LEQ506, Smoothened 同源物拮抗剂

小分子

2-PYRAZINEMETHANOL, 5-((2R)-4-(4,5-DIMETHYL-6-(PHENYLMETHYL)-3-PYRIDAZINYL)-2-METHYL-1-PIPERAZINYL)-.ALPHA.,.ALPHA.-DIMETHYL- | 6SJX1T5HJD | 2-[5-[(2R)-4-(6-benzyl-4,5-dimethylpyridazin-3-yl)-2-methylpiperazin-1-yl]pyrazin-2-yl]propan-2-ol | NVP-LEQ506 |

LEQ506

L650147-5mg

5mg

≥98%

-20°C储存

超低温冰袋运输

LEQ506 is a second-generation inhibitor of smoothened ( Smo ) with IC 50 s of 2 and 4 nM in human and mouse, respectively. In Vitro LEQ506 is a second-generation inhibitor of smoothened (Smo) with IC 50 s of 2 and 4 nM in human and mouse, respectively. LEQ506 inhibits Hedgehog (Hh) signaling in a human cell line (HEPM) as measured by the amount of Gli mRNA with an IC 50 ~6-fold lower than that of Compound 2. LEQ506 is an efficacious compound by consistently decreasing Gli1 mRNA by about 70 to 80%. LEQ506 shows a tendency to preferentially inhibit Gli1 rather than Ptch1 mRNA. LEQ506 (at 1%) is also an efficacious compound with an inhibition of 80 to 90% for Gli1 and of 60 to 70% for Ptch1. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Assay DAOY cells are serum starved 16 h before experiments and subsequently incubated for 24 h with sonic Hedgehog (SHH) (50 nM) and LEQ506 at different concentrations . Cells are then washed twice with PBS and stored at -80°C until RNA isolation. Total RNA is isolated using the RNeasy Mini Kit. The amount and quality of extracted RNA are determined using the 2100 Bioanalyzer. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Form:Solid IC50& Target:IC50: 2 nM (human smo), 4 nM (mouse smo)

LEQ506 是第二代平滑肌酶（Smo）抑制剂，在人和小鼠体内的 IC 50 s 分别为 2 和 4 nM。

1204975-42-7

C25H32N6O

432.56 g/mol

45100669

C[C@@H]1CN(CCN1C2=NC=C(N=C2)C(C)(C)O)C3=NN=C(C(=C3C)C)CC4=CC=CC=C4

2-[5-[(2R)-4-(6-benzyl-4,5-dimethylpyridazin-3-yl)-2-methylpiperazin-1-yl]pyrazin-2-yl]propan-2-ol

1S/C25H32N6O/c1-17-16-30(11-12-31(17)23-15-26-22(14-27-23)25(4,5)32)24-19(3)18(2)21(28-29-24)13-20-9-7-6-8-10-20/h6-10,14-15,17,32H,11-13,16H2,1-5H3/t17-/m1/s1

POERAARDVFVDLO-QGZVFWFLSA-N

CC1CN(CCN1C2=NC=C(N=C2)C(C)(C)O)C3=NN=C(C(=C3C)C)CC4=CC=CC=C4

45100669

1204975-42-7

NVP-LEQ506

DMSO : ≥ 100 mg/mL (231.18 mM)

1

7

5

432.264 Da

432.264 Da

78.300 Ų

32

0

597.000

0

1

2.900

2.9

拮抗剂

Smoothened 同源物拮抗剂