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 >
Apoptosis Bcl-2 Family c-Myc Caspase DAPK Ferroptosis IAP MDM-2/p53 PKD RIP kinase Survivin Thymidylate Synthase TNF Receptor
Autophagy >
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Antifolate APC ATM/ATR Aurora Kinase Casein Kinase CDK Checkpoint Kinase (Chk) CRISPR/Cas9 Deubiquitinase DNA Alkylator/Crosslinker DNA-PK DNA/RNA Synthesis Eukaryotic Initiation Factor (eIF) G-quadruplex Haspin Kinase HDAC HSP IRE1 Kinesin LIM Kinase (LIMK) Microtubule/Tubulin Mps1 Nucleoside Antimetabolite/Analog p97 PAK PARP PERK Polo-like Kinase (PLK) PPAR RAD51 ROCK Sirtuin SRPK Telomerase TOPK Topoisomerase Wee1
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Metabolic Enzyme/Protease >
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
Neuronal Signaling >
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NF-κB >
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Akt AMPK ATM/ATR DNA-PK GSK-3 MELK mTOR PDK-1 PI3K PI4K PIKfyve PTEN
PROTAC >
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Protein Tyrosine Kinase/RTK >
Ack1 ALK Bcr-Abl BMX Kinase Btk c-Fms c-Kit c-Met/HGFR Discoidin Domain Receptor DYRK EGFR Ephrin Receptor FAK FGFR FLT3 IGF-1R Insulin Receptor IRAK Itk PDGFR PKA Pyk2 ROS Src Syk TAM Receptor Trk Receptor VEGFR
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Casein Kinase ERK Gli GSK-3 Hedgehog Hippo (MST) JAK Notch Oct3/4 PKA Porcupine ROCK sFRP-1 Smo STAT TGF-beta/Smad Wnt YAP β-catenin γ-secretase
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Microtubule inhibitor 3

Compounds 17O (ic50= 14.0 nm, NCI-H460) and 17p (ic50= 2.9 nm, NCI-H460) and furan groups showed effective cytotoxic activity against various human cancer cell lines at the nanomolar level.

  • CAS Number: 1236141-96-0
  • MF: C26H23FN4O3
  • MW: 458.48
  • Catalog: Microtubule/Tubulin
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Pinatuzumab

Pinatuzumab is a CD22 monoclonal antibody. Pinatuzumab targets the cell-surface antigen CD22. Pinatuzumab can be used for synthesis of antibody drug conjugates (ADCs) to research several diseases including non-Hodgkin lymphoma (NHL)[1][2].

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

Paclitaxel

Paclitaxel is a potent anticancer medication which can promote microtubule (MT) assembly, inhibit MT depolymerization, and change MT dynamics required for mitosis and cell proliferation.

  • CAS Number: 33069-62-4
  • MF: C47H51NO14
  • MW: 853.906
  • Catalog: ADC Cytotoxin
  • Density: 1.4±0.1 g/cm3
  • Boiling Point: 957.1±65.0 °C at 760 mmHg
  • Melting Point: 213 °C (dec.)(lit.)
  • Flash Point: 532.6±34.3 °C

Tau-aggregation-IN-1

Tau-aggregation-IN-1 (Compound D-519) is a tau441 protein aggregation inhibitor with an IC50 of 21 µM. Tau-aggregation-IN-1 is also a dopamine D2 and D3 receptor agonist[1].

  • CAS Number: 1619269-19-0
  • MF: C28H37N5O2S
  • MW: 507.69
  • Catalog: Microtubule/Tubulin
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Tubulysin A

Tubulysin A(TubA) is a myxobacterial product that can function as an antiangiogenic agent in many in vitro assays; anti-microtubule, anti-mitotic, an apoptosis inducer, anticancer, anti-angiogenic, and antiproliferative.IC50 value: Target: microtubuleTubulysin A is a novel antibiotic, which is anti-microtubule, anti-mitotic, apoptosis inducer, anticancer, anti-angiogenic, and antiproliferative. Tubulysins are cytotoxic peptides, which include 9 members (A-I). Tubulysin A has potential application as an anticancer agent. It arrests cells in the G2/M phase. Tubulysin A inhibits polymerization more efficiently than vinblastine and induces depolymerization of isolated microtubules. Tubulysin A has potent cytostatic effects on various tumor cell lines with IC50 in the picomolar range.

