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 >
Arenavirus Bacterial CMV Enterovirus Filovirus Fungal HBV HCV HIV HSV Influenza Virus Parasite Reverse Transcriptase RSV SARS-CoV
Antibody-drug Conjugate >
ADC Cytotoxin ADC Linker Drug-Linker Conjugates for ADC PROTAC-linker Conjugate for PAC
Apoptosis >
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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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Tubulin inhibitor 33

Tubulin inhibitor 33, a tubulin polymerization inhibitor, inhibits tubulin polymerization in a dose-dependent manner with an IC50 of 9.05 μM. Tubulin inhibitor 33 has antitumor effects and induces cell apoptosis that can be used for antitumor research[1].

  • CAS Number: 2944462-67-1
  • MF: C24H22N4O3
  • MW: 414.46
  • Catalog: Apoptosis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Tubulin polymerization-IN-31

Tubulin polymerization-IN-31 (Compound 4c) is a tubulin polymerization inhibitor with an IC50 of 3.64 μM. Tubulin polymerization-IN-31 induces cancer cell apoptosis and shows antitumor activity[1].

  • CAS Number: 2421121-79-9
  • MF: C18H13ClFN3
  • MW: 325.77
  • Catalog: Apoptosis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Paclitaxel-d5

Paclitaxel D5 is a deuterium-labeled Paclitaxel. Paclitaxel is a naturally occurring antineoplastic agent and stabilizes tubulin polymerization[1].

  • CAS Number: 1129540-33-5
  • MF: C47H46D5NO14
  • MW: 858.93700
  • Catalog: ADC Cytotoxin
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Fmoc-MMAE

Fmoc-MMAE is a protective group-conjugated monomethyl auristatin E (MMAE), which is a potent tubulin inhibitor. Fmoc-MMAE can be used in the synthesis of ADC[1].

  • CAS Number: 474645-26-6
  • MF: C54H77N5O9
  • MW: 940.22
  • Catalog: ADC Cytotoxin
  • Density: 1.1±0.1 g/cm3
  • Boiling Point: 1036.4±65.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 580.6±34.3 °C

KSP-IA

A potent, specific, allosteric and cell-active inhibitor of KSP with IC50 of 11 nM; has no ihibitory activity toward other kinesins, includin CENP-E, MKLP-1, KIF-3A, and uKHC (IC50>50 uM); induces the formation of monoastral spindles, causes mitotic arrest in a dose-dependent manner (EC50=30 nM) in A2780 ovarian carcinoma cells; sustained KSP inhibition activates the proapoptotic protein, Bax, and both activation of the spindle checkpoint and subsequent mitotic slippage are required for Bax activation.

  • CAS Number: 639074-49-0
  • MF: C21H22F2N2O
  • MW: 356.417
  • Catalog: Kinesin
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

KIF18A-IN-3

KIF18A-IN-3 is a potent KIF18A inhibitor (IC50=61 nM). KIF18A-IN-3 causes significant mitotic arrest and increases the number of mitotic cells in tumor tissues. KIF18A-IN-3 can be used for researching cancer[1].

  • CAS Number: 2600577-49-7
  • MF: C28H38N4O5S2
  • MW: 574.76
  • Catalog: Microtubule/Tubulin
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

H-Arg-Gly-Asp-Ser-Pro-Ala-Ser-Ser-Lys-Pro-OH acetate salt

RGDSPASSKP is a RGDS-containing fibronectin decapeptide[1].

  • CAS Number: 91575-25-6
  • MF: C40H68N14O16
  • MW: 1001.05000
  • Catalog: Integrin
  • Density: 1.61g/cm3
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Mivobulin

Mivobulin (NSC 613862) is a tubulin inhibitor, binds to tubulin in the region that overlaps the colchicine site, and inhibits tubulin polymerization. Mivobulin (NSC 613862) promotes the formation of abnormal polymers and a GTPase activity in the tubulin dimer. Anti-cancer activity[1].

  • CAS Number: 122332-18-7
  • MF: C17H19N5O2
  • MW: 315.40700
  • Catalog: Microtubule/Tubulin
  • Density: 1.36
  • Boiling Point: 483ºC at 760mmHg
  • Melting Point: N/A
  • Flash Point: 245.9ºC

Taxinine B

Taxinine B is a taxoid that can be isolated from Japanese Yew Taxus Cuspid. Taxinine B inhibits CaCl2-induced depolymerization of microtubule. Taxinine B is useful for overcoming multidrug resistance in tumor cells[1].

  • CAS Number: 18457-44-8
  • MF: C37H44O11
  • MW: 664.74
  • Catalog: Microtubule/Tubulin
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: 705.4±60.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 286.7±32.9 °C

Galacto-RGD trifluoroacetate salt

Galacto-RGD is an RGD analogue that can be coupled with the radioactive isotope 18F and used as an integrin α₅β₃ selective tracer[1].

