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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KX2-391 (Mesylate)

KX2-391 Mesylate is an inhibitor of Src that targets the peptide substrate site of Src, with GI50 of 9-60 nM in cancer cell lines.

  • CAS Number: 1080645-95-9
  • MF: C27H33N3O6S
  • MW: 527.63200
  • Catalog: Microtubule/Tubulin
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Efalizumab

Efalizumab is a targeted T cell modulator, and is a humanized monoclonal antibody of CD11a, the α subunit of LFA-1. Efalizumab inhibits T cell activation, cutaneous T cell trafficking, and T cell adhesion to keratinocytes, can be used for plaque psoriasis research[1].

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

Abituzumab

Abituzumab (DI17E6) is a humanised anti-integrin αV monoclonal antibody (IgG2 type). Abituzumab effectively reduces the phosphorylation of FAK, Akt and ERK. Abituzumab can be used in cancer research, particularly in prostate cancer[1].

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

7-Xylosyltaxol

7-xylosyltaxol(Taxol-7-xyloside) is a taxol (Paclitaxel) derivative; Paclitaxel binds to tubulin and inhibits the disassembly of microtubules.IC50 Value:Target: Microtubule/TubulinPaclitaxel is a compound extracted from the Pacific yew tree with antineoplastic activity. Paclitaxel also induces apoptosis by binding to and blocking the function of the apoptosis inhibitor protein Bcl-2 (B-cell Leukemia 2). Paclitaxel inhibits DNA synthesis and stimulates the release of tumor necrosis factor-α. Paclitaxel induces apoptosis in murine mammary carcinoma MCA-4 and ovarian carcinoma OCA-1 tumors.

  • CAS Number: 90332-66-4
  • MF: C52H59NO18
  • MW: 986.021
  • Catalog: Microtubule/Tubulin
  • Density: 1.5±0.1 g/cm3
  • Boiling Point: 1062.3±65.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 596.3±34.3 °C

Tubulin inhibitor 24

Tubulin inhibitor 24 is a potent tubulin inhibitor. Tubulin inhibitor 24 inhibits tubulin polymerization. Tubulin inhibitor 24 induces cell cycle arrest at the G2/M phase in a concentration-dependent manner. Tubulin inhibitor 24 shows antitumor activity with no obvious toxicity[1].

  • CAS Number: 2415761-65-6
  • MF: C22H21N3O3
  • MW: 375.42
  • Catalog: Microtubule/Tubulin
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Tubulin polymerization-IN-15

Tubulin polymerization-IN-15 (compound 4) is a potent inhibitor of tubulin polymerization. Tubulin polymerization-IN-15 has the potential for the research of cancer diseases[1].

  • CAS Number: 2055517-66-1
  • MF: C18H17N3O4
  • MW: 339.35
  • Catalog: Microtubule/Tubulin
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Mps1-IN-4

Mps1-IN-4 is a selective Monopolar spindle 1 (Mps1) inhibitor with antiproliferative activity for cancer research[1].

  • CAS Number: 1263423-94-4
  • MF: C26H31F3N6O2
  • MW: 516.56
  • Catalog: Mps1
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Tubulin polymerization-IN-56

Tubulin polymerization-IN-56 (compound 8l), an indazole derivative, is a potent tubulin polymerization inhibitor through interacting with the colchicine site, resulting in cell cycle arrest and cellular apoptosis. polymerization-IN-56 reduces cell migration and leads to more potent inhibition of tumor growth in vivo[1].

  • CAS Number: 2966790-98-5
  • MF: C22H22ClN3O3
  • MW: 411.88
  • Catalog: Apoptosis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Tubulin inhibitor 35

Tubulin inhibitor 35 (compound 6b) is a dual inhibitor of topoisomerase I (IC50=~50 μM) and tubulin polymerization (IC50=5.69 μM). Tubulin inhibitor 35 inhibits migration and invasion of MGC-803 and RKO cell lines,and induces apoptosis via arresting cell cycle at G2/M phase. Tubulin inhibitor 35 exhibis potent efficacy in gastrointestinal tumor inhibiton (inhibits MGC-803 (IC50=0.09 μM) and RKO (IC50=0.2 μM) cell lines)[1].

  • CAS Number: 2247047-77-2
  • MF: C21H21N3O
  • MW: 331.41
  • Catalog: Apoptosis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Paprotrain

Paprotrain is a cell-permeable inhibitor of the kinesin MKLP-2, inhibits the ATPase activity of MKLP-2 with an IC50 of 1.35 μM and a Ki of 3.36 μM and shows a moderate inhibition activity on DYRK1A with an IC50 of 5.5 μM.

