| DC47923 |
PF-06380101-d8 |
PF-06380101 D8 (Aur0101 D8) is a deuterium labeled PF-06380101. PF-06380101, an Auristatin microtubule inhibitor, is a cytotoxic Dolastatin 10 analogue. |
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| DC48080 |
MiTMAB |
MiTMAB is a selective dynamin inhibitor that targets the dynamin-phospholipid interaction. MiTMAB inhibits dynamin GTPase activity with a Ki of 940 nM. |
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| DC48131 |
αvβ5 integrin-IN-1 |
αvβ5 integrin-IN-1 is a first potent and selective αvβ5 integrin inhibitor (pIC50 = 8.2) . |
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| DC48132 |
Bexotegrast
Featured
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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). |
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| DC48133 |
Sudocetaxel |
Sudocetaxel is a microtubule depolymerization inhibitor for pH-sensitive docetaxel delivery. |
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| DC48134 |
DHA-paclitaxel |
DHA-paclitaxel is an inert prodrug composed of the natural fatty acid DHA covalently linked to the C2'-position of paclitaxel. The paclitaxel moiety binds to tubulin and inhibits the disassembly of microtubules, thereby resulting in the inhibition of cell division. Compared to Paclitaxel, DHA-Paclitaxel targets tumor cells more specifically because tumor cells absorb large amounts of natural fatty acids for use as biochemical precursors and energy sources. |
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| DC48135 |
Tesetaxel |
Tesetaxel is a orally active, semisynthetic microtubule inhibitor of the taxane class for the treatment of cancer, including colorectal and gastric cancer. |
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| DC48136 |
cis-Trismethoxy resveratrol |
Cis-trismethoxy resveratrol is a potent anti-mitotic reagent.Cis-trismethoxy resveratrol inhibits tubulin polymerization with an IC50 value of 4 μM. |
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| DC48439 |
Verubulin hydrochloride
Featured
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Verubulin hydrochloride(MPC 6827 hydrochloride) is a microtubule destabilizer and vascular disrupting agent that achieve high brain concentration relative to plasma in animals. |
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| DC48690 |
Wiskostatin |
Wiskostatin is a potent and selective inhibitor of neuronal Wiskott-Aldrich syndrome protein (N-WASP)-mediated actin polymerization. Wiskostatin causes a rapid, profound, and irreversible decrease in cellular ATP levels. |
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| DC48738 |
LG308 |
LG308 is a novel synthetic compound with antimicrotubule activity. LG308 induces mitotic phase arrest and inhibits G2/M progression significantly which is associated with the upregulation of cyclin B1 and mitotic marker MPM-2 and the dephosphorylation of cdc2. LG308 also induces apoptosis and cell death. LG308 significantly suppresses tumor growth. LG308 with antimitotic activity has the potential for the research of prostate cancer. |
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| DC48963 |
Dynole 2−24 |
Dynole 2−24 is an indole-based dynamin GTPase inhibitor (IC50=0.56 μM for dynamin I). Dynole 2−24 is nontoxic and shows increased potency against dynamin I and II in vitro and in cells (IC₅₀(CME)=1.9 μM). Dynole 2−24 also shows 4.4-fold selectivity for dynamin I. Dynole 2−24 is active in-cell inhibitor of clathrin-mediated endocytosis. CME: Clathrin mediated endocytosis |
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| DC49182 |
TC113 |
TC113 is a c(RGDyK)-Based conjugate of Gemcitabine (GEM). TC113 could be internalized by A549 cells through integrin αvβ3. TC113 shows potent antiproliferative properties against WM266.4 and A549 cells. |
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| DC49570 |
Alicaforsen |
Alicaforsen is a 20-base antisense oligonucleotide inhibiting ICAM-1 production, which is an important adhesion molecule involved in leukocyte migration and trafficking to the site of inflammation. |
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| DC49572 |
(R)-AM-5308 |
(R)-AM-5308 is a potent kinesin KIF18A inhibitor (WO2021211549A1, C13). |
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| DC49573 |
(S)-AM-5308 |
(S)-AM-5308 (compound 7-13) is a potent kinesin KIF18A inhibitor with an IC50 of 46 nM for KIF18A ATPase. (S)-AM-5308 has the potential for cancer research. |
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| DC49574 |
SB-216
Featured
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SB-216 is a potent tubulin polymerization inhibitor. SB-216 shows strong antiproliferative potency in a panel of human cancer cell lines, including melanoma, lung cancer, and breast cancer. SB-216 can be used for cancer research. |
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| DC49575 |
OXi8007 |
OXi8007 is a water-soluble phosphate prodrug of OXi8006, a tubulin-binding compound. |
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| DC49576 |
2-Methoxyestradiol-13C6 |
2-Methoxyestradiol-13C6 (2-ME2-13C6) is the 13C-labeled 2-Methoxyestradiol. 2-Methoxyestradiol (2-ME2), an orally active endogenous metabolite of 17β-estradiol (E2), is an apoptosis inducer and an angiogenesis inhibitor with potent antineoplastic activity. 2-Methoxyestradiol also destablize microtubules. 2-Methoxyestradio, also a potent superoxide dismutase (SOD) inhibitor and a ROS-generating agent, induces autophagy in the transformed cell line HEK293 and the cancer cell lines U87 and HeLa. |
