KGDS is synthetic peptides, targeting integrin GPIIb-IIIa located on the membrane of human activated platelets. Amino acid sequence: Lys-Gly-Asp-Ser[1].
Dynapyrazole A is a specific inhibitor of microtubule dynamin that specifically inhibits the ATPase activity of microtubule-stimulated dynamin without blocking microtubule-independent basal activity[1].
Auristatin F is a cytotoxic tubulin modifier with potent and selective antitumor activity; MMAF analog and cytotoxin in Antibody-drug conjugates.
Cyclo(Arg-Gly-Asp-D-Phe-Val) (TFA) is an inhibitor of integrin αvβ3, with antitumor activity.
BTB-1 is a potent, selective and reversible mitotic motor protein Kif18A inhibitor with an IC50 of 1.69 μM.
Microtubule inhibitor 4 (compound 2) is a potent microtubule inhibitor. Microtubule inhibitor 4 shows cytotoxicity with IC50s of 4.0, 3.2, 2.1 nM for NCI-H460, BxPC-3, HT-29 cells, respectively. Microtubule inhibitor 4 shows the inhibition of tubulin polymerization[1].
Amphethinile is an anti-tubulin agent. The affinity constant for the association (Ka) of Amphethinile with tubulin is 1.3 μM.
HA-100 hydrochloride is a potent protein kinase inhibitor, with IC50s of 4 μM, 8 μM, 12 μM and 240 μM for cGMP-dependent protein kinase (PKG), cAMP-dependent protein kinase (PKA), protein kinase C (PKC) and MLC-kinase, respectively. HA-100 hydrochloride also used as a ROCK inhibitor[1][2].
Myosin Light Chain Kinase Substrate (smooth muscle) is a smooth muscle myosin light chain kinase (MLCK) synthetic peptide substrate[1].
LDV-FITC, a fluorescent peptide, is a FITC-conjugated LDV peptide (HY-P2267). LDV-FITC binds to the α4β1 integrin with high affinity (Kd: 0.3 nM and 12 nM for binding to U937 cells in the presence and absence of Mn2+ respectively). LDV-FITC can be used to detect α4β1 integrin affinity[1][2].
SB-743921 free base is a potent selective inhibitor of the mitotic kinesin KSP (Eg5), with a Ki of 0.1 nM. SB-743921 free base can induce mitotic arrest, block cell cycle progression, induce apoptosis, and can be used in the research of myeloma, leukemia and other diseases[1][2].
Tubulin polymerization-IN-30 (compound 6e) is a potent Tubulin polymerization inhibitor. Tubulin polymerization-IN-30 is a colchicine binding site inhibitor. Tubulin polymerization-IN-30 can disrupt intracellular microtubule organization, arrest cell cycle at the G2/M phase. Tubulin polymerization-IN-30 exhibits the high potency against the cancer cell lines including SGC-7901, A549 and HeLa, with IC50 values of 2.16, 2.21, and 0.403 μM[1].
5-Aminosalicylic acid acts as a specific PPARγ agonist and also inhibits p21-activated kinase 1 (PAK1) and NF-κB.
Wikstrol A is a potent antifungal, antimitotic and anti-HIV-1 Agent. Wikstrol A induces morphological deformation of P. oryzae mycelia with an MMDC value of 70.1 µM. Wikstrol A shows activity against microtubule polymerization with an IC50 value of 131 µM. Wikstrol A shows anti-HIV-1 activity with an IC50 value of 67.8 µM[1].
Bexotegrast is a potent inhibitor of ανβ6 integrin. Bexotegrast can be used for researching fibrosis such as idiopathic pulmonary fibrosis (IPF) and nonspecific interstitial pneumonia (NSIP) (extracted from patent WO2020210404A1, compound 5)[1].
Taltobulin trifluoroacetate (HTI-286; SPA-110) is an analogue of Hemiasterlin; potent tubulin inhibitor; ADCs cytotoxin.IC50 value:Target: tubulinin vitro: HTI-286 significantly inhibited proliferation of all three hepatic tumor cell lines (mean IC50 = 2 nmol/L +/- 1 nmol/L) in vitro. Interestingly, no decrease in viable primary human hepatocytes (PHH) was detected under HTI-286 exposure [1]. In all cell lines tested, HTI-286 was a potent inhibitor of proliferation and induced marked increases in apoptosis. Despite similar transcriptomic changes regarding cell death and cell cycle regulating genes after exposure to HTI-286 or docetaxel, array analysis revealed distinct molecular signatures for both compounds [2].in vivo: Intravenous administration of HTI-286 significantly inhibited tumor growth in vivo (rat allograft model) [1]. HTI-286 significantly inhibited growth of PC-3 and LNCaP xenografts and retained potency in PC-3dR tumors. Simultaneous castration plus HTI-286 therapy was superior to sequential treatment in the LNCaP model [2].