  • CAS Number: 57046-73-8
  • MF: C16H11N3
  • MW: 245.279
  • Catalog: Kinesin
  • Density: 1.3±0.1 g/cm3
  • Boiling Point: 470.1±40.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 149.2±12.5 °C

Tubulin polymerization-IN-12

Tubulin polymerization-IN-12 is a tubulin polymerization inhibitor (IC50=0.75 μM). Tubulin polymerization-IN-12 arrests cell cycle at G2/M phase, and exhibits cytotoxicity against cancer cells[1].

  • CAS Number: 2377301-45-4
  • MF: C23H23N5O6
  • MW: 465.46
  • Catalog: Microtubule/Tubulin
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

2-Naphthalenecarboxylic acid, 3-hydroxy-, 2-[(2,4,5-trihydroxyphenyl)Methylene]hydrazide

Hydroxy Dynasore (Dyngo-4a), a structural analog of Dynasore (HY-15304), is an potency improved, low cytotoxicity and non‐specific binding dynamin inhibitor with IC50 values of 0.38 μM and 2.3 μM for brain dynamin I and recombinant rat dynamin II, respectively. Hydroxy Dynasore inhibits dynamin‐dependent endocytosis of transferrin with an IC50 of 5.7 μM in vitro.

  • CAS Number: 1256493-34-1
  • MF: C18H14N2O5
  • MW: 338.314
  • Catalog: Dynamin
  • Density: 1.5±0.1 g/cm3
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Ansamitocin P-3

Ansamitocin P-3 is a microtubule inhibitor. Ansamitocin P-3 is a macrocyclic antitumor antibiotic.

  • CAS Number: 66584-72-3
  • MF: C32H43ClN2O9
  • MW: 635.145
  • Catalog: ADC Cytotoxin
  • Density: 1.3±0.1 g/cm3
  • Boiling Point: 833.1±65.0 °C at 760 mmHg
  • Melting Point: 190-192℃
  • Flash Point: 457.7±34.3 °C

MPH-220

MPH-220 is a selective and orally active inhibitor of skeletal muscle myosin-2. MPH-220 enables muscle relaxation. MPH-220 is anti-spastic agent that can be used in the research of spasticity and muscle stiffness[1].

  • CAS Number: 2649776-79-2
  • MF: C20H21N3O3S
  • MW: 383.46
  • Catalog: Myosin
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

A 286982

A-286982 is a potent and allosteric LFA-1/ICAM-1 interaction inhibitor with IC50s of 44 nM and 35 nM in an LFA-1/ICAM-1 binding and LFA-1-mediated cellular adhesion assay, respectively[1][2].

  • CAS Number: 280749-17-9
  • MF: C24H27N3O4S
  • MW: 453.55400
  • Catalog: Integrin
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Solidagonic acid

Solidagonic acid inhibits HSET motor activity by promoting the conversion from abnormal monopolar to bipolar spindles. Solidagonic acid suppresses fission yeast cell death and enables reversion of the mitotic spindles from a monopolar to bipolar morphology. Solidagonic acid showed the growth inhibitory activity on the seedlings of Lactuca sativa L. and Lolium multiflorum Lam[1][2].

  • CAS Number: 19941-91-4
  • MF: C22H34O4
  • MW: 362.503
  • Catalog: Kinesin
  • Density: 1.1±0.1 g/cm3
  • Boiling Point: 464.9±28.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 150.9±17.5 °C

Phomopsin A

Phomopsin A is a cyclic hexapeptide mycotoxin isolated from the fungus Phomopsis leptostomiformis. Phomopsin A is a noncompetitive inhibitor of the binding of radiolabeled vincristine to tubulin[1].

  • CAS Number: 64925-80-0
  • MF: C36H45ClN6O12
  • MW: 789.22800
  • Catalog: Microtubule/Tubulin
  • Density: 1.48g/cm3
  • Boiling Point: 1188.2ºC at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 672.4ºC

Pentachloropseudilin

Pentachloropseudilin (Antibiotic A 15104 Y; PClP) is a reversible and allosteric potent inhibitor of Myo1s (class 1 myosins) with IC50s range from 1 to 5 μM for mammalian class-1 myosins and greater than 90 μM for class-2 and class-5 myosins. Pentachloropseudilin is a potent inhibitor of transforming growth factor-β (TGF-β)-stimulated signaling, with an IC50 of 0.1 to 0.2 μM for TGF-β[1][2].

  • CAS Number: 69640-38-6
  • MF: C10H4Cl5NO
  • MW: 331.41
  • Catalog: Myosin
  • Density: 1.733g/cm3
  • Boiling Point: 445.9ºC at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 223.5ºC

Tubulin inhibitor 20

Tubulin inhibitor 20 (compound 1) is a potent inhibitor of tubulin. Tubulin inhibitor 20 has the potential for the research of cancer diseases[1].

  • CAS Number: 860356-56-5
  • MF: C19H18O4
  • MW: 310.34
  • Catalog: Microtubule/Tubulin
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Cilengitide TFA

Cilengitide is a potent and selective integrin inhibitor for αvβ3 and αvβ5 receptor, with IC50 values of 4 nM and 79 nM, respectively.