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| DC49577 |
Microtubule destabilizing agent-1 |
Microtubule destabilizing agent-1 (Compound 12b) acts as a microtubule destabilizing agent (MDA) based on hydroxamic acid, could serve as a potential MDA for further investigation. Microtubule destabilizing agent-1 shows favorable metabolism stability, high bioavailability, and potent antitumor activity. |
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| DC49578 |
AMXI-5001 hydrochloride |
AMXI-5001 hydrochloride is a potent, orally active, and dual parp1/2 and microtubule polymerization inhibitor. MXI-5001 hydrochloride exhibits selective antitumor cytotoxicity across a wide variety of human cancer cells with much lower IC50s than existing clinical PARP1/2 inhibitors. AMXI-5001 hydrochloride induces complete regression of established tumors, including exceedingly large tumors. |
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| DC49579 |
Microtubule inhibitor 2 |
Microtubule inhibitor 2 is a potent and selective, orally active microtubule inhibitor. Microtubule inhibitor 2 triggers cell death through ferroptosis . Microtubule inhibitor 2 shows antitumor activity. |
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| DC70154 |
BRD70326 |
A small molecule that inhibits tubulin polymerization. |
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| DC70235 |
Azo-EMD |
Azo-EMD is a cell permeable, photoswitchable compound that inhibits mitotic kinesin Eg5 more potently in its light-induced cis form, used for optical control mitosis.Under UV light conditions, HeLa cells undergo mitotic arrest, as evidenced by the formation of a monopolar spindle. |
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| DC70281 |
C67399 |
C67399 is a small molecule that blocks the integrin β1 binding site of TLN1, reduces the malignant behaviours of TNBC in vitro (MDA-MB-231 cell, IC50=2.0 uM).C67399 treatment significantly reduced the viability of BT549 cells.C67399 (2 uM) significantly reduced the expression of integrin β1, AKT, FAK, and phosphorylated FAK in MDA-MB-231 cells, while did not affect the expression of integrin β3.C67399 inhibited the binding of TLN1 to integrin β1 in MDA-MB-231 cells.C67399 (1.75 mg/kg) inhibited tumour growth and metastasis of MDA-MB-231 cells in mice, without causing obvious structural toxic changes. |
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| DC70445 |
GSK-1 |
GSK-1 is an ATP-competitive inhibitor of the mitotic kinesin KSP with HCT116 cell IC50 of 36 nM; induces monopolar spindle formation in SKOV3 cells, and shows markedly greater potency (IC50 of 0.5 nM) in the ispinesib-resistant HCT116-D130V cell line. |
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| DC70507 |
IMB5476 |
IMB5476 (IMB 5476) is a nitrobenzoate microtubule inhibitor, exerts broad-spectrum cytotoxicity against various human tumor cell lines (NCI-H460, IC50=144 nM).IMB5476 inhibits purified tubulin polymerization in vitro, binds to tubulin at the colchicine pocket.IMB5476 induced cell death by mitotic catastrophe and apoptosis, disrupted microtubule networks in cells and arrested cell cycle at G2/M phase.IMB5476 is a poor substrate of P-glycoprotein and exhibited potent cytotoxicity against drug-resistant tumor cells.IMB5476 inhibited angiogenesis in vitro, also inhibited the growth of drug-resistant KBV200 xenografts in mice. |
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| DC70540 |
KIF18A inhibitor 24 |
KIF18A inhibitor 24 is a highly potent, in vivo active inhibitor of mitotic kinesin KIF18A with IC50 of 61 nM.KIF18A inhibitor 24 binds at the interface of KIF18A and tubulin.KIF18A inhibitor 24 exhibits significant mitotic arrest in MDA-MB-157 mitotic cells with EC50 of 11 nM, followed by cell death either in mitosis or in the subsequent interphase, which is sustained for 24 h. |
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| DC70597 |
Microtubule inhibitor PP-13 |
Microtubule inhibitor PP-13 is a novel microtubule-destabilizing agent, directly inhibits microtubule assembly by targeting the colchicine-binding site in β-tubulin.PP-13 inhibits the growth of a wide range of cancer cell types, including targeted therapy-resistant and multidrug-resistant (MDR) cell lines (IC50=76-255 nM).PP-13 overcomes the multidrug-resistant (MDR) phenotype in cancer cells, induces mitotic blockade in cancer cells, interferes with both mitotic microtubule organization and spindle pole integrity.PP-13 induces cell prometaphase arrest then asymmetric division or direct apoptotic death.PP-13 reduces tumour growth and metastasis invasion in vivo. |
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| DC70680 |
PCH-1 |
PCH-1 is a potent antitumor agent that disrupts microtubule assembly, leading to cancer cell death, interacts vinblastine binding site on tubulin;
PCH-1 exhibits the strongest cytotoxic activity through interaction with tubulin, leading to cell cycle arrest and induction of apoptosis.
PCH-1 efficiently inhibits the growth of NSCLC cancer cell lines at micromolar concentrations (A-549 IC50=4.32 uM, H226 IC50=4.69 uM), and non-toxic to normal cells. |
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