| DC72605 |
JB062 |
JB062 is a nonmuscle myosin inhibitor with IC50 values of 1.6, 5.4, and >100 μM for Skeletal muscle myosin, Cardiac muscle myosin, and Smooth muscle myosin II, respectively. JB062 has cytotoxic to human cancer cells but not normal cells. JB062 can be used in research of muscle spasticity, chronic musculoskeletal pain, and hypertrophic cardiomyopathy. |
|
| DC72606 |
JB061 |
JB061 is a nonmuscle myosin inhibitor with IC50s of 4.4 μM (Cardiac muscle myosin), 9.1 μM (Skeletal muscle myosin), and >100 μM (Smooth muscle myosin II), respectively. JB061 poorly decreases ATPase activity (IC50>200 μM). JB061 shows cytotoxicity against COS-7 cells with an IC50 value of 39 μM. |
|
| DC72850 |
Fradafiban hydrochloride |
Fradafiban (BIBU-52) hydrochloride 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. |
|
| DC72908 |
AZD4877 |
AZD4877 is another isostere to Ispinesib and also a kinesin spindle protein (Eg5) inhibitor with IC50 of 2 nM.AZD4877 arrests cell mitosis, leads to the formation of the monopolar spindle phenotype and induces apoptosis. AZD4877 inhibits circulating peripheral blood mononuclear cells (PBMCs) and has anti-cancer activity. |
|
| DC73230 |
SD133 |
SD133 (Sd-133) is a drug-like small molecule inhibitor of adhesion molecule cadherin 11 (CDH11), binds specifically to the CDH11 binding pocket with KD of 25.2 uM in SPR assays. |
|
| DC73231 |
GB1490 |
GB1490 is a potent, selective and orally available galectin-1 (gal-1) inhibitor with Kd value of 0.4 uM and 0.23 uM for human and mouse galectin-1, respectively. |
|
| DC73232 |
6-B345TTQ |
6-B345TTQ is a small molecule inhibitor of the α4 integrin-paxillin interaction, impairs the interaction of native paxillin with α4 integrin, decreases α4-mediated cell migration. |
|
| DC73233 |
7HP349 |
Alintegimod (7HP349) is a small molecule activator of the integrins αLβ2 (LFA-1) and α4β1 (VLA-4). 7HP349 directly activates integrin cell adhesion receptors crucial for the generation of an immune response. |
|
| DC73234 |
A7B7C7 |
A7B7C7 (11-A7B7C7) is a potent Paxillin-α4 integrin binding antagonist with IC50 of 300 nM in vitro, decreases α4β1-mediated T cell migration. |
|
| DC73235 |
AXT107 |
AXT107 (AXT-107) mimetic peptide derived from collagen IV, binds integrins αvβ3 and α5β1 (Kd=1.29 and 2.21 nM), disrupts VEGFR2-β3 complex formation. |
|
| DC73236 |
GSK3335103
Featured
|
GSK3335103 is a highly potent and orally bioavailable nonpeptidic αvβ6 integrin inhibitor with pIC50 of 8.0. GSK3335103 shows high desirable oral pharmacokinetic profiles in rat, dog, and minipig, with low to moderate clearance, moderate volumes of distributio, high to complete oral bioavailabilities and high solubility in all physiological media. |
|
| DC73237 |
GW559090 |
GW559090 is a potent, selective, competitive and high-affinity α4β1 integrin (VLA-4) antagonist with Kd of 0.19/1.04 nM for huamn/rat α4β1, respectively. |
|
| DC73238 |
IVL745 |
IVL745 (IVL-745) is a small molecule very late antigen (VLA-4) antagonist with IC50 of 20 nM and 2 nM for adhesion to VCAM-1 and fibronectin, respectively. |
|
| DC73239 |
MSR03 |
MSR03 is a potent, pure small molecule αVβ3 antagonist with IC50 of 1.5 uM for inhibition of adhesion of cells expressing human αVβ3 to immobilized fibrinogen. |
|
| DC73240 |
TBC4746 |
TBC 4746 (AVA4746) is a small molecule mimetic of VCAM-1 that binds VLA-4 on B-ALL cells with high affinity and efficiently blocks ligand-binding with VCAM-1 with EC50 of 38.52 nM. |
|
| DC73241 |
AM-1882
Featured
|
AM-1882 (AM1882) is a potent, selective mitotic kinesin KIF18A inhibitor with IC50 of 230 nM in kinesin-8 microtubule (MT)-ATPase motor assays. |
|
| DC73242 |
AM-9022
Featured
|
AM-9022 (AM9022) is a potent, selective and orally active mitotic kinesin KIF18A inhibitor with IC50 of 47 nM in kinesin-8 microtubule (MT)-ATPase motor assays. |
|
| DC73243 |
ALM201 |
ALM201 is a small 23 amino acid peptide derived from the FK506 binding protein FKBPL, a targeted microtubule binding agent which exhibits potent anti-angiogenic activity in vitro and in vivo. |
|
| DC73244 |
CH-2-77 |
CH-2-77 is a potent colchicine-binding site inhibitor (CBSI) targeting tubulin, shows potent anti-proliferative activity against a panel of cancer cells in vitro and efficacious anti-tumor effects in vivo. |
|
| DC73245 |
CH-2-77 analogue 60c |
CH-2-77 analogue 60c is a potent colchicine-binding site tubulin inhibitor, inhibits tubulin polymerization and is effective against P-glycoprotein-mediated multiple drug resistance and taxol resistance. |
|
| DC73246 |
EAPB02303 |
EAPB02303 (EAPB 02303) is a novel microtubule-disrupting agent with in-vivo activity in PDAC and in-vitro synergy with Paclitaxel, inhibits A375 melanoma cell line with IC50 of 3 nM. |
|
| DC73247 |
FiVe1
Featured
|
FiVe1 is a vimentin binding small molecule that promotes vimentin disorganization and phosphorylation during metaphase, causes mitotic catastrophe, multinucleation, and the loss of stemness in cancer cells. |
|
| DC73248 |
KGP591 |
KGP591 is a small molecule inhibitor of tubulin polymerization with IC50 of 0.57 uM, exhibits cytotoxicity against the MCF-7 and MDA-MB-231 human breast cancer cell lines with GI50 of 320 and 102 nM, respectively. |
|
| DC73249 |
KGP618 |
KGP618 is the phosphate prodrug salt of KGP591, which is a small molecule inhibitor of tubulin polymerization with IC50 of 0.57 uM. |
|
| DC73250 |
Lexibulin |
An orally active tubulin polymerization inhibitor with potent cytotoxic and vascular disrupting activity in vitro and in vivo. |
|
| DC73251 |
R-huezole |
R-huezole is a phase-separating small molecule that forms liquid droplets to selectively sequester tubulin, enters cultured human cells and prevents cell mitosis by forming tubulin-concentrating condensates in cells. |
|
| DC73252 |
TN-2 |
TN-2 is a potent, dual tubulin/NRP1-targeting inhibitor with IC50 of 0.71 uM (tubulin polymerization) and 0.85 uM (NRP-1), inhibits proliferation and angiogenesis of tumor cells. |
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