Microtubule/Tubulin Modulator

Epothilone B is a microtubule stabilizer (MSA) with a K_i of 0.71μM, and is a MSA with blood-brain barrier permeability. Epothilone B acts by binding to the αβ-tubulin heterodimer subunit which causes decreasing of αβ-tubulin dissociation.

Davunetide is an eight amino acid snippet derived from activity-dependent neuroprotective protein (ADNP), a neurotrophic factor that exists in the mammalian CNS. Davunetide possesses neuroprotective, neurotrophic and cognitive protective roperties. Davunetide, a microtubule-stabilizing peptide, interacts with and stabilises neuron-specific βIII-tubulin in vitro. Davunetide penetrates the blood-brain barrier and is non-toxic. Davunetide inhibits Aβ aggregation and Aβ-induced neurotoxicity.

KIF2C-IN-1 is a cell-penetrating, selective KIF2C inhibitor with fluorescent properties (E_x/E_m = 410/510 nm). KIF2C-IN-1 exhibits notable cytotoxicity and weak inhibitory effects on KIF2A/B. KIF2C-IN-1 prohibits the dissociation of KIF2C from microtubules. KIF2C-IN-1 inhibiting KIF2C reverses cross-resistance to microtubule-targeting agents. KIF2C-IN-1 reduces tumorigenesis in chemoresistant triple-negative breast cancer (TNBC) model in mice with the combination of Paclitaxel (HY-B0015).

TPI-287, a blood-brain barrier-permeable microtubule stabilizer, can significantly reduce metastatic colonization of breast cancer in the brain.

PROTAC HDAC6 degrader 2 is a non‑hydroxamate selective HDAC6 degrader with an IC₅₀ of 0.643 μM and shows high selectivity for HDAC6 over HDAC1-4. PROTAC HDAC6 degrader 2 recruits VHL E3 ubiquitin ligase to trigger HDAC6 ubiquitination and subsequent proteasomal degradation. PROTAC HDAC6 degrader 2 selectively elevates acetylated α-tubulin levels in cancer cells, and does not induce histone H3 hyperacetylation or obvious loss of cell viability. PROTAC HDAC6 degrader 2 is applicable for research on multiple myeloma.

PROTAC HDAC6 degrader 3 is a selective HDAC6 degrader with an IC₅₀ of 0.686 μM and shows high selectivity for HDAC6 over HDAC1-4. PROTAC HDAC6 degrader 3 recruits cereblon (CRBN) to trigger HDAC6 ubiquitination and subsequent proteasomal degradation. PROTAC HDAC6 degrader 3 selectively elevates acetylated α-tubulin levels in cancer cells, and does not induce histone H3 hyperacetylation or obvious loss of cell viability. PROTAC HDAC6 degrader 3 is applicable for research on multiple myeloma.

Flutax-2 (5/6-mixture) is an active fluorescent derivative of paclitaxel. Flutax-2 (5/6-mixture) binds to a polymerized α,β tubulin dimer. Excitation/emission wavelength: 496/524 nm. Paclitaxel, a diterpenoid secondary metabolite produced by Taxus species, can be used for the research of a variety of cancers.

PBOX 6 is a pyrrolo-1,5-benzoxazepine (PBOX) compound, acts as a microtubule-depolymerizing agent and an apoptotic agent.

Fosbretabulin (tromethamine), also known as combretastatin A4 phosphate (CA4P), is a vascular disrupting agent evaluated for its efficacy against anaplastic thyroid carcinoma (ATC). It targets tumor neovasculature, causing acute and reversible reductions in tumor blood flow and central necrosis.

Syk/HDAC6-IN-1 is a dual SYK/HDAC6 selective inhibitor with IC₅₀ values of 0.19 nM (SYK) and 0.66 nM (HDAC6). Syk/HDAC6-IN-1 downregulates p-SYK to block downstream AKT/FOXO1 signaling, elevates acetylated histone H3 and α-tubulin via HDAC suppression, represses SREBF1 -mediated lipid biosynthetic pathways, triggers G0/G1 cell cycle arrest and robust mitochondrial-dependent caspase-3-mediated apoptosis in leukemia cells. Syk/HDAC6-IN-1 can be used for the research of FLT3-mutant acute myeloid leukemia.

Epothilone B (Standard) is the analytical standard of Epothilone B. This product is intended for research and analytical applications. Epothilone B is a microtubule stabilizer with a Ki of 0.71μM. It acts by binding to the αβ-tubulin heterodimer subunit which causes decreasing of αβ-tubulin dissociation.

NMK-TD-100 is a modulator for microtubule. NMK-TD-100 binds to tubulin, inhibits the tubulin polymerization with an IC₅₀ of 17.5 µM, inhibits mitosis, and decreases mitochondrial membrane potential (MMP). NMK-TD-100 inhibits the proliferation of HeLa with an IC₅₀ of 1.42 µM, arrests cell cycle at G2/M phase, induces apoptosis in HeLa.

P34cdc2 Kinase Fragment is associated with the completion of DNA replication in yeast mitosis. P34cdc2 Kinase can phosphorylate mitogen-activated protein 2 (MAP2) to regulate microtubules polymerization in Xenopus oocytes meiosis.

Synstab A is a mitosis modulator to promote interactions between α- and β-tubulin. Synstab A can polymerizes microtubules from purified tubulin, and produces microtubule bundles in interphase cells.

HDAC6-IN-74 is an orally active, selective histone deacetylase 6 (HDAC6) inhibitor with an IC₅₀ of 0.036 μM. HDAC6-IN-74 induces tumor cell apoptosis, arrests cells at the S phase of the cell cycle, and impairs cell migration, invasion and colony-forming abilities. HDAC6-IN-74 exerts anticancer effects with no obvious toxicity. HDAC6-IN-74 can be used in the research of cancers such as liver cancer.

Multi-kinase-IN-14 is an orally active and blood-brain barrier-permeable multi-kinase inhibitor. Multi-kinase-IN-14 reduces the excessive phosphorylation of α-synuclein by inhibiting four kinases (ABL1, DYRK1A, GSK3β, and LRRK2) and stabilizing microtubules. Multi-kinase-IN-14 is applicable for research on neurodegenerative diseases such as Parkinson’s disease and Alzheimer’s disease.

Davunetide (Standard) is the analytical standard of Davunetide (HY-105066). This product is intended for research and analytical applications. Davunetide is an eight amino acid snippet derived from activity-dependent neuroprotective protein (ADNP), a neurotrophic factor that exists in the mammalian CNS. Davunetide possesses neuroprotective, neurotrophic and cognitive protective roperties. Davunetide, a microtubule-stabilizing peptide, interacts with and stabilises neuron-specific βIII-tubulin in vitro. Davunetide penetrates the blood-brain barrier and is non-toxic. Davunetide inhibits Aβ aggregation and Aβ-induced neurotoxicity.

Cytochalasin J is a cytochalasin detivative. Cytochalasin J affects mitotic spindel microtubule organization and kinetochore structure, and exhibits cytotoxicity in human leukemia K562 cell with IC₅₀ of 1.5 μM.