MT-228 (BPN-0026709) is a selective and blood-brain barrier permeable non-muscle myosin II inhibitor. MT-228 markedly improves tolerability by selectively targeting NMIIB (KI = 1.5 μM) over CMII (KI = 17 μM), and the sequence of SmMll MD is 83.6% identical to that of NMllB. MT-228 shows long-lasting efficacy in animal models of stimulant use disorder.

Salvianolic acid A derivative-1 (Compound SAA-30) is a orally active derivative of Salvianolic acid A. Salvianolic acid A derivative-1 binds to transgelin with a KD of 2.39 μM. Salvianolic acid A derivative-1 promotes cell contractions by facilitating the aggregation of actin. Salvianolic acid A derivative-1 can be used for prevention of myocardial ischemia or other diseases associated with IR tissue injuries.

UR-12947 is a platelet glycoprotein (GP) IIb-IIIa antagonist. UR-12947 exhibits potent inhibitory activity against platelet aggregation in human platelet-rich plasma, with an IC50 value of 3.5 nM. UR-12947 can be used in the research of arterial thrombotic diseases.

ER-67880 is a potent microtubule inhibitor. ER-67880 exhibits anti-proliferative activity against KB, Colon 38 and P338 cells with IC50s of 0.55, 0.2 and 0.76 μg/mL. ER-67880 causes G2/M phase arrest and is accompanied by abnormal DNA replication. ER-67880 exhibits a down-regulation pattern of G1 phase-related genes, suggesting potential dehydrogenase inhibitory activity. ER-67880 can be used in various cancer studies, including those of nasopharyngeal carcinoma and murine adenocarcinoma.

Ispinesib (SB-715992) mesylate is a specific inhibitor of kinesin spindle protein (KSP), with a Ki app of 1.7 nM.

MT-110 (BPN-0027490) is a selective and blood-brain barrier permeable non-muscle myosin II inhibitor. MT-110 markedly improves tolerability by selectively targeting NMII over CMII. MT-110 can be used the study of neurological disease.

CP-664511 is an orally active and potent α4β1 integrin antagonist with anti-inflammatory effects (IC50=0.52 nM). CP-664511 inhibits the interaction between α4β1 and vascular cell adhesion molecule-1 (VCAM-1), significantly reducing eosinophil infiltration into lung tissue. CP-664511 is promising for research of asthma and allergic airway diseases.

EMD527040 (hydrochloride) is a highly potent and selective αvβ6 antagonist with anti-fibrotic activity. EMD527040 (hydrochloride) is used in the research of liver cancer and liver fibrosis.

FR-158999 is a potent orally active fibrinogen inhibitor. FR-158999 exhibits potent anti-platelet activities with a pIC50 of 7.50. FR-158999 can be used for antithrombotic research.

ZD 2486 is a glycoprotein IIb/IIIa (GP IIb/IIIa) antagonist. ZD 2486 inhibits platelet aggregation by blocking the binding of fibrinogen to the GP IIb/IIIa receptor on platelets. ZD 2486 can be used for the study of conditions related to unwanted platelet aggregation, such as acute coronary syndrome, unstable angina pectoris, acute myocardial infarction, and complications from cardiovascular interventional procedures[1]

NOTA-IMB-RGD is a dual molecular probe targeting integrin αvβ3 and programmed death ligand-1 (PD-L1). NOTA-IMB-RGD blocks the PD-1/PD-L1 signaling pathway and integrin αvβ3-overexpressing tumor vasculature. NOTA-IMB-RGD is promising for research of solid tumors co-expressing PD-L1 and αvβ3 (e.g., glioma, breast cancer).

RGD-DA6 is an αvβ3-targeted ligand. RGD-DA6 consists of RGDfK (an integrin αvβ3-targeted RGD peptide), DOTADG, d-Glu, Lys, AMBA, and IPBA. RGD-DA6 can be radiolabeled as an αvβ3-targeted radioligand and used for high-contrast tumor imaging and enhanced anticancer efficacy.

RGN6024 is a brain-penetrant, orally active and reversible small molecule tubulin destabilizer. RGN6024 inhibits microtubule polymerization both in biochemical and cellular assays, binds to the colchicine binding pocket of β-tubulin (SPR: Kd = 6.7 μM; tryptophan assay: Kd = 7.4 μM), and triggers G2/M arrest in glioblastoma (GB) cells. RGN6024 retains activity in βIII-tubulin overexpressing cells. RGN6024 inhibits tumor growth in a GB xenograft mouse model. RGN6024 can be used for the study of glioblastoma (GB).

NSC 330770, a demethylated hydrogenated molecule, is a potent tubulin polymerization inhibitor (IC50 of 2 μM). NSC 330770 elicites GTPase activity and the formation of abnormal polymers.

