Microtubule/Tubulin Inhibitor

Monomethyl auristatin E (MMAE; SGD-1010) is a synthetic derivative of dolastatin 10 and functions as a potent mitotic inhibitor by inhibiting tubulin polymerization. MMAE is widely used as a cytotoxic component of antibody-drug conjugates (ADCs) to treat several different cancer types.

Nocodazole (Oncodazole) is a rapidly-reversible inhibitor of microtubule. Nocodazole binds to β-tubulin and disrupts microtubule assembly/disassembly dynamics, which prevents mitosis and induces apoptosis in tumor cells. Nocodazole inhibits Bcr-Abl.

Docetaxel (RP-56976) is a microtubule depolymerization inhibitor, with an IC₅₀ of 0.2 μM. Docetaxel attenuates the effects of bcl-2 and bcl-xL gene expression. Docetaxel arrests the cell cycle at G2/M and leads to cell apoptosis. Docetaxel has anti-cancer activity.

VcMMAE (mc-vc-PAB-MMAE) is a agent-linker conjugate for ADC with potent antitumor activity by using the anti-mitotic agent, monomethyl auristatin E (MMAE, a tubulin inhibitor), linked via the lysosomally cleavable dipeptide, valine-citrulline (vc).

3-Bromocarbazole is an inhibitor of the aryl hydrocarbon receptor (AHR). 3-Bromocarbazole induces the mRNA expression of CYP1A1 and CYP1B1, with EC₅₀ values of 2500 nM and 1100 nM, respectively. 3-Bromocarbazole inhibits motor neuron axon length by downregulating the mRNA transcription levels of α1-tubulin, Gap43, Syn2a and shha in zebrafish larvae. 3-Bromocarbazole reduces central nervous system neurogenesis by downregulating the mRNA transcription levels of elavl3, nrd, mbp and gfap in zebrafish larvae. 3-Bromocarbazole induces developmental neurotoxicity and decreases body length in zebrafish larvae or embryos; at high concentrations, it also reduces hatching rate, and increases mortality and malformation rate. 3-Bromocarbazole can be used in studies related to developmental neurotoxicity and breast cancer.

Monascorubramine is a metabolite derived from Monascus with antibacterial, cytotoxic and antimitotic activities. Monascorubramine interferes with mitotic spindle tubulin, triggers metaphase mitotic arrest, induces abnormal c‑mitosis division, and exerts antimitotic effects. Monascorubramine exhibits antibacterial activity and inhibits both Gram-positive and Gram-negative bacteria. Monascorubramine can be used in studies related to bacterial infections.

Iso cephalomannine is a tubulin-targeting cytotoxic agent. Iso cephalomannine induces cytotoxicity in breast cancer cells. Iso cephalomannine can be used in breast cancer-related research.

Colchicine, an orally active alkaloid, is a potent tubulin inhibitor and a microtubule disrupting agent. Colchicine inhibits microtubule polymerization with an IC₅₀ of 3 nM. Colchicine is also a competitive antagonist of the α3 glycine receptors (GlyRs). Colchicine prevents non-steroidal anti-inflammatory drug (NSAID)-induced small intestinal injury by inhibiting activation of the NLRP3 inflammasome. Colchicine has extensive anti-inflammatory, immunosuppressive and strong anti-fibrosis effects and has the potential for gouty arthritis research.

Vincristine (Leurocristine; NSC-67574; 22-Oxovincaleukoblastine) sulfate is a microtubule inhibitor that disrupts microtubule polymerization by binding to β-tubulin (with a K_i of 85 nM in bovine), arrests the cell cycle and induces apoptosis. Vincristine sulfate inhibits cell replication, tumor blood flow and the proliferation of various cancer cells, while triggering effects such as oxidative stress, inflammation, calcium overload, epithelial-mesenchymal transition and peripheral neuropathic pain. Vincristine sulfate upregulates the expression of various transporters and nuclear receptors, and enriches gastric cancer stem-like cells. Vincristine sulfate is used in research related to various tumors including acute lymphoblastic leukemia, lymphoma, melanoma, gastric cancer, solid tumors and sarcomas.

Nab-Paclitaxel (Nanoparticle albumin-bound Paclitaxel) is an albumin-bound nanoparticle formulation of Paclitaxel (HY-B0015). Nab-Paclitaxel is composed of albumin and the active pharmaceutical ingredient Paclitaxel, in which human albumin is used as an excipient to disperse and stabilize particles and carry the main drug. Nab-Paclitaxel is a solvent-free taxane with higher response rates and improved tolerability. Nab-Paclitaxel displays less toxicity and greater antitumor activity. Nab-Paclitaxel is more readily available for tumor cell uptake in three rhabdomyosarcoma, seven neuroblastoma cell lines, and one ostersarcoma cell line Nab-Paclitaxel can be studied in cancer research for example breast cancer and solid tumors. (The product specifications below only indicate the effective content of Paditaxel, the actual albumin quality depends on the batch; the ratio of each ingredient in this product is Paditaxel: albumin -1:7~1:11).

MMAF (Monomethylauristatin F) is a potent tubulin polymerization inhibitor and is used as a antitumor agent. MMAF (Monomethylauristatin F) is widely used as a cytotoxic component of antibody-drug conjugates (ADCs) such as vorsetuzumab mafodotin and SGN-CD19A.

Mertansine (DM1) is a microtubulin inhibitor and is an antibody-conjugatable maytansinoid that is developed to overcome systemic toxicity associated with maytansine and to enhance tumor-specific delivery. Mertansine can be attached to a monoclonal antibody with a linker to create an antibody-drug conjugate (ADC).

Vinblastine sulfate is a cytotoxic alkaloid used against various cancer types. Vinblastine sulfate inhibits the formation of microtubule and suppresses nAChR with an IC₅₀ of 8.9 μM.

Eribulin (E7389) is a microtubule targeting agent that is used for the research of metastatic breast cancer. Eribulin inhibits the proliferation of cancer cells by binding microtubule proteins and microtubules.

Vinorelbine (ditartrate) is an anti-mitotic agent which inhibits the proliferation of Hela cells with IC₅₀ of 1.25 nM.

MMAE-d₈ is a deuterated labeled MMAE, a potent mitotic inhibitor and a tubulin inhibitor.

Eribulin mesylate is an inhibitor for microtubule. Eribulin mesylate inhibits the proliferation of cancer cell LM8 and Dunn, inhibits the cell migration of LM8, arrests the cell cycle at G2/M phase, and induces apoptosis in LM8. Eribulin mesylate exhibits antitumor efficacy in mouse model.

Telisotuzumab vedotin (ABBV-399) (Teliso-V) is an anti-c-Met antibody-drug conjugate. Telisotuzumab vedotin consists of an anti-c-Met monoclonal antibody Telisotuzumab (ABT-700) (HY-P99391) and Monomethyl Auristatin E (HY-15162). Telisotuzumab vedotin exerts antitumor activity with acceptable toxicity in vivo. Telisotuzumab vedotin can be used for non-small cell lung cancer (NSCLC) research.

DM4 is is an antitubulin agent that inhibit cell division. DM4 can be used in the preparation of antibody agent conjugate.

Demecolcine is a potent mitotic inhibitor with an IC₅₀ value of 2.4 μM for inhibition of tubulin polymerization. Colcemid (Demecolcine) can interact with tubulin dimers to induce anti-mitotic action and inhibit microtubule growth. Colcemid (Demecolcine) can be used for inflammatory disorders and cancer research.