The cytoskeleton is a filamentous network of F-actin, microtubules, and intermediate filaments (IFs) composed of one of three chemically distinct subunits, actin, tubulin, or one of several classes of IF protein. Cytoskeleton not only helps cells maintain their shape and internal organization, but also provides mechanical support that enables cells to carry out essential functions like division and movement.

The cytoskeleton is involved in intracellular signal transduction at least two ways. First, individual proteins of the cytoskeleton might participate directly in signal transduction by linking two or more signaling proteins. Second, the cytoskeleton might provide a macromolecular scaffold, which spatially organizes components of a signal transduction cascade. Cell migration is a complex and multistep process involved in homeostasis maintenance, morphogenesis, and disease development, such as cancer metastasis, and requires coordination of cytoskeletal dynamics and reorganization, cell adhesion, and signal transduction, and takes a variety of forms. Many signaling pathways including Rho-family GTPases, Paxillin/FAK signaling and PI3K signaling is involved in the process by regulating cytoskeletal activity.

Since the cytoskeleton is involved in virtually all cellular processes, abnormalities in this essential cellular component frequently result in disease. Drugs that modulate microtubule stability, inhibitors of posttranslational modifications of cytoskeletal components, specifically compounds affecting the levels of tubulin acetylation, and compounds targeting signaling molecules which regulate cytoskeleton dynamics, constitute the mostly addressed therapeutic interventions for the diseases including cancer and neurodegenerative disorders.

References:
[1] Janmey PA. Physiol Rev. 1998 Jul;78(3):763-81.
[2] Forgacs G, et al. J Cell Sci. 2004 Jun 1;117(Pt 13):2769-75.
[3] Eira J, et al. . Prog Neurobiol. 2016 Jun;141:61-82.


Anti-infection >
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15-PGDH 5 alpha Reductase 5-Lipoxygenase Acetyl-CoA Carboxylase Acyltransferase Adenosine Deaminase Adenosine Kinase Aldehyde Dehydrogenase (ALDH) Aldose Reductase Aminopeptidase Angiotensin-converting Enzyme (ACE) ATGL ATP Citrate Lyase Carbonic Anhydrase Carboxypeptidase Cathepsin CETP COMT Cytochrome P450 Dipeptidyl Peptidase Dopamine β-hydroxylase E1/E2/E3 Enzyme Elastase Enolase FAAH FABP Factor Xa Farnesyl Transferase Fatty Acid Synthase (FAS) FXR Glucokinase GSNOR Gutathione S-transferase HCV Protease Hexokinase HIF/HIF Prolyl-Hydroxylase HIV Integrase HIV Protease HMG-CoA Reductase (HMGCR) HSP Indoleamine 2,3-Dioxygenase (IDO) Isocitrate Dehydrogenase (IDH) Lactate Dehydrogenase LXR MAGL Mineralocorticoid Receptor Mitochondrial Metabolism MMP Nampt NEDD8-activating Enzyme Neprilysin PAI-1 PDHK PGC-1α Phosphatase Phosphodiesterase (PDE) Phospholipase Procollagen C Proteinase Proteasome Pyruvate Kinase RAR/RXR Renin ROR Ser/Thr Protease SGK Stearoyl-CoA Desaturase (SCD) Thrombin Tryptophan Hydroxylase Tyrosinase Xanthine Oxidase
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Tirofiban hydrochloride

Tirofiban (L700462) hydrochloride is a Gp IIb/IIIa receptor antagonist of nonpeptide derivative of tyrosine. Tirofiban hydrochloride induces proliferation and migration on endothelial cell by inducing production of VEGF. Tirofiban hydrochloride can significantly reduces myocardial no-reflow and ischemia-reperfusion injury by alleviating myocardial microvascular structural and endothelial dysfunction in the ischemic area[1][2].

  • CAS Number: 142373-60-2
  • MF: C22H39ClN2O6S
  • MW: 495.073
  • Catalog: Integrin
  • Density: N/A
  • Boiling Point: 611.7ºC at 760mmHg
  • Melting Point: 223-225ºC
  • Flash Point: 323.7ºC

docetaxel trihydrate

Docetaxel Trihydrate is a semi-synthetic taxane analogue, acts as a microtubule stabilizer.

