BTT-3033

BTT-3033 is an orally active conformation-selective inhibitor of α2β1 (EC50: 130 nM) by binding to the α2I domain. BTT-3033 inhibits platelet binding to collagen I and cell proliferation, and induces cell apoptosis. BTT-3033 can be used in the research of prostate cancer, inflammation and cardiovascular disease[1][2][4].

Product Specifications

CAS Number

[1259028-99-3]

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Apoptosis; Integrin

Type

Reference compound

Related Pathways

Apoptosis; Cytoskeleton

Applications

COVID-19-immunoregulation

Field of Research

Cancer; Inflammation/Immunology; Cardiovascular Disease

Assay Protocol

https://www.medchemexpress.com/btt-3033.html

Purity

99.04

Solubility

DMSO : 250 mg/mL (ultrasonic)

Smiles

O=C(NC1=CC=C(N(S(=O)(C2=CN(C3=CC=C(C=C3)F)N=C2)=O)C)C=C1)NC4=CC=CC=C4

Molecular Formula

C23H20FN5O3S

Molecular Weight

465.50

Precautions

H302, H315, H319, H335

References & Citations

[1]Liisa Nissinen, et al. Novel α2β1 integrin inhibitors reveal that integrin binding to collagen under shear stress conditions does not require receptor preactivation. J Biol Chem. 2012 Dec 28;287 (53) :44694-702. |[2]Liisa Nissinen, et al. Sulfonamide inhibitors of α2β1 integrin reveal the essential role of collagen receptors in in vivo models of inflammation. Pharmacol Res Perspect. 2015 Jun;3 (3) :e00146. |[3]Bingsheng Li, et al. Inhibition of neurogenic and thromboxane A 2 -induced human prostate smooth muscle contraction by the integrin α2β1 inhibitor BTT-3033 and the integrin-linked kinase inhibitor Cpd22. Prostate. 2020 Aug;80 (11) :831-849. |[4]Zahra Salemi, et al. Integrin α2β1 inhibition attenuates prostate cancer cell proliferation by cell cycle arrest, promoting apoptosis and reducing epithelial-mesenchymal transition. J Cell Physiol. 2021 Jul;236 (7) :4954-4965. |[5]Takashi Kanamoto, et al. Integrin α2β1 plays an important role in the interaction between human articular cartilage-derived chondrocytes and atelocollagen gel. Sci Rep. 2021 Jan 19;11 (1) :1757.