  • CAS Number: 922175-70-0
  • MF: C34H52N10O12
  • MW: 792.83600
  • Catalog: Integrin
  • Density: 1.61±0.1 g/cm3 (20 °C, 760 mmHg)
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

S-Tritylcysteine

S-Trityl-L-cysteine (NSC 83265) is a selective and allosteric kinesin Eg5 inhibitor with an IC50 of 1 μM for the inhibition of basal ATPase activity and 140 nM for the microtubule-activated ATPase activity. S-Trityl-L-cysteine has antitumor activities[1][2].

  • CAS Number: 2799-07-7
  • MF: C22H21NO2S
  • MW: 363.47
  • Catalog: Apoptosis
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: 524.7±50.0 °C at 760 mmHg
  • Melting Point: 182-183 °C (dec.)(lit.)
  • Flash Point: 271.2±30.1 °C

Monastrol

Monastrol is a potent and cell-permeable inhibitor of the mitotic kinesin Eg5 with an IC50 value of 14 μM.

  • CAS Number: 329689-23-8
  • MF: C14H16N2O3S
  • MW: 292.353
  • Catalog: Kinesin
  • Density: 1.3±0.1 g/cm3
  • Boiling Point: 441.3±55.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 220.7±31.5 °C

Clathrin-IN-4

Clathrin-IN-4 (compound 8b), a Wiskostatin (HY-12534) analogue, is a potent inhibitor of clathrin mediated endocytosis with an IC50 of 2.1 μM. Clathrin-IN-4 is a dynamin I GTPase activity inhibitor with an IC50 of 9.1 μM[1].

  • CAS Number: 762242-59-1
  • MF: C17H18Br2N2O
  • MW: 426.15
  • Catalog: Dynamin
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

BMS 688521

BMS-688521 is a highly potent, orally active inhibitor of the LFA-1/ICAM interaction, with an IC50 of 2.5 nM in the adhesion assay and an IC50 of 60 nM in the MLR assay. BMS-688521 is efficacious in a mouse allergic eosinophilic lung inflammation model[1].

  • CAS Number: 893397-44-9
  • MF: C26H19Cl2N5O4
  • MW: 536.36600
  • Catalog: Integrin
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Vincristine-d3-ester sulfate

Vincristine-d3-ester (Leurocristine-d3-ester) 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].

  • CAS Number: 1217854-24-4
  • MF: C46H55D3N4O14S
  • MW: 926.05
  • Catalog: Apoptosis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

ML-9

ML-9 is a selective and potent inhibitor of Akt kinase, inhibits myosin light-chain kinase (MLCK) and stromal interaction molecule 1 (STIM1) activity[3]. ML-9 inhibits inhibits MLCK, PKA and PKC activity with Ki values of 4, 32 and 54 μM, respectively[1]. ML-9 induces autophagy by stimulating autophagosome formation and inhibiting their degradation[3].

  • CAS Number: 105637-50-1
  • MF: C15H18Cl2N2O2S
  • MW: 361.287
  • Catalog: Myosin
  • Density: N/A
  • Boiling Point: 508.8ºC at 760mmHg
  • Melting Point: 196-200ºC
  • Flash Point: 261.5ºC

H-Gly-Arg-Gly-Asp-Asn-Pro-OH

RGD peptide acts as an inhibitor of integrin-ligand interactions and plays an important role in cell adhesion, migration, growth, and differentiation[1]. RGD peptides promote apoptosis through activation of conformation changes that enhance pro-caspase-3 activation and autoprocessing[2][3].

  • CAS Number: 114681-65-1
  • MF: C23H38N10O10
  • MW: 614.61
  • Catalog: Integrin
  • Density: 1.7±0.1 g/cm3
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Tubulysin IM-2

Tubulysin IM-2 is an ADC Cytotoxin and tubulin binder used as anti-microtubule toxins.

  • CAS Number: 1032072-50-6
  • MF: C26H42N4O6S
  • MW: 538.70
  • Catalog: ADC Cytotoxin
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

AZ 13705339

AZ13705339 is a potent, selective PAK1 inhibitor with IC50 of 0.33 nM, displays 14-, 470-, 4100- and 2600-fold selectivity over Src, FGFR1, KDR and PAK4; inhibits cellular pPAK1 inhibition in MCF10A cell line with IC50 of 59 nM.

  • CAS Number: 2016806-57-6
  • MF: C33H36FN7O3S
  • MW: 629.747
  • Catalog: PAK
  • Density: 1.4±0.1 g/cm3
  • Boiling Point: 868.7±75.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 479.2±37.1 °C

Lygosporin A

Cytochalasin D (Zygosporin A; NSC 209835) is a potent and cell-permeable inhibitor of actin polymerization derived from fungus, inhibits the G-actin–cofilin interaction by binding to G-actin. Cytochalasin D (Zygosporin A; NSC 209835) also inhibits the binding of cofilin to F-actin and decreases the rate of both actin polymerization and depolymerization in living cells[1][2][3].