  • CAS Number: 148408-66-6
  • MF: C43H59NO17
  • MW: 861.925
  • Catalog: Microtubule/Tubulin
  • Density: 1.37 g/cm3
  • Boiling Point: 1016.9ºC at 760 mmHg
  • Melting Point: 186-192ºC
  • Flash Point: 568.8ºC

Tubulysin F

Tubulysin F is a highly cytotoxic peptide isolated from the myxobacterial species Archangium geophyra and Angiococcus disciformis. Tubulysin displays extremely potent cytotoxic activity in mammalian cells, including multidrug-resistant cell lines, with IC50 values in the lower nanomolar range[1]. Tubulysin F is a cytotoxic activity tubulysin which inhibits tubulin polymerization and leads to cell cycle arrest and apoptosis[2].

  • CAS Number: 368870-67-1
  • MF: C41H61N5O9S
  • MW: 800.02
  • Catalog: Apoptosis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

SR121566A

SR121566A is a novel non-peptide Glycoprotein IIb/IIIa (GP IIb-IIIa) antagonist, which can inhibit ADP-, arachidonic acid- and collagen-induced human platelet aggregation with IC50s of 46±7.5, 56±6 and 42±3 nM, respectively.

  • CAS Number: 180144-61-0
  • MF: C20H25N5O4S
  • MW: 431.51
  • Catalog: Integrin
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Tubulin/JAK2-IN-1

Tubulin/JAK2-IN-1 (compound 7g) is a dual inhibitor of Janus kinase 2 (JAK2) and microtubule. Tubulin/JAK2-IN-1 has potent antiproliferative activity against the cancer cells[1].

  • CAS Number: 2933938-46-4
  • MF: C22H20N6O3
  • MW: 416.43
  • Catalog: Microtubule/Tubulin
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Tubulin/MMP-IN-2

Tubulin/MMP-IN-2 is dual inhibitor of tubulin and matrix metalloproteinases. Tubulin/MMP-IN-2 can strongly inhibit tubulin polymerization and induces cell Apoptosis. Tubulin/MMP-IN-2 has inhibitory activities against MMP-2, MMP-3 and MMP-9 with IC50 values of 24.95 μM, 31.60 μM and 22.37 μM, respectively. Tubulin/MMP-IN-2 can be used for the research of cancer[1].

  • CAS Number: 2734877-51-9
  • MF: C40H48NO11P
  • MW: 749.78
  • Catalog: Apoptosis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Dynamin IN-2

Dynamin IN-2 (compound 43), a Wiskostatin (HY-12534) analogue, is a potent dynamin inhibitor, with an IC50 of 1.0 μM for dynamin I GTPase. Dynamin IN-2 also blocks clathrin mediated endocytosis (CME), with an IC50 of 9.5 μM[1].

  • CAS Number: 1345853-49-7
  • MF: C22H21ClN2O
  • MW: 364.87
  • Catalog: Dynamin
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

GNE 2861

PAK-IN-1 is a PAK inhibitor that displays group II selectivity. PAK-IN-1 inhibits PAK4, PAK5 and PAK6 with IC50s of 7.5, 36, 126 nM, respectively.

  • CAS Number: 1394121-05-1
  • MF: C22H26N6O2
  • MW: 406.48
  • Catalog: PAK
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

TN-16

TN-16 is a potent inhibitor of microtubule polymerization with IC50 of 0.4-1.7 µM[1].

  • CAS Number: 33016-12-5
  • MF: C19H18N2O2
  • MW: 306.35800
  • Catalog: Microtubule/Tubulin
  • Density: 1.249g/cm3
  • Boiling Point: 532.7ºC at 760 mmHg
  • Melting Point: 182-185 °C
  • Flash Point: 195.5ºC

iRGD peptide

iRGD peptide is a 9-amino acid cyclic peptide, triggers tissue penetration of drugs by first binding to av integrins, then proteolytically cleaved in the tumor to produce CRGDK/R to interact with neuropilin-1, and has tumor-targeting and tumor-penetrating properties.

  • CAS Number: 1392278-76-0
  • MF: C35H57N13O14S2
  • MW: 948.04
  • Catalog: Peptides
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

estramustine

Estramustine is an antineoplastic agent. Estramustine depolymerizes microtnbules by binding to tubulin 1, exhibits antimitotic activity with an IC50 value of ~16 μM for mitosis of DU 145 cells. Estramustine blocks cells at mitosis in prostate tumor xenografts[1].

  • CAS Number: 2998-57-4
  • MF: C23H31Cl2NO3
  • MW: 440.40300
  • Catalog: Microtubule/Tubulin
  • Density: 1.253 g/cm3
  • Boiling Point: 565.8ºC at 760 mmHg
  • Melting Point: 104 - 105ºC
  • Flash Point: 296ºC

W-7 hydrochloride

W-7 hydrochloride is a selective calmodulin antagonist. W-7 hydrochloride inhibits the Ca2+-calmodulin-dependent phosphodiesterase and myosin light chain kinase with IC50 values of 28 μM and 51 µM, respectively[1][2]. W-7 hydrochloride induces apoptosis and has antitumor activity[3].