  • CAS Number: 205304-86-5
  • MF: C43H65N5O10S
  • MW: 844.06900
  • Catalog: ADC Cytotoxin
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

ML-7 hydrochloride

ML-7 hydrochloride is a naphthalene sulphonamide derivative, potently inhibits MLCK (IC50=300 nM) and TRPC6 channel (IC50>10 μM).

  • CAS Number: 110448-33-4
  • MF: C15H18ClIN2O2S
  • MW: 452.738
  • Catalog: Myosin
  • Density: N/A
  • Boiling Point: 542.7ºC at 760 mmHg
  • Melting Point: 246-249ºC dec.
  • Flash Point: 282ºC

Tubulin inhibitor 26

Tubulin inhibitor 26 (compound 3c) is a potent inhibitor of tubulin. Tubulin inhibitor 26 is an indazole derivative compound. Tubulin inhibitor 26 shows noteworthy low nanomolar potency against HepG2, HCT116, SW620, HT29 and A549 cancer cell lines. Tubulin inhibitor 26 arrests tumor cell in G2/M phase and induced cell apoptosis. Tubulin inhibitor 26 suppresses tumor growth in vivo without affecting the mice body weight[1].

  • CAS Number: 2379241-70-8
  • MF: C17H19N3O3
  • MW: 313.35
  • Catalog: Microtubule/Tubulin
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

SF0166

SF0166 is a topically administered αvβ3 integrin antagonist, inhibits integrin-ligand interactions with IC50 of 0.6 nM to 13 nM for human αvβ3, αvβ6, and αvβ8; inhibits cellular adhesion to vitronectin across human, rat, rabbit, and dog cell lines with IC50 of 7.6 pM-76 nM; significantly decreases neovascularization in the oxygen-induced retinopathy mouse models. Other Indication Phase 2 Clinical

  • CAS Number: 1621332-91-9
  • MF: C23H27F2N5O4
  • MW: 475.497
  • Catalog: Integrin
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Echistatin

Echistatin, the smallest active RGD protein belonging to the family of disintegrins that are derived from snake venoms, is a potent inhibitor of platelet aggregation. Echistatin is a potent inhibitor of bone resorption in culture. Echistatin is a potent antagonist of αIIbβ3, αvβ3 and α5β1[1][2][3][4].

  • CAS Number: 154303-05-6
  • MF: C217H341N71O74S9
  • MW: 5417.0
  • Catalog: Integrin
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

(-)-Blebbistatin

(-)-Blebbistatin is an S enantiomer of blebbistatin. Blebbistatin is a potent and selective myosin II inhibitor with IC50s ranging from 0.5 to 5 μM.

  • CAS Number: 856925-71-8
  • MF: C18H16N2O2
  • MW: 292.33
  • Catalog: Myosin
  • Density: 1.3±0.1 g/cm3
  • Boiling Point: 486.7±55.0 °C at 760 mmHg
  • Melting Point: 210-212ºC
  • Flash Point: 248.1±31.5 °C

Fradafiban

Fradafiban is a nonpeptide platelet glycoprotein IIb/IIIa antagonist, which binds to the human platelet GP IIb/IIIa complex with a Kd value of 148 nM.

  • CAS Number: 148396-36-5
  • MF: C20H21N3O4
  • MW: 367.39800
  • Catalog: Integrin
  • Density: 1.38g/cm3
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Anticancer agent 48

Anticancer agent 48 (compound 48) is a broad spectrum anticancer agent. Anticancer agent 48 inhibits tubulin polymerization. Anticancer agent 48 shows antiproliferative activity. Anticancer agent 48 shows antitumor activity in vivo. Anticancer agent 48 has the potential for the research of solid and hematological tumors[1].

