Microtubule/Tubulin Activator

Kinesore is an inhibitor of the KLC2-SKIP Interaction.

Larotaxel (XRP9881) is an orally active and blood-brain barrier penetrant Microtubule stabilizer with an IC₅₀ of 0.21 μM. Larotaxel shows activity in Taxane-resistant tumor models. Larotaxel exhibits antitumor activity in intracranial glioblastoma models. Larotaxel can be used for research on advanced solid tumors.

HDAC6-IN-77 is a highly selective HDAC6 inhibitor with an IC₅₀ of 7.0 nM.HDAC6-IN-77 induces neurite outgrowth.HDAC6-IN-77 exerts neuroprotective activity.HDAC6-IN-77 shows no significant toxicity on dopaminergic cells.HDAC6-IN-77 can be used for the research of Alzheimer's disease.

WMJ-J-09 is an HDAC inhibitor with IC₅₀ values of 7.5 nM (HDAC1), 21.3 nM (HDAC2), 18.4 nM (HDAC3), 90.9 nM (HDAC8), 3.9 nM (HDAC6) and 8715.7 nM (HDAC4). WMJ-J-09 blocks the cell cycle and induces apoptosis in cancer cells. WMJ-J-09 induces cancer cell death through the LKB1-AMPK-p38MAPK-p63-survivin signaling cascade.WMJ-J-09 inhibits HDAC enzyme activity, leading to acetylation of key proteins and thereby regulating cancer cell death. WMJ-J-09 can be used in HCT116 cells and FaDu cells research^[1][2].

9-cis-UAB30 is a rexinoid agonist. 9-cis-UAB30 significantly decreases the proliferation, viability, and motility of both patient-derived xenografts (PDXs). 9-cis-UAB30 induced cell-cycle arrest as demonstrated by the significant increase in the percentage of cells in G1 and a decrease in the percentage of cells in S phase by downregulating SKP2 and/or 20S proteasome activity, which leads to increased p27kip1 protein stability. 9-cis-UAB30 downregulates the abundance of stem cell marker mRNAs (Oct4, Nanog, Sox2, nestin) and upregulates the abundance of differentiation marker mRNAs (β3-tubulin, NSE, HOXC9, GAP43). 9-cis-UAB30 has no adverse effects on the central nervous system and cardiovascular system at the tested dose. 9-cis-UAB30 can be used for the study of neuroblastoma, cutaneous T-cell lymphomas, and breast cancer.

Larotaxel-d₉ (XRP9881-d₉) is the d₉-labeled Larotaxel (HY-125374). Larotaxel (XRP9881) is an orally active and blood-brain barrier penetrant Microtubule stabilizer with an IC₅₀ of 0.21 μM. Larotaxel shows activity in Taxane-resistant tumor models. Larotaxel exhibits antitumor activity in intracranial glioblastoma models. Larotaxel can be used for research on advanced solid tumors.

Viriditoxin ((-)-Viriditoxin) is a mycotoxin. Viriditoxin promotes tubulin polymerization, and inhibits FtsZ polymerization and GTPase activity. Viriditoxin exhibits cytotoxicity against cancer cells, induces apoptosis, inhibits cell migration and colony formation, induces G₂/M phase arrest, and triggers autophagic cell death. Viriditoxin activates caspase-3, cleaves PARP, promotes cytochrome c release, and induces ROS production. Viriditoxin possesses broad-spectrum antibacterial activity against Gram-positive pathogenic bacteria, fish pathogenic bacteria, and permeabilized Gram-negative bacteria. Viriditoxin can be used in research related to ovarian cancer, lung cancer, nasopharyngeal carcinoma, colon cancer, neuroblastoma, prostate cancer, leukemia, lymphoma, bacterial infections, and streptococcosis.

ARN25699 is a kinase inhibitor with an IC₅₀ of 5.5 nM against GSK-3β, 2.2 nM against FYN-α, and 242.3 nM against DYRK1A, and it exhibits oral bioavailability. ARN25699 reduces hyperphosphorylation of tau protein and promotes microtubule bundle formation. ARN25699 has a broader kinome inhibitory profile and targets kinases associated with the pathogenic mechanisms linked to Alzheimer's disease. ARN25699 can be used in the research of Alzheimer's disease and related tauopathies.

HDAC-IN-99 is a histone deacetylase (HDAC) inhibitor with an IC₅₀ of 37.73 nM, and it exhibits potent inhibitory activity against HDAC1 (IC₅₀ = 48.09 nM), HDAC2 (IC₅₀ = 300.28 nM) and HDAC6 (IC₅₀ = 9.16 nM). HDAC-IN-99 exerts broad-spectrum antiproliferative activity in various cancer cell lines. HDAC-IN-99 induces S-phase cell cycle arrest and apoptosis in colon cancer cells, increases the acetylation levels of histone H3, histone H4 and α-tubulin, and upregulates the expression of p21 as well as the cleavage of caspase-3. HDAC-IN-99 displays antitumor activity in colon cancer xenograft models. HDAC-IN-99 can be used for the research of colon cancer.

HDAC1 Degrader-1 is a HDAC1 degrader with an IC₅₀ of 192.3 nM. HDAC1 Degrader-1 induces degradation of HDAC1 in multiple myeloma cells via the proteasome system and enhances apoptosis of multiple myeloma cells. HDAC1 Degrader-1 can be used for research on multiple myeloma.

