NMS-P715 is a selective, ATP-competitive inhibitor of MPS1, with an IC50 of 182 nM.
Vindesine sulfate is a potent tubulin inhibitor with an Ki of 0.110 µM. Vindesine sulfate shows anti-proliferation effect in vitro. Vindesine sulfate shows antitumor effect in vivo[1].
Tubulysin C is a highly cytotoxic peptide isolated from the myxobacterial species Archangium geophyra and Angiococcus disciformis. Tubulysin displays extremely potent cytotoxic activity in mammalian cells, including multidrug-resistant cell lines, with IC50 values in the lower nanomolar range[1]. Tubulysin C is a cytotoxic activity tubulysin which inhibits tubulin polymerization and leads to cell cycle arrest and apoptosis[2].
Dynole 34-2 is a dynamin GTPase inhibitor (IC50s=6.9 and 14.2 µM for dynamin1 and dynamin2 GTPase activity, respectively) with antimitotic effect. Dynole 34-2 induces apoptosis, as revealed by cell blebbing, DNA fragmentation, and PARP cleavage[1]. Dynole 34-2 also potently inhibits receptor mediated endocytosis (RME)[2].
Carotegrast is an orally available α4 integrin receptor inhibitor with anti-inflammatories activities.
Fmoc-MMAF-OMe is an anticancer agent and tubulin polymerization inhibitor with an Fmoc protecting group. The active ingredient of Fmoc-MMAF-OMe, MMAF (HY-15579), is the cytotoxic (ADC Cytotoxin) component of classic antibody drug conjugates (ADCs)[1].
Tubulysin B is a highly cytotoxic peptide and potent microtubule destabilizing agents isolated from the myxobacteria Archangium geophyra and Angiococcus disciformis. Tubulysin B has IC50 values in the picomolar range against many cancer cell lines, including those with multidrug resistant properties[1].Tubulysin B is a cytotoxic activity tubulysin which inhibits tubulin polymerization and leads to cell cycle arrest and apoptosis[2].
10-Deacetyltaxol (10-Deacetylpaclitaxel) is a taxane derivative isolated from Taxus wallichiana Zucc[1]. 10-Deacetyltaxol (10-Deacetylpaclitaxel) promotes the polymerization of tubulin and to inhibit the depolymerization of microtubules induced by cold or by calcium ions in vitro[2]. 10-Deacetyltaxol (10-Deacetylpaclitaxel) exhibits cytotoxicity in human glial and neuroblastoma cell-lines[3].
Plocabulin (PM060184) is a novel tubulin-binding agent binding to αβ-tubulin dimer with nanomolar affinity, inhibits a panel of 23 tumor cell lines with GI50 of 20 pM-5 nM; inhibits angiogenesis by modulation of microtubule dynamics in endothelial cells; also shows antifungal activity virtually abolishing growth of the filamentous fungus Aspergillus nidulans.
Clathrin-IN-2 is potent inhibitor of clathrin mediated endocytosis (CME) with an IC50 value of 2.3 μM. Clathrin-IN-2 also has inhibitiory for dyn I GTPase with an IC50 value of 7.7 μM[1].
Dynasore is a cell-permeable dynamin inhibitor with an IC50 of 15 μM.
Enlimomab (BI-RR 0001), a murine IgG2a monoclonal antibody to the human ICAM-1, inhibits leukocyte adhesion to the vascular endothelium, thereby decreasing leukocyte extravasation and inflammatory tissue injury. Enlimomab has anti-inflammatory effects, and can be used for stroke research[1] [2] .
Veltuzumab (IMMU-106) is a humanized anti-CD20 monoclonal antibody. Veltuzumab has low EC50 value of 0.08-0.09 μg/mL in the Daudi cell line. Veltuzumab can be used for the research of cancer including non-Hodgkin lymphoma (NHL)[1].
GR 144053 trihydrochloride is a selective and non-peptic GPIIb/IIIa inhibitor (IC50=37 nM)[1].