  • CAS Number: 199807-35-7
  • MF: C29H41F3N8O9
  • MW: 702.67900
  • Catalog: Autophagy
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Docetaxal

Docetaxal (10-Acetyl docetaxel; PNU-101383), an analog of Docetaxel (HY-B0011), is a microtubule disassembly inhibitor, with antimitotic activity. Docetaxal has cytotoxicity for murine leukemic cells[1].

  • CAS Number: 125354-16-7
  • MF: C45H55NO15
  • MW: 849.916
  • Catalog: Microtubule/Tubulin
  • Density: 1.4±0.1 g/cm3
  • Boiling Point: 901.4±65.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 499.0±34.3 °C

Myosin V-IN-1

Myosin V-IN-1 (compound 8) is a potent and selective Myosin V inhibitor, with a Ki of 6 μM. Myosin V-IN-1 shows acute inhibition of myosin V. Myosin V-IN-1 slows the actin-activated myosin V ATPase by specifically inhibiting ADP release from the actomyosin complex[1][2].

  • CAS Number: 1259177-59-7
  • MF: C29H26N6O3S
  • MW: 538.62
  • Catalog: Myosin
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

αvβ6 integrin inhibitor 2

αvβ6 integrin inhibitor 2 is a potent ανβ6 integrin inhibitor with an IC50 of 96.5 nM (WO2020081154A1, example 19)[1].

  • CAS Number: 313709-47-6
  • MF: C21H30N4O3
  • MW: 386.49
  • Catalog: Integrin
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

SB-267268

SB-267268 is a selective and nonpeptidic alpha(v)beta3 (αvβ3) and alpha(v)beta5 (αvβ5) integrins antagonist, with Kis of 0.9, 0.5 and 0.7 nM for human αvβ3, monkey αvβ3 and human αvβ5, respectively. SB-267268 inhibits human and mouse αvβ3 with IC50s of 0.68 and 0.29 nM, respectively. SB-267268 reduces angiogenesis and VEGF expression[1].

  • CAS Number: 205678-26-8
  • MF: C22H24F3N3O4
  • MW: 451.44
  • Catalog: Integrin
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

EILEVPST

EILEVPST is a recombinant human fibronectinderived low-molecular-weight peptide fragment. EILEVPST can promote cell type-specific α4 integrin-mediated adhesion. EILEVPST can be used for the research of thrombogenesis[1].

  • CAS Number: 239075-62-8
  • MF: C39H66N8O15
  • MW: 886.98600
  • Catalog: Integrin
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

GAP-134

Danegaptide (GAP-134), a small modified dipeptide, has been identified as a potent and selective second generation gap junction modifier with oral bioavailability.

  • CAS Number: 943134-39-2
  • MF: C14H17N3O4
  • MW: 291.30200
  • Catalog: Gap Junction Protein
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

JB002

JB002 is a myosin II inhibitor, with an IC50 of ≤10 μM. JB002 can be used for the research of muscle spasticity, chronic musculoskeletal pain, and hypertrophic cardiomyopathy[1].

  • CAS Number: 30408-07-2
  • MF: C18H15NO3
  • MW: 293.32
  • Catalog: Myosin
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Colchicine

Colchicine is a tubulin inhibitor and a microtubule disrupting agent. Colchicine inhibits microtubule polymerization with an IC50 of 3 nM.

  • CAS Number: 64-86-8
  • MF: C22H25NO6
  • MW: 399.437
  • Catalog: Autophagy
  • Density: 1.3±0.1 g/cm3
  • Boiling Point: 726.0±60.0 °C at 760 mmHg
  • Melting Point: 150-160 °C (dec.)(lit.)
  • Flash Point: 392.9±32.9 °C

Vincristine-d3 sulfate

Vincristine-d3 (Leurocristine-d3) sulfate is the deuterium labeled Vincristine sulfate. Vincristine sulfate is an antitumor vinca alkaloid which inhibits microtubule formation in mitotic spindle, resulting in an arrest of dividing cells at the metaphase stage. It binds to microtubule with a Ki of 85 nM[1][2].

  • CAS Number: 1246817-10-6
  • MF: C46H55D3N4O14S
  • MW: 926.05
  • Catalog: Apoptosis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Oryzalin

Oryzalin is a dinitroaniline herbicide, binding to plant tubulin and inhibits microtubule (MT) polymerization in vitro. Oryzalin depolymerizes MTs and prevented the polymerization of new MTs at all stages of the mitotic cycle[1].

  • CAS Number: 19044-88-3
  • MF: C12H18N4O6S
  • MW: 346.36000
  • Catalog: Microtubule/Tubulin
  • Density: 1.2
  • Boiling Point: 514ºC at 760mmHg
  • Melting Point: 141°C
  • Flash Point: 264.6ºC