BTT-3034, a sulfonamide derivative, is an α2β1 integrin inhibitor. BTT-3034 inhibits cell adhesion to rat tail collagen I with an EC50 of 160 nM and a corresponding Emaxof 86%. BTT-3034 inhibits collagen binding by an α2 variant carrying the conformationally activating E318W mutation.

BAS00602705 is an E-cadherin inhibitor. BAS00602705 exerts its function by blocking the trans-interactions of E-cadherin molecules within junctional complexes, without permanently altering E-cadherin expression levels. BAS00602705 significantly impairs invadopodia formation in pancreatic cancer cells. BAS00602705 can be used for the study of anti-invasive therapeutic strategies in cancers characterized by dysregulated E-cadherin-mediated invadopodia activity, such as pancreatic ductal adenocarcinoma (PDAC).

4SC-207 is a potent, orally active microtubule inhibitor. 4SC-207 inhibits microtubule growth to inhibit tumor cell proliferation in vitro and in vivo, and promotes a mitotic delay/arrest, followed by apoptosis or aberrant divisions. 4SC-207 inhibits tumor growth in taxane resistant xenograft mouse models. 4SC-207 can be used for cancer research, such as colon adenocarcinoma and other malignancies.

J-30 is an orally active and potent tubulin inhibitor (IC50=15-20 nM). J-30 disrupts microtubule polymerization and induces G2/M phase arrest. J-30 is promising for research of solid tumors (e.g., gastric, oral).

BAS00093476 is an E-cadherin inhibitor. BAS00093476 exhibits inhibitory activity against E-cadherin-mediated cell-cell adhesion in human pancreatic tumor BxPC-3 cells. BAS00093476 can be applied to the research on the modulation of E-cadherin-mediated cell-cell adhesion in solid tumors expressing cadherins.

ME-3277 is a potent GPIIb/IIIa antagonist. ME-3277 reduces cerebral infarction without enhancing intracranial hemorrhage in photothrombotic occlusion of rabbit middle cerebral artery (MCA). ME-3277 can be used for the acute cerebral infarction research.

Tub114 is a drug-linker conjugate for ADC. Tub114 is a Tubulysin B analog with a stable hydrophilic linker. Tub114 can be used for synthesis of ADCs.

GP1 precursor has high affinity to GPIIb/IIIa receptors of activated platelets. GP1 precursor can be radiolabeled with [18F] and used as a PET Tracer for visualizing active platelet aggregation at the molecular level. GP1 precursor can be used for the detection of Thrombi.

XV459 is an orally active platelet GPIIb/IIIa receptor antagonist. XV459 blocks all agonist induced platelet aggregation by binding to platelet GPIIb/IIIa receptors. XV459 can significantly prolong occlusion time, reduce thrombus weight, and maintain blood flow. XV459 can be used for anti thrombotic research.

ON 01500 is a tubulin inhibitor with a Kd of 21 nM. ON 01500 exerts microtubule-destabilizing effects in cells. ON 01500 can be used the study of cancers.

ZJS178 is a novel inhibitor of myosin I. ZJS178 is a fungicide that has inhibitory activity against Fusarium graminearum and can reduce DON toxin synthesis. ZJS178 can be used for research on plant diseases such as wheat scab.

NVP-BQS481 (Compound 1) is a selective Kinesin spindle protein-5 (Eg5) inhibitor with an IC50< 0.5 nM. NVP-BQS481 has significant antimitotic and antitumor activity (IC50: 0.0.9 nM for SK-OV-3ip cells). NVP-BQS481 can be used as a cytotoxic payload for synthesis of antibody-drug conjugates (ADCs).

CLT-28643 is an integrin α5β1 inhibitor. CLT-28643 can inhibit the high expression of integrin α5β1 in the bleb at early time-points after surgery and promote wound healing process.

A-259745 is an orally active antimitotic agent that binds to the colchicine-binding site of tubulin. A-259745 exhibits potent in vitro cytotoxic activity against both multi-drug-resistant and non-multi-drug-resistant cancer cell lines, with ED50 values of 0.018 μM against HCT-15 and 0.028 μM against NCI-H460 cell lines. A-259745 inhibits tubulin polymerization, disrupts the dynamic equilibrium of the mitotic spindle, arrests dividing cells in metaphase, and subsequently induces apoptosis. A-259745 shows dose-dependent antitumor efficacy in murine tumor models. A-259745 can be used for the study of cancer.

Emvistegrast is a quinolone derivative. Emvistegrast is an antagonist of α4β7 integrin. Emvistegrast can be studied in research for diseases that are mediated by α4β7 integrin, such as infkammatory bowel disease.

MT-125 is a specific and well-tolerated inhibitor of non-muscle myosin IIA (Ki,NMIIA = 2.7 μM) and IIB (EC50 = 1.7 μM). MT-125 can pass through the blood-brain barrier. MT-125 induces ferroptosis and DNA damage by increasing the levels of reactive oxygen species (ROS) within tumor cells. MT-125 can enhance the PDGFR signaling pathway. MT-125 can be used for research on glioblastoma.