL-60 leukemia cells and S phase arrest in HL-60 cells, significantly affecting cell cycle signaling molecules such as Wee1, cyclin B1, cdc2 on Tyr15, and Chk1. DHI1 inhibits the migration and invasiveness of Jurkat and HL-60 cells by disrupting the cytoskeletal actin filaments, making it useful for research on hematological malignancies.

Cytochalasin H ((16-Benzyl-5,12-dihydroxy-5,7,14-trimethyl-13-methylidene-18-oxo-17-azatricyclo[9.7.0.01,15]octadeca-3,9-dien-2-yl) acetate) is a potent inhibitor of actin incorporation into filaments.

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].

Swinholide A is a polyketone compound that can be extracted from sponges and binds to actin to dimerize actin with Kd of about 50 nM. Swinholide A is a cytotoxin that stabilizes actin dimers and severs actin filaments. Swinholide A has antifungal activity and can damage the actin cytoskeleton of cells.

Phalloidin-retramethylrhodamine conjugate is an orange fluorescent probe (ex/em = 546/575 nm) that selectively binds to F-actin. It can be used to localize actin filaments in living or fixed cells, as well as for visualizing individual actin filaments in vitro.

L-AP4 (L-APB) monohydrate is a potent and specific agonist for group III mGluRs, with EC50s of 0.13, 0.29, 1.0, and 249 μM for mGlu4, mGlu8, mGlu6, and mGlu7 receptors, respectively [1][2].

Cytochalasin B is a mycotoxin binding to the barbed end of actin filaments. It can disrupt the formation of actin polymers (Kd: 1.4-2.2 nM for F-actin).

Miuraenamide A (SMH 27-4A) is an antifungal and antitumor antibiotic that also acts as an actin filament stabilizer. It effectively stabilizes actin filaments and exhibits potent antifungal activity, particularly against the plant pathogenic oomycete Phytophthora capsici.

Human cardiac troponin (mixture) (cTn) is a regulatory protein critical for muscle contraction, located on the thin filaments of the contractile proteins. It plays a significant role in controlling muscle contraction and relaxation.