Gap 26 is a connexin mimetic peptide corresponding to the residues 63-75 of connexin 43, which is a gap junction blocker.
KIF18A-IN-4 is a moderately potent ATP and microtubule (MT) noncompetitive KIF18A inhibitor (IC50=6.16 μM). KIF18A-IN-4 has selectivity against a large panel of mitotic kinesins and kinases, and does not show any direct effects on tubulin assembly. KIF18A-IN-4 exhibits anti-tumor activity[1].
Tubulin polymerization-IN-52 (compound SC23) is a potent tubulin polymerization inhibitor, with an IC50 of 2.9 μM[1].
Taccalonolide AJ is a semi-synthesis compound with cellular microtubule stabilizing activity. Taccalonolide AJ exhibits high potency antiproliferative activity against cancer cells, with an IC50 of 4.2 nM for HeLa cells[1].
Sertaconazole (FI7056 free base) is a broad-spectrum topical antifungal agent, exhibits anti-inflammatory activity via activation of a p38-COX-2-PGE2 pathway. Sertaconazole is also a microtubule inhibitor, shows antiproliferative effect, induces apoptosis and autophagy, and can also inhibit the migration of cells[1][2][3][4].
Blebbistatin is a selective non-muscle myosin II (NMII) inhibitor, promotes directional migration of corneal endothelial cells (CECs) and accelerates wound healing, and better preserves cell junctional integrity and barrier function[1].
SS28, a SRT501 analog with oral bioavailability, inhibits tubulin polymerization to cause cell cycle arrest at G2/M phase. SS28 results in apoptosis rather than necrosis tubulin[1].
Eribulin (E7389; ER-086526), a synthetic analogue of halichondrin B in phase III clinical trials for breast cancer, binds to tubulin and microtubules.Target: Microtubule/TubulinEribulin suppressed centromere dynamics at concentrations that arrest mitosis. At 60 nmol/L eribulin (2 x mitotic IC(50)), the relaxation rate was suppressed 21%, the time spent paused increased 67%, and dynamicity decreased 35% (but without reduction in mean centromere separation), indicating that eribulin decreased normal microtubule-dependent spindle tension at the kinetochores, preventing the signal for mitotic checkpoint passage [1]. [(3)H]eribulin binds soluble tubulin at a single site; however, this binding is complex with an overall K(d) of 46 microM, but also showing a real or apparent very high affinity (K(d) = 0.4 microM) for a subset of 25% of the tubulin. Eribulin also binds microtubules with a maximum stoichiometry of 14.7 +/- 1.3 molecules per microtubule (K(d) = 3.5 microM), strongly suggesting the presence of a relatively high-affinity binding site at microtubule ends. At 100 nM, the concentration that inhibits microtubule plus end growth by 50%, we found that one molecule of eribulin is bound per two microtubules, indicating that the binding of a single eribulin molecule at a microtubule end can potently inhibit its growth. Eribulin does not suppress dynamic instability at microtubule minus ends [2]. Eribulin's in vivo superiority derives from its ability to induce irreversible mitotic blockade, which appears related to persistent drug retention and sustained Bcl-2 phosphorylation [3].
AT-1002, a 6-mer synthetic peptide[1], is a tight junction regulator and absorption enhancer[2].
Mps1-IN-3 is a potent and selective MPS1 kinase inhibitor, with an IC50 of 50 nM.
Tubulin polymerization-IN-21 (compound 9a) is a tubulin polymerization inhibitor. Tubulin polymerization-IN-21 exhibits anti-cancer activity through disrupting cellular integrity and affecting glucose metabolism[1].
KX2-391 Mesylate is an inhibitor of Src that targets the peptide substrate site of Src, with GI50 of 9-60 nM in cancer cell lines.
Efalizumab is a targeted T cell modulator, and is a humanized monoclonal antibody of CD11a, the α subunit of LFA-1. Efalizumab inhibits T cell activation, cutaneous T cell trafficking, and T cell adhesion to keratinocytes, can be used for plaque psoriasis research[1].