Tirofiban-d9 (L700462-d9) hydrochloride is the deuterium labeled Tirofiban. Tirofiban(L700462) is a potent non-peptide, glycoprotein IIb/IIIa (integrins alphaIIbbetaIII) antagonist[1][2].
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].
Zagotenemab (LY3303560) is a humanised anti-tau antibody that selectively binds and neutralises tau deposits in the brain. Zagotenemab can be used in Alzheimer's disease research[1].
MMAF sodium (Monomethylauristatin F sodium) is an antitubulin agent that inhibit cell division; attenuates its cytotoxic activity compared to MMAE. MMAF sodium is widely used as a cytotoxic component of antibody-drug conjugates (ADCs) to treat several different cancer types.
Eleutherobin is a potent β-microtubule inhibitor with an IC50 value of 2 μM. Eleutherobin can be isolated from a marine soft coral. Eleutherobin has cytotoxic activity against cancer cells with similar potency to that of Paclitaxel (HY-B0015). Anticancer activity[1][2].
Tubulin inhibitor 11 is a potent and orally active tubulin inhibitor. Tubulin inhibitor 11 targets the Colchicine binding site on tubulin, inhibits tubulin polymerization, promotes mitotic blockade and apoptosis[1].
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.
PI3K/AKT-IN-2 (Compound 12c) is a PI3K and AKT inhibitor. PI3K/AKT-IN-2 blocks the epithelial-mesenchymal transition (EMT) and induces apoptosis. PI3K/AKT-IN-2 inhibits the polymerization of tubulin[1].
16-38-Thymosin β4 (cattle) is a Ca2+-independent MLCK activator with high affinity.
Tubulin polymerization-IN-27 (compound 5j) is a tubulin polymerization inhibitor. Tubulin polymerization-IN-27 can arrest cell cycle at G2/M phase and induce apoptosis[1].
Tubulysin H is a highly cytotoxic peptide isolated from the myxobacterial species Archangium geophyra and Angiococcus disciformis[1]. Tubulysin displays extremely potent cytotoxic activity in mammalian cells, including multidrug-resistant cell lines, with IC50 values in the lower nanomolar range[2]. Tubulysin H is a cytotoxic activity tubulysin which inhibits tubulin polymerization and leads to cell cycle arrest and apoptosis[3].
Tubulin polymerization-IN-29 (compound 6g) is a potent tubulin polymerization inhibitor. Tubulin polymerization-IN-29 exhibits potent antiproliferative activity. Tubulin polymerization-IN-29 can induce HeLa cells arrest in G2/M phase[1].
CW-069 is an allosteric inhibitor of HSET with an IC50 of 75 μM.
Glembatumumab vedotin (CDX-011) is an ADC (antibody-drug conjugates (ADCs)) comprising a fully human IgG2 monoclonal antibody (CR011) directed against glycoprotein NMB (GPNMB) and conjugated to the potent tubulinbinding cytotoxic agent MMAE via a protease-sensitive vc linker. Glembatumumab vedotin has potent anticancer effects[1].
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].
Cephalomannine is a taxol derivative with antitumor, antiproliferative properties. IC50 value:Target: Cephalomannine is an active anti-cancer agent obtained from Taxus yunnanensis and has an antineoplastic effect on tumors found in mice. Cephalomannine is a chemotherapy drug that is given as a treatment for some types of cancer. Cephalomannine is most commonly used to treat non-small cell lung cancer.
Tubulin polymerization-IN-47 (Compound 4h) is a tubulin polymerization inhibitor and mitotic inhibitor. Tubulin polymerization-IN-47 inhibits neuroblastoma cancer cell proliferation, with IC50s of 7 and 12 nM for Chp-134 and Kelly cell line[1].
AZA197 is a selective small molecule inhibitor of Cdc42.AZA197 suppresses colon cancer cell proliferation, cell migration, invasion and increases apoptosis by down-regulating the PAK1 and ERK signaling pathways in vitro. AZA197 reduces tumor growth and significantly increases mouse survival in SW620 tumor xenografts[1].
Valecobulin (CKD516), a valine prodrug of (S516) and a vascular disrupting agent (VDA), is a potent beta-tubulin polymerization inhibitor with marked antitumor activity against murine and human solid tumors[1][2].
Polatuzumab vedotin is an antibody-drug conjugate targeting CD79b. It contains a humanized anti-CD79b IgG1 monoclonal antibody linked to monomethyl auristatin E (MMAE), a potent microtubule inhibitor. Polatuzumab vedotin has the potential for the research of Large B-cell lymphomas (LBCL)[1].
RO0270608, the active metabolite of R411, is a dual alpha4beta1-alpha4beta7 (α4β1/α4β7) integrin antagonist. Antiinflammatory activity[1][2].
Tubulin polymerization-IN-18 (compound 8) is a potent inhibitor of tubulin polymerization. Tubulin polymerization-IN-18 has the potential for the research of breast cancers and chemoresistant colon cancers[1].
3-Hydroxyxanthone (3-Hydroxy-xanthen-9-one) is a xanthone compound, with . 3-Hydroxyxanthone inhibits NADPH-catalysed lipid peroxidation in human umbilical vein endothelial cells (HUVECs). 3-Hydroxyxanthone also inhibits TNF-alpha induced ICAM-1 expression[1].
XVA143, an α/β I-like allosteric antagonist, inhibits LFA-1 dependent firm adhesion, while at the same time it enhances adhesion in shear flow and rolling both in vitro and in vivo[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].
Cyclo(RGDyK) trifluoroacetate is a potent and selective αVβ3 integrin inhibitor with an IC50 of 20 nM.
PF-06380101 is a novel cytotoxic Dolastatin 10 analogue; with excellent potencies in tumor cell proliferation assays and differential ADME properties when compared to other synthetic auristatin analogues that are used in the preparation of ADCs.IC50 value: ~0.2 nM(GI50 in BT474, MDA-MB-361-DYT2 and N87 cell line) [1]Target: ADCs cytotoxin; tubulin inhibitorAfter an IV dose of 20a at 20 μg/kg to Wistar Han rats, PF-06380101 exhibited a mean systemic clearance (Cl) of 70 mL/min/kg and a volume of distribution (Vss) of 14.70 L/kg, resulting in a terminal elimination half-life (t1/2) of approximately 6 h. PF-06380101 preferentially distributes into human plasma relative to whole blood and that PF-06380101 is a P-glycoprotein (P-gp) substrate. PF-06380101 is anticipated to be of low risk to perpetrate pharmacokinetic drug interactions with compounds for which CYP1A2, CYP2B6, CYP2C8, CYP2C9, CYP2C19, CYP2D6, and/or CYP3A4/5-mediated metabolism constitutes the primary mechanism of clearance. The utility of the new auristatin analogues as ADC payloads including the development of the lead analogue 20a (PF-06380101) will be reported in due course.
Tubulin inhibitor 27 (DYT-1) is a tubulin polymerisation inhibitor with an IC50 of 25.6 µM. Tubulin inhibitor 27 shows anti-angiogenesis and antitumor activities[1].
Cilengitide is a potent and selective integrin inhibitor for αvβ3 and αvβ5 receptor, with IC50s of 4 and 79 nM, respectively.