Cytoskeletal Signaling

Compound 4c: Strong tubulin inhibitor with anti-cancer & anti-angiogenic effects; halts MGC-803 cells in G2/M, triggers Caspase-mediated apoptosis.

FPDT combats glioblastoma by inhibiting the AKT pathway; IC50: >100 μM (astrocytes), 45-68 μM (GBM cells).

Iroxanadine hydrobromide is a MAPK p38 inhibitor potentially for the treatment of atherosclerosis.

<p>Lisavanbulin (BAL-101553) is a prodrug of Avanbulin (BAL 27862), a microtubule-targeting agent. It exhibits antitumor activity, particularly effective against tumors with high expression of end-binding protein 1.</p>

MonomethylauristatinE intermediate-17 is an intermediate compound used in the synthesis of MonomethylauristatinE. MonomethylauristatinE (MMAE) functions as a microtubule/tubulin inhibitor with anticancer properties. It is widely utilized as the cytotoxic component in antibody-drug conjugates (ADCs).

Nic-15 (compound 4n) serves as an anti-constrictive agent targeting the low vascular characteristics of pancreatic tumors. These characteristics enable cancer cells to adapt to the nutrient-deficient tumor microenvironment and develop resistance to treatment. Nic-15 modulates the PI3K/Akt/mTOR pathway and alleviates ER stress induced by Gemcitabine. It significantly inhibits migration and colony formation in MIA PaCa-2 and PANC-1 pancreatic cancer cells. When used in combination with Gemcitabine, Nic-15 effectively addresses resistance issues in pancreatic tumors. In xenograft models in vivo, Nic-15 notably enhances the efficacy of Gemcitabine.

ETB is a potent inhibitor of Hsp60 chaperone activity. It can impede the chaperone function of both wild-type proteins and the C237A and C447A mutant proteins. ETB binds to Hsp60 at Cys442, and the C442A mutant demonstrates resistance to ETB inhibition.

"Tubulin-IN-34 inhibits oxazolylisoindole microtubule assembly, selective for VL51 lymphoma."

KUNG65 acts as a selective Grp94 inhibitor, demonstrating a target dissociation constant (K_d) of 540 nM. It exhibits a minimum selectivity of 73-fold compared to other Hsp90 isoforms.

Tubulin polymerization-IN-74 (compound 11) is an inhibitor of tubulin polymerization, with an IC50 value of 15 μM. It is applicable to cancer research.

Hsp90 inhibitor

Isodienestrol, a derivative of Diethylstilbestrol, acts as a microtubule (Microtubule) inhibitor. It is utilized in cancer research.

TTBK1/2-IN-3 (compound 10) is a potent inhibitor of Tau tubulin kinase 1 (TTBK1) and TTBK2, with IC50 values of 579 nM and 258 nM, respectively. TTBK1/2-IN-3 can reduce the expression of primary cilia on the surface of human induced pluripotent stem cells (iPSC).

C086 is a novel and potent Hsp90 inhibitor that suppresses cell cycle progression, induces apoptosis, and exhibits anti-metastatic properties by modulating various mechanisms in different cell types.

Onalespib lactate is a second-generation, potent and selective HSP90 Inhibitor with antitumor activity.

Wikstrol A: antifungal, anti-mitotic, anti-HIV agent with various IC50/MDC values (67.8-131 µM) and deforms P. oryzae mycelia.

<p>PROTACα-synuclein degrader 6 (compound T3) is a PROTAC degrader of α-synuclein and tau, with an EC50 of 1.57 μM and 4.09 μM, respectively. This compound plays a significant role in neurodegenerative disease (ND) research.</p>

Tubulin polymerization-IN-75 (Compound 6) is an inhibitor of tubulin polymerization, with an IC50 value of 30 μM. It effectively suppresses the proliferation of cancer cells Huh7 and 293T, demonstrating IC50 values of 14.3 μM and 13.8 μM, respectively.

