| Bioactivity | 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]. | |||||||||
| Invitro | BTT-3033 (1 nM-100 μM, 2 h) inhibits CHO-α2wt cell adhesion to rat tail collagen Ⅰ (EC50: 130 nM), exhibits selectivity for α2β1 over α3β1, α4β1, α5β1 and αv[1].BTT-3033 (10 μM, 5 min) inhibits human platelet binding to collagenⅠcoated capillaries under flow, with the EC50 value for mouse whole blood to be 6 μM[1].BTT-3033 (10 μM, 5 min) inhibits binding of α2-expressing CHO cells to collagen Ⅰ under shear stress conditions[1].BTT-3033 (1 μM, 60 min) inhibits of neurogenic and thromboxane A2‐induced human prostate smooth muscle contraction[3].BTT-3033 (25 and 50 μM, 48 h) inhibits cell viability and proliferation by inducing G1 cell cycle arrest in LNcap‐FGC, and DU‐145 cells[4].BTT-3033 (50 μM, 48 h) induces apoptosis through the activation of ROS, Bax protein upregulation, caspase‐3 activation, and depletion of ΔΨm[4].BTT-3033 (10 μM, 15/28 days) suppresses MMP13 expression, increases the expression of MMP1 and MT-MMP1 in human articular cartilage‑derived chondrocytes[5]. Cell Viability Assay[4] Cell Line: | |||||||||
| Name | BTT-3033 | |||||||||
| CAS | 1259028-99-3 | |||||||||
| Formula | C23H20FN5O3S | |||||||||
| Molar Mass | 465.50 | |||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | |||||||||
| Storage |
|