  • CAS Number: 61714-27-0
  • MF: C16H22Cl2N2O2S
  • MW: 377.329
  • Catalog: Apoptosis
  • Density: N/A
  • Boiling Point: 518.8ºC at 760 mmHg
  • Melting Point: 220-222 °C
  • Flash Point: 267.6ºC

HI5

HI5 is a potent tublin and IDO inhibitor, with an IC50 value of 70 nM in HeLa cells. HI5 inhibit IDO expression and decrease kynurenine production, leading to stimulating T cells activation and proliferation. HI5 can inhibit tubulin polymerization and cell migration, cause G2/M phase arrest, and induce apoptosis via the mitochondrial dependent apoptosis pathway and cause reactive oxidative stress generation in HeLa cells. HI5 can be used for researching anticancer[1].

  • CAS Number: 2411548-90-6
  • MF: C42H43N5O8
  • MW: 745.82
  • Catalog: Apoptosis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

SB26019

SB26019 is a potent anti-neuroinflammatory agent. SB26019 regulates NF-κB activation by inducing monomeric α-tubulin formation. SB26019-induced α-tubulin monomer inhibits p65 translocation[1].

  • CAS Number: 1233078-90-4
  • MF: C24H20O4
  • MW: 372.41
  • Catalog: Microtubule/Tubulin
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Sevasemten

Sevasemten is an allosteric inhibitor of skeletal muscle myosin. Sevasemten exhibits selectively myosin inhibition with IC50s of ≤10 μM (skeletal), >100 μM (cardiac), respectively[1][2].

  • CAS Number: 2417395-15-2
  • MF: C16H11F4N5O2
  • MW: 381.28
  • Catalog: Myosin
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

D-64131

D-64131 is a novel inhibitor of Tubulin polymerization that competitively binds with [(3)H]colchicine to αβ-Tubulin. IC50 Value: N/ATarget: Microtubule/Tubulinin vitro: D-64131 is cytotoxic and inhibits tumor cell proliferation in vitro (IC50 = 74 nM). D-64131 prevents growth of tumor models in mice following oral administration in vivo. D-64131 has significant potential in cancer treatment. The proliferation of tumor cells from 12 of 14 different organs and tissues was inhibited with mean IC(50)s of 62 nM by D-64131.in vivo: In animal studies, no signs of systemic toxicity were observed after p.o. dosages of up to 400 mg/kg of D-64131. In xenograft experiments with the human amelanoic melanoma MEXF 989, D-64131 was highly active with treatment resulting in a growth delay of 23.4 days at 400 mg/kg. Therefore, D-64131 and analogues have the potential to be developed for cancer therapy, replacing or supplementing standard therapy regimens with tubulin-targeting drugs from natural sources.

  • CAS Number: 74588-78-6
  • MF: C16H13NO2
  • MW: 251.280
  • Catalog: Microtubule/Tubulin
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: 455.2±25.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 229.1±23.2 °C

ALB-109564 hydrochloride

ALB-109564 (12'-Methylthiovinblastine) hydrochloride, a tubulin inhibitor, is a cytotoxic agent designed to kill cancer cells by disrupting mitosis[1].

  • CAS Number: 1300114-12-8
  • MF: C47H62Cl2N4O9S
  • MW: 929.99
  • Catalog: Microtubule/Tubulin
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

SB273005

SB-273005 is a potent nonpeptide and orally active integrin antagonist with Kis of 1.2 nM and 0.3 nM for αvβ3 receptor and αvβ5 receptor, respectively[1].

  • CAS Number: 205678-31-5
  • MF: C22H24F3N3O4
  • MW: 451.44
  • Catalog: Integrin
  • Density: 1.3±0.1 g/cm3
  • Boiling Point: 662.9±55.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 354.7±31.5 °C

Scoulerine

Scoulerine ((-)-Scoulerine), an isoquinoline alkaloid, is a potent antimitotic compound. Scoulerine is also an inhibitor of BACE1 (ß-site amyloid precursor protein cleaving enzyme 1). Scoulerine inhibits proliferation, arrests cell cycle, and induces apoptosis in cancer cells[1].