<p>Hsp90-IN-38 (compound 20m) is an inhibitor of HSP90 (heat shock protein). It demonstrates a strong binding affinity to HSP90 with a Kd of 87 nM. The compound inhibits ATPase activity with an IC50 of 0.13 μM. Hsp90-IN-38 also shows inhibitory effects on HCT116, MCF-7, SKBr3, K562, and A549 cells with IC50 values of 0.187, 0.072, 0.105, 0.403, and 0.031 μM, respectively.</p>

RMS-07, a covalent MPS1/TTK inhibitor, has an IC50 of 13.1 nM, targeting a kinase hinge cysteine.

GSD-11: Potent, selective anti-austerity agent; blocks Akt/mTOR pathway, hinders PANC-1 cell migration & colony growth. Promising for pancreatic cancer study.

KAA, an anticancer compound, inhibits centrosome clustering and targets HSET+ yeast and cancer cells.

AKT-IN-26 (Compound 453) is an AKT inhibitor that binds to the Pleckstrin Homology (PH) domain of AKT. It is useful for research related to cell proliferation and cancer involving the AKT pathway.

Icafolin-methyl is a plant-specific herbicide that acts as an inhibitor of tubulin polymerization. In plants, it metabolizes into the carboxylic acid icafolin, potentially inhibiting plant tubulin polymerization by binding to β-tubulin.

Compound 13m, a difluoro derivative, activates Nrf2/HO-1, showing neuroprotective and antioxidant effects, useful in PD research.

UM1 upregulates utrophin, has EC50 of 0.11 μM, useful in DMD research.

NRX-103094 boosts β-catenin binding to SCFβ-TrCP ligase with EC50 62 nM and Kd 0.6 nM.

NRX-1532 is a small molecule β-catenin:β-TrCP interaction enhancer.

AKT Kinase Inhibitor is an Akt inhibitor with antitumor activity that selectively inhibits cell proliferation in a dose-dependent manner.Cost-effective and quality-assured.

NRX-252114 promotes mutant β-catenin degradation, binding it to E3 ligase SCFβ-TrCP (EC50: 6.5 nM; Kd: 0.4 nM).

INS018 055 (TNIK&amp;MAP4K4-IN-2) is a TNIK and MAP4K4 inhibitor with anti-fibrotic activity.

Ombrabulin is a derivative of CA-4 phosphate. It is known to show antivascular effects through selective disruption of the tubulin cytoskeleton of endothelial cells.

Sevasemten is an allosteric inhibitor that targets skeletal muscle myosin. It displays selectivity in its inhibition, demonstrated by IC50 values of ≤10 μM for skeletal muscle myosin and >100 μM for cardiac myosin, respectively.

24-Methylenecycloartanyl ferulate, a compound belonging to the γ-oryzanol family, demonstrates the ability to enhance parvin-beta expression within human breast cancer cells. Furthermore, it exhibits potential as an ATP-competitive Akt1 inhibitor, with an EC 50 value of 33.3 μM.

ZW4864 is a selective inhibitor of the β-catenin/B-Cell Lymphoma 9 protein (β-catenin/BCL9 PPI) interaction, demonstrating oral activity. It inhibits β-catenin/BCL9 PPI with a K_i value of 0.76 μM and an IC_50 value of 0.87 μM.

Tau tracer 2 (Pl-2620) is a specific imaging agent designed to detect and visualize Tau protein aggregates, primarily used for diagnosing neurodegenerative diseases [1].

Cercosporin, produced by the plant pathogen Cercospora kikuchii and the elsinochromes, is a potent photosensitizer with a short activation wavelength. Cercosporin contains perylene quinone structural features essential for PKC activity (IC50: 0.6-1.3 μM).

Methyl (6-chloro-1H-benzo[d]imidazol-2-yl)carbamate is a useful organic compound for research related to life sciences. The catalog number is T65302 and the CAS number is 20367-38-8.

CMX-2043 is a drug potentially to block oxidative damage and activate cell survival pathways.

Cevipabulin (TTI-237) fumarate is a microtubule-active antitumor compound and inhibits the binding of [3H] vinblastine to tubulin (IC50: 18-40 nM in the human tumor cell line).

<p>BCR-ABL-IN-8 (compound 26f) is a BCR-ABL inhibitor featuring a trimethoxy group [1].</p>