SML0965

LDN-212854

≥98% (HPLC)

• 別名: 5-[6-[4-(1-Piperazinyl)phenyl]pyrazolo[1,5-a]pyrimidin-3-yl]-quinoline
• 実験式（ヒル表記法）: C₂₅H₂₂N₆
• CAS番号: 1432597-26-6
• 分子量: 406.48
• UNSPSCコード: 51111800
• NACRES: NA.77

特性

• 品質水準: 100
• アッセイ: ≥98% (HPLC)
• フォーム: powder
• 色: white to beige
• 溶解性: DMSO: 1 mg/mL, clear (warmed)
• 保管温度: 2-8°C
• SMILES記法: [n]21ncc(c2ncc(c1)c5ccc(cc5)N6CCNCC6)c3c4c(nccc4)ccc3
• InChI: 1S/C25H22N6/c1-3-21(22-4-2-10-27-24(22)5-1)23-16-29-31-17-19(15-28-25(23)31)18-6-8-20(9-7-18)30-13-11-26-12-14-30/h1-10,15-17,26H,11-14H2
• InChI Key: BBDGBGOVJPEFBT-UHFFFAOYSA-N

詳細

生物化学的／生理学的作用

LDN-212854 is a selective and potent inhibitor of the bone morphogenetic protein (BMP) type I receptor kinases with over 5,000-fold selectivity for BMP versus the closely related TGF-β and activin type I receptors. LDN-212854 has some selectivity for ALK2 with an IC₅₀ of 1.3 nM in preference to other BMP type I receptors, ALK1 (IC₅₀=2.4 nM) and ALK3 (IC₅₀=85.8 nM). LDN-212854 shows better selectivity than LDN193189 in cell-based assays of BMP signaling. LDN-212854 inhibited BMP6-induced osteogenic differentiation, which functions primarily via ALK2, more potently than BMP4, which functions primarily with ALK3 (IC₅₀s of 10 nM versus 40.5 nM), whereas LDN-193189 inhibited both equally. The only off target effects found against a panel of 198 kinases were for RIPK2, ABL1, and PDGFR-β with IC₅₀ values < 100 nM.

LDN-212854 is a selective and potent inhibitor of the bone morphogenetic protein (BMP) type I receptor kinases.

LDN-212854 is also known as 5-[6-[4-(1-Piperazinyl)phenyl]pyrazolo[1,5-a]pyrimidin-3-yl]-quinoline. LDN-212854 prevents heterotopic ossification in an inducible mutant ALK2 (activin receptor-like kinase 2).

安全性情報

• 保管分類コード: 11 - Combustible Solids
• WGK: WGK 3
• 引火点(°F): Not applicable
• 引火点(℃): Not applicable