  • CAS Number: 6451-73-6
  • MF: C19H21NO4
  • MW: 327.374
  • Catalog: Apoptosis
  • Density: 1.4±0.1 g/cm3
  • Boiling Point: 503.3±50.0 °C at 760 mmHg
  • Melting Point: 192ºC
  • Flash Point: 258.2±30.1 °C

Odulimomab

Odulimomab (anti-LFA1) is an anti-LFA-1 monoclonal antibody. Odulimomab inhibits proliferation of T lymphocyte and shows protective effects against ischemia and reperfusion injury. Odulimomab can be used for the research of transplant rejection and immunological disease[1][2].

  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

BTS

BTS is a potent inhibitor of Ca2+-stimulated myosin S1 ATPase (IC50 ~ 5 μM) and reversibly blocks the gliding motility. IC50 value: 5 uMTarget: Ca2+-stimulated myosin S1 ATPaseBTS also weakens myosin’s interaction with F-actin. BTS is much less effective in suppressing contraction in rat myocardial or rabbit slow twitch muscle and has no effect on platelet myosin II.

  • CAS Number: 1576-37-0
  • MF: C14H15NO2S
  • MW: 261.33900
  • Catalog: Myosin
  • Density: 1.204 g/cm3
  • Boiling Point: 419.1ºC at 760 mmHg
  • Melting Point: 115 °C
  • Flash Point: 207.3ºC

Mumefural

Mumefural is a bioactive component of the processed fruit of Prunus mume Sieb. Mumefural inhibits platelet aggregation. Mumefural shows anti-thrombotic effects and ameliorates cognitive impairment[1][2].

  • CAS Number: 222973-44-6
  • MF: C12H12O9
  • MW: 300.22
  • Catalog: Integrin
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

KX2-361

KX2-361 (KX-02) is a Src-kinase and tubulin polymerization inhibitor. KX2-361 shows good oral bioavailability and readily crosses the BBB in mice. KX2-361 shows anti-tumor activity and induces apoptosis of Glioblastoma (GBM) cell[1].

  • CAS Number: 897016-26-1
  • MF: C24H24FN3O2
  • MW: 405.46
  • Catalog: Apoptosis
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: 660.1±55.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 353.0±31.5 °C

Synstab A

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[1][2].

  • CAS Number: 257612-36-5
  • MF: C15H13BrCl3N3O3S
  • MW: 501.61
  • Catalog: Microtubule/Tubulin
  • Density: 1.73g/cm3
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

KY-04031

KY-04031 is a PAK4 inhibitor with IC50 of 0.79 uM, a basic building block in designing novel imidazo[4,5-b]pyridine-based PAK4 inhibitors.

  • CAS Number: 468056-29-3
  • MF: C21H20N8O
  • MW: 400.446
  • Catalog: PAK
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Tubulin polymerization-IN-19

Tubulin polymerization-IN-19 (compound 4) is a potent inhibitor of tubulin polymerization. Tubulin polymerization-IN-20 has the potential for the research of breast cancers and chemoresistant colon cancers[1].

  • CAS Number: 2340345-85-7
  • MF: C25H25NO5
  • MW: 419.47
  • Catalog: Microtubule/Tubulin
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

2-Methoxyestradiol-d5

2-Methoxyestradiol-d5 is the deuterium labeled 2-Hydroxyestradiol. 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[1][2][3][4][5][6][7].

  • CAS Number: 358731-34-7
  • MF: C19H21D5O3
  • MW: 307.44
  • Catalog: Apoptosis
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: 464.4±45.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 234.7±28.7 °C

CFI402257

CFI-402257 is a highly selective and orally bioavailable TTK and Mps1 inhibitor with Kis of 0.1 and 0.09 nM, respectively.

  • CAS Number: 1610759-22-2
  • MF: C28H30N6O3
  • MW: 498.58
  • Catalog: Mps1
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Mavacamten-d6

Mavacamten-d6 (MYK461-d6; SAR439152-d6) is deuterium labeled Mavacamten (HY-109037). Mavacamten (MYK461) is an orally active modulator of cardiac myosin, with IC50s of 490, 711 nM for bovine cardiac and human cardiac, respectively.

  • CAS Number: 2453251-18-6
  • MF: C15H13D6N3O2
  • MW: 279.37
  • Catalog: Myosin
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Cys-McMMAF

Cys-McMMAF is the released payload of AlMcMMAF, an anti-5T4 humanized A1 antibody conjugated to the microtubule disrupting MMAF (HY-15579) via a maleimidocaproyl linker. Cys-McMMAF has antitumor efficacy in two tumor mouse models (H1975 and MDA-MB-361-DYT2 models)[1].

  • CAS Number: 1160590-05-5
  • MF: C52H83N7O13S
  • MW: 1046.32
  • Catalog: Microtubule/Tubulin
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A