  • CAS Number: 22144-77-0
  • MF: C30H37NO6
  • MW: 507.618
  • Catalog: Arp2/3 Complex
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: 712.1±60.0 °C at 760 mmHg
  • Melting Point: 255-260ºC
  • Flash Point: 384.5±32.9 °C

Tadocizumab

Tadocizumab (C4G1; YM-337) is a humanized monoclonal antibody tageting integrin αIIbβ3. Tadocizumab has antiplatelet and antithrombotic effects, and can be used for cardiovascular disease research[1][2].

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

Tubulin inhibitor 12

Tubulin inhibitor 12 (Hit 9) is a novel tubulin inhibitor (IC50=25.3 μM). Tubulin inhibitor 12 shows anti-tumor activity and anti-proliferative activity[1].

  • CAS Number: 92575-00-3
  • MF: C24H20N2O
  • MW: 352.43
  • Catalog: Microtubule/Tubulin
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Wiskostatin

Wiskostatin is a potent and selective inhibitor of neuronal Wiskott-Aldrich syndrome protein (N-WASP)-mediated actin polymerization. Wiskostatin causes a rapid, profound, and irreversible decrease in cellular ATP levels[1].

  • CAS Number: 253449-04-6
  • MF: C17H18Br2N2O
  • MW: 426.146
  • Catalog: Arp2/3 Complex
  • Density: 1.6±0.1 g/cm3
  • Boiling Point: 320.2±22.0 °C at 760 mmHg
  • Melting Point: 153-155ºC
  • Flash Point: 147.4±22.3 °C

Violanone

Violanone, an isoflavanone compound, can inhibit tubulin polymerization. Violanone also exhibits larvicidal activity against A. aegypti[1][2].

  • CAS Number: 52250-38-1
  • MF: C17H16O6
  • MW: 316.305
  • Catalog: Microtubule/Tubulin
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

MK-0429

MK-0429 is a potent integrin antagonist with IC50s of 12.2 nM (α5β1 integrin) and 2.8 nM (αvβ3 integrin), respectively.

  • CAS Number: 227963-15-7
  • MF: C23H29N5O4
  • MW: 439.508
  • Catalog: Integrin
  • Density: 1.3±0.1 g/cm3
  • Boiling Point: 699.0±55.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 376.5±31.5 °C

Anticancer agent 98

Anticancer agent 98 (compound 12k) is a microtubule/tubulin-polymerization inhibitor (Kd=16.9 μM). Anticancer agent 98 exerts antiproliferative potency against tumor cells, exhibits anti-angiogenesis effect in vitro. Anticancer agent 98 exhibits good human and mouse liver microsomes stability with both t1/2>300 min[1].

  • CAS Number: 2857070-72-3
  • MF: C17H19N5O2
  • MW: 325.37
  • Catalog: Microtubule/Tubulin
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Tubulin inhibitor 18

Tubulin inhibitor 18 (compound 5j) is a potent inhibitor of tubulin. Tubulin inhibitor 18 is a chalcone compound. Tubulin inhibitor 18 has the potential for the research of cancer diseases[1].

  • CAS Number: 2762382-51-2
  • MF: C22H26O5
  • MW: 370.44
  • Catalog: Microtubule/Tubulin
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Vinblastine

Vinblastine is a cytotoxic alkaloid used against various cancer types. Vinblastine inhibits the formation of microtubule and suppresses nAChR with an IC50 of 8.9 μM.

  • CAS Number: 865-21-4
  • MF: C46H58N4O9
  • MW: 810.974
  • Catalog: Microtubule/Tubulin
  • Density: 1.4±0.1 g/cm3
  • Boiling Point: N/A
  • Melting Point: 211 - 216ºC
  • Flash Point: N/A

Tirofiban

Tirofiban(L700462;MK383) is a potent non-peptide, glycoprotein IIb/IIIa (integrins alphaIIbbetaIII) antagonistTarget: integrin IIb/IIIa Tirofiban hydrochloride monohydrate blocks platelet aggregation and thrombus formation. Tirofiban is an antithrombotic used in the treatment of unstable angina.Tirofiban, in a concentration-dependent manner reduced platelet aggregation evoked by ADP (IC50 approximately 70 ng/ml), collagen (IC50 approximately 200 ng/ml), and thrombin (IC50 approximately 5,000 ng/ml).

  • CAS Number: 144494-65-5
  • MF: C22H36N2O5S
  • MW: 440.597
  • Catalog: Integrin
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: 611.7±65.0 °C at 760 mmHg
  • Melting Point: 223-225ºC
  • Flash Point: 323.7±34.3 °C

JNJ-26076713

JNJ-26076713 is a potent and orally active alpha V integrin antagonist with IC50 values of 2.3 nM and 6.3 nM for alpha(V)beta(3) and alpha(V)beta(5), respectively. JNJ-26076713 inhibits retinal neovascularization[1].

  • CAS Number: 669076-03-3
  • MF: C29H38N4O3
  • MW: 490.63700
  • Catalog: Integrin
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A