  • CAS Number: 2395009-13-7
  • MF: C26H25N3O4
  • MW: 443.49
  • Catalog: Microtubule/Tubulin
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

NVS-PAK1-1

NVS-PAK1-1 is a potent and selective allosteric PAK1 inhibitor with an IC50 of 5 nM.

  • CAS Number: 1783816-74-9
  • MF: C23H25ClF3N5O
  • MW: 479.93
  • Catalog: PAK
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Pironetin

Pironetin is an α/β unsaturated lactone isolated from Streptomyces species. Pironetin binds to α-tubulin and is a potent inhibitor of microtubule polymerization, and has cell cycle arrest and antitumor activity[1][2].

  • CAS Number: 151519-02-7
  • MF: C19H32O4
  • MW: 324.45500
  • Catalog: Microtubule/Tubulin
  • Density: 0.993 g/cm3
  • Boiling Point: 473.1ºC at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 160.3ºC

BIO 5192

BIO5192 is a selective and potent integrin α4β1 (VLA-4) inhibitor (Kd<10 pM). BIO5192 selectively binds to α4β1 (IC50=1.8 μM) over a range of other integrins. BIO5192 results in a 30-fold increase in mobilization of murine hematopoietic stem and progenitors (HSPCs) over basal levels[1][2].

  • CAS Number: 327613-57-0
  • MF: C38H46Cl2N6O8S
  • MW: 817.778
  • Catalog: Integrin
  • Density: 1.4±0.1 g/cm3
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Ceratamine A

Ceratamine A is an antimitotic heterocyclic alkaloid isolated from the marine sponge Pseudoceratina sp., acts as a microtubule-stabilizing agent. Ceratamine A exhibits cytotoxicity against human cancer cell lines[1][2][3].

  • CAS Number: 634151-15-8
  • MF: C17H16Br2N4O2
  • MW: 468.14300
  • Catalog: Microtubule/Tubulin
  • Density: 1.722g/cm3
  • Boiling Point: 543.271ºC at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 282.36ºC

ML-9 Free Base

ML-9 (Free Base) 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 (Free Base) inhibits inhibits MLCK, PKA and PKC activity with Ki values of 4, 32 and 54 μM, respectively[1]. ML-9 (Free Base) induces autophagy by stimulating autophagosome formation and inhibiting their degradation[3].

  • CAS Number: 110448-31-2
  • MF: C15H17ClN2O2S
  • MW: 324.82600
  • Catalog: Myosin
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

N2'-Deacetyl-N2'-[3-(methyldithio)-1-oxopropyl]maytansine

DM1-SMe is an unconjugated form of the Maytansinoid in IMGN901. DM1-SMe is about 3-10-fold more potent than the parent drug Maytansine, with IC50s ranging from 0.003 to 0.01 nM for DM1-SMe in a panel of human tumor cell lines[1].

  • CAS Number: 138148-68-2
  • MF: C36H50ClN3O10S2
  • MW: 784.37900
  • Catalog: ADC Cytotoxin
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Mavacamten

Mavacamten is a modulator of cardiac myosin, with IC50s of 490, 711 nM for bovine cardiac and human cardiac, respectively.

  • CAS Number: 1642288-47-8
  • MF: C15H19N3O2
  • MW: 273.330
  • Catalog: Myosin
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Tubulin inhibitor 23

Tubulin inhibitor 23 is a potent Tubulin inhibitor with an IC50 of 4.8 µM. Tubulin inhibitor 23 induces cell apoptosis. Tubulin inhibitor 23 shows antiangiogenic activity in a dose-dependent manner. Tubulin inhibitor 23 has the potential for the research of leukaemia[1].

  • CAS Number: 170488-57-0
  • MF: C26H23NO6S
  • MW: 477.53
  • Catalog: Apoptosis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

NMS-P715

NMS-P715 analog is an inhibitor of MPS1, with an IC50 of 84 nM.