Mertansine (DM1) is a microtubulin inhibitor which binds at the tips of microtubules and suppresses the dynamicity of microtubules.. Mertansine is an antibody-conjugatable maytansinoid that was developed to overcome systemic toxicity associated with maytansine and to enhance tumor-specific delivery.
Latrunculin A (LAT-A) is a toxin isolated from the red sea sponge Latrunculia magnifica, binds to actin monomers, inhibits polymerization of actin, with Kds of 0.1, 0.4, 4.7 μM and 0.19 μM for ATP-actin, ADP-Pi-actin, ADP-actin and G-actin, respectively[1][2].
Integrin-IN-2 (compound 39) is an orally bioavailable pan αv integrin inhibitor. Integrin-IN-2 can increases the αvβ6, αvβ3, αvβ5 and αvβ8 binding affinities with pIC50 values of 7.8, 8.4, 8.4 and 7.4, respectively[1].
Sirt1/2-IN-1 (Compound 7) is a SIRT1 and SIRT2 inhibitor with IC50 values of 1.81, 2.10 and 20.5 µg/mL against SIRT1, SIRT2 and SIRT3, respectively. Sirt1/2-IN-1 displays activity in hyperacetylation of α-tubulin protein with an IC50 of 32.05 µg/mL. Sirt1/2-IN-1 shows prominent anticancer activity[1].
Ixabepilone is an orally bioavailable microtubule inhibitor, which binds to tubulin and promotes tubulin polymerization and microtubule stabilization, thereby arrests cells in the G2-M phase of the cell cycle and induces tumor cell apoptosis.
Cyclo(RGDyK) is a potent and selective αVβ3 integrin inhibitor with an IC50 of 20 nM.
Entasobulin is a β-tubulin polymerization inhibitor with potential anticancer activity.
Cantuzumab mertansine (SB-408075; huC242-DM1), an ADC, is an immunoconjugate of the potent maytansine derivative (DM1; HY-19792) and the humanized monoclonal antibody (huC242) directed to CanAg. Cantuzumab mertansine has cytotoxic toward colon cancer cells and has broad antitumor efficacy against a range of CanAg-positive human tumor xenografts[1][2].
KX2-391 is an inhibitor of Src that targets the peptide substrate site of Src, with GI50 of 9-60 nM in cancer cell lines.
PM050489 is an effective polyketone inhibitor of Microtubule/Tubulin that can be isolated from Madagascan sponge Lithoplocamia lithistoides. PM050489 inhibits mitosis with an IC50 value of 26.4 nM. PM050489 has antitumor activity and can be used in cancer research[1][2].
Mps1-IN-1 is a potent, selective and ATP-competitive Mps1 kinase inhibitor, with an IC50 and a Kd of 367 nM and 27 nM.
Antitumor agent-68 is a potent tubulin inhibitor. Antitumor agent-68 shows potent anticancer activity with IC50s of 3.6 and 3.8 µM for HeLa and MCF-7 cells, respectively. Antitumor agent-68 exhibits good scavenging activity of ROS and DPPH radical in a dose-dependent manner[1].
BI-1950 is a potent, selective LFA-1 antagonist that inhibits the binding of LFA-1 to ICAM-1 with Kd value of 9 nM; displays >1,000 fold selectivity against the most closely related b2-integrin Mac-1 and b1-integrin function; inhibits the production of IL-2 in human PBMC and whole blood with IC50 value of 3 nM and 120 nM, respectively; exhibits an attractive DMPK profile, BI-1950 is a excellent molecule for testing pharmacological hypotheses in vitro and in vivo.
Drp1-IN-1 (comp A-7) is a dynamin-1-like protein (Drp1) inhibitor, with an IC50 of 0.91 μM[1].
Rovelizumab is a humanized monoclonal leukointegrin antibody. Rovelizumab is a monoclonal antibody directed against the CD11/CD18 cell adhesion proteins. Rovelizumab can be used for research of multiple sclerosis (MS), hemorrhagic shock, myocardial infarction (MI) and stroke[1].
Tesetaxel is a orally active, semisynthetic microtubule inhibitor of the taxane class for the treatment of cancer, including colorectal and gastric cancer.