2'-Deoxy-PTX is a Paclitaxel (HY-B0015) derivative and microtubule assembly inducer. 2'-Deoxy-PTX binds to GMPcPP-stabilized microtubules, with a Ka_app of 0.50 × 10⁶ M^-1. 2′-Deoxy-PTX induces Tubulin to assemble into normal microtubules. 2'-Deoxy-PTX can be used for the research of prostate cancer.

HDAC6-IN-87 is a selective HDAC6 inhibitor (IC₅₀ = 4.29 nM). HDAC6-IN-87 weakly inhibits HDAC1 (IC₅₀ = 749.59 nM), HDAC3 (IC₅₀ = 813.09 nM), and HDAC10 (IC₅₀ = 679.25 nM). HDAC6-IN-87 exhibits broad-spectrum antitumor activity, elevates α-tubulin acetylation levels without affecting histone H3 acetylation, and induces cell cycle arrest and apoptosis. HDAC6-IN-87 can be used for cancer-related research.

COX-2/HDAC6-IN-1 (Compound 11e) is a dual COX-2 and HDAC6 inhibitor, with an IC₅₀ of 0.12 μM against HDAC6 and an IC₅₀ of 0.66 μM against COX-2. COX-2/HDAC6-IN-1 enhances the acetylation level of α-tubulin, regulates epigenetic gene expression, and inhibits the expression of pro-inflammatory mediators (COX-2, IL-1β, IL-6 and TNF-α). COX-2/HDAC6-IN-1 promotes Amyloid-β clearance and reduces excessive phosphorylation of Tau protein. COX-2/HDAC6-IN-1 maintains neuronal morphology by stabilizing MAP2, protects synaptic integrity by regulating synapsin, and restores the expression of memory-related genes. COX-2/HDAC6-IN-1 possesses neuroprotective activity and improves learning and memory abilities in Scopolamine (HY-N0296)-induced Alzheimer's disease mouse models. COX-2/HDAC6-IN-1 is applicable to research related to Alzheimer's disease.

GV-001 is a selective and orally active HDAC6 inhibitor with an IC₅₀ of 1.18 nM against HDAC6. GV-001 selectively enhances α-tubulin acetylation, reduces sIL-6 and Collagen I levels, suppresses renal cyst growth, and upregulates PC1 expression. GV-001 can be used for the study of autosomal dominant polycystic kidney disease (ADPKD).

PKM2-IN-11 is a PKM2 inhibitor (IC₅₀ = 0.363 μM). PKM2-IN-11 has dual mechanisms involving pyruvate kinase M2 (PKM2) inhibition and microtubule stabilization. PKM2-IN-11 can decrease PKM2 protein levels in MCF-7 cells. PKM2-IN-11 can slightly reduce reactive oxygen species (ROS) levels and significantly increase early apoptotic cells. PKM2-IN-11 induces G2/M phase arrest. PKM2-IN-11 can be used for the study of breast cancer.

Larotaxel dihydrate (XRP9881 dihydrate) is an orally active and blood-brain barrier penetrant Microtubule stabilizer with an IC₅₀ of 0.21 μM. Larotaxel dihydrate shows activity in Taxane-resistant tumor models. Larotaxel dihydrate exhibits antitumor activity in intracranial glioblastoma models. Larotaxel dihydrate can be used for research on advanced solid tumors.

Tubulin polymerization activator-1 is a Tubulin polymerization promoter. Tubulin polymerization activator-1 induces Apoptosis, G2/M phase cell cycle arrest, and mitochondrial membrane potential depolarization. Tubulin polymerization activator-1 inhibits angiogenesis. Tubulin polymerization activator-1 exhibits anticancer activity against prostate cancer, melanoma, and cervical cancer. Tubulin polymerization activator-1 can be used for research on prostate cancer.

Milataxel (MAC-321) is an orally active taxane analog of Docetaxel (HY-B0011). Milataxel enhances the rate of tubulin polymerization. Milataxel can be used in the research of colorectal cancer and non-small cell lung cancer.

PROTAC HDAC8 Degrader-5 is a selective HDAC8 PROTAC degrader that mediates ubiquitination and proteasomal degradation through the formation of a ternary complex. PROTAC HDAC8 Degrader-5 degrades HDAC8 with a DC₅₀ of 1.8 nM in MDA-MB-231 cells and a DC₅₀ of 4.7 nM in Jurkat cells. PROTAC HDAC8 Degrader-5 inhibits cancer cell migration and proliferation, induces apoptosis through caspase 3/7 activation, and increases acetylated SMC3 and α-tubulin. PROTAC HDAC8 Degrader-5 is useful for cancer-related research, such as leukemia, triple-negative breast cancer, etc..

DNA-PK/HDAC6-IN-2 is an orally active and selective dual-target inhibitor of DNA-PK and HDAC6, with an IC₅₀ of 34.22 nM for DNA-PK and an IC₅₀ of 241.2 nM for HDAC6. DNA-PK/HDAC6-IN-2 upregulates Ac‑α‑tubulin, inhibits p‑DNA‑PK, and increases γ‑H2AX. DNA-PK/HDAC6-IN-2 exhibits antiproliferative activity against multiple solid tumor cell lines, induces apoptosis and cell cycle arrest, and inhibits migration and invasion. DNA-PK/HDAC6-IN-2 has in vivo antitumor efficacy in melanoma and breast cancer models and enhances the efficacy of Doxorubicin (HY-15142A). DNA-PK/HDAC6-IN-2 can be used for research on various cancers such as melanoma, breast cancer, and colorectal cancer.