  • CAS Number: 1202055-34-2
  • MF: C35H42N8O3
  • MW: 622.760
  • Catalog: Mps1
  • Density: 1.3±0.1 g/cm3
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

MMAF (Hydrochloride)

MMAF hydrochloride is an antitubulin agent that inhibit cell division; inhibits H3397 cell growth with an IC50 of 105 nM.

  • CAS Number: 1415246-68-2
  • MF: C39H66ClN5O8
  • MW: 768.42300
  • Catalog: ADC Cytotoxin
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

BAY1217389

BAY 1217389 is a potent, and selective inhibitor of the monopolar spindle 1 (MPS1) kinase with an IC50 value less than 10 nM.

  • CAS Number: 1554458-53-5
  • MF: C27H24F5N5O3
  • MW: 561.503
  • Catalog: Mps1
  • Density: 1.5±0.1 g/cm3
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

METHYLENE BLUE

Methylene blue (Basic Blue 9) hydrate is a guanylyl cyclase (sGC), monoamine oxidase A (MAO-A) and NO synthase (NOS) inhibitor. Methylene blue is a vasopressor and is often used as a dye in several medical procedures. Methylene blue hydrate through the nitric oxide syntase/guanylate cyclase signalling pathway to reduce prepulse inhibition. Methylene blue hydrate is a REDOX cycling compound and able to cross the blood-brain barrier. Methylene blue hydrate is a Tau aggregation inhibitor. Methylene blue hydrate reduces cerebral edema, attenuated microglial activation and reduced neuroinflammation[1][2][3].

  • CAS Number: 122965-43-9
  • MF: C16H20ClN3OS
  • MW: 337.86800
  • Catalog: Microtubule/Tubulin
  • Density: 0.6600g/ml
  • Boiling Point: N/A
  • Melting Point: 190ºC
  • Flash Point: N/A

AZ82

AZ82 is a selective HSET/KIFC1 inhibitor, with a Ki of 43 nM and an IC50 of 300 nM for KIFC1.

  • CAS Number: 1449578-65-7
  • MF: C28H31F3N4O3S
  • MW: 560.63
  • Catalog: Kinesin
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Vorsetuzumab mafodotin

Vorsetuzumab mafodotin (SGN-75) is an Auristatin-based anti-CD70 antibody-drug conjugate (ADC). Vorsetuzumab mafodotin consists of a humanized monoclonal antibody, Vorsetuzumab and an ADC cytotoxin MMAF. Vorsetuzumab mafodotin has antineoplastic activity[1].

  • CAS Number: 1165741-01-4
  • MF:
  • MW: 150 (kDa)
  • Catalog: Microtubule/Tubulin
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Dynamin IN-1

Dynamin IN-1 is a potent dynamin inhibitor with an IC50 value of 1.0 µM[1].

  • CAS Number: 1345853-50-0
  • MF: C23H24N2O
  • MW: 344.45
  • Catalog: Dynamin
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Larazotide

Larazotideis a peptide which is an orally active zonulin antagonist. Larazotide shows antiviral activity to varicella-zoster virus (VZV) with EC50s of 44.14 and 59.06 μM for strain OKA and 07-1, respectively. Larazotide can be used for the research of celiac disease and infection[1][2].

  • CAS Number: 258818-34-7
  • MF: C32H55N9O10
  • MW: 725.83300
  • Catalog: Gap Junction Protein
  • Density: 1.254
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

SB743921

SB-743921 is a potent inhibitor of the mitotic kinesin KSP (Eg5), with a Ki of 0.1 nM.

  • CAS Number: 940929-33-9
  • MF: C31H34Cl2N2O3
  • MW: 553.519
  • Catalog: Kinesin
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Abrilumab

Abrilumab is a fully human monoclonal antibody directed against α4β7. Abrilumab selectively binds the α4β7 integrin heterodimer. Abrilumab can be used for the research of inflammatory bowel disease (IBD)[1].

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