| LX7101 HCLDual LIM-kinase and ROCK inhibitor |

Sample solution is provided at 25 µL, 10mM.
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- Purity = 98.00%
- COA (Certificate Of Analysis)
- MSDS (Material Safety Data Sheet)
- Datasheet
Chemical structure


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| Cas No. | 1192189-69-7 | SDF | Download SDF |
| Chemical Name | InChI=1S/C23H29N7O3.ClH/c1-15-12-25-19-18(15)20(27-14-26-19)30-9-7-23(13-24,8-10-30)21(31)28-16-5-4-6-17(11-16)33-22(32)29(2)3;/h4-6,11-12,14H,7-10,13,24H2,1-3H3,(H,28,31)(H,25,26,27);1H | ||
| Canonical SMILES | CC1=CNC2=NC=NC(N3CCC(C(NC4=CC(OC(N(C)C)=O)=CC=C4)=O)(CN)CC3)=C21.Cl | ||
| Formula | C23H30ClN7O3 | M.Wt | 487.98 |
| Solubility | <4.88mg l="" in="" dmso="">4.88mg> | Storage | Store at -20°C |
| Physical Appearance | A solid | Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. | ||
Description:
IC50: 4.3, 32, 69 and 32 nM for LIMK2, KIMK1, ROCK1 and ROCK2, respectivley
LIM-kinases 1 and 2 (LIMK1 and LIMK2) regulate cytoskeletal dynamics by phosphorylating and deactivating cofilin, a protein that depolymerizes actin filaments. ROCK, a kinase upstream of LIMK in the signaling cascade that regulates actin filament dynamics, are being investigated in the clinic for reduction of IOP through relaxation of the trabecular meshwork. LX7101 is a dual LIM-kinase and ROCK inhibitor for the treatment of glaucoma.
In vitro: LX7101 proved significantly more selective for LIMK2. In addition, LX7101 was screened against a panel of 403 kinases. Moderate selectivity was observed in this screen (34 assays including LIMK2 and ROCK2 indicated that the Kd is most likely <1 μm)="" [1].="">1>
In vivo: At a well-tolerated dose, LX7101 achieved additional reduction of IOP compared to the 0.1% formulation and demonstrated a long duration of action, with IOP not returning to baseline until more than 8 h postdose. More critically, LX7101 produced a significantly greater reduction of IOP than either timolol or latanoprost [1].
Clinical trial: LX7101 completed IND enabling studies and was tested in a Phase 1 clinical trial in glaucoma patients, where it showed efficacy in lowering intraocular pressure [1].
Reference:[1] Harrison BA, Almstead ZY, Burgoon H, Gardyan M, Goodwin NC, Healy J, Liu Y, Mabon R, Marinelli B, Samala L, Zhang Y, Stouch TR, Whitlock NA, Gopinathan S, McKnight B, Wang S, Patel N, Wilson AG, Hamman BD, Rice DS, Rawlins DB. Discovery and Development of LX7101, a Dual LIM-Kinase and ROCK Inhibitor for the Treatment of Glaucoma. ACS Med Chem Lett. 2014 Nov 24;6(1):84-8.
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我的邮箱:maoyuanqing@citiz.net
**捷向您推荐美国Trevigen的一款通用PARP分析试剂盒检测试剂盒。该试剂盒是检测凋亡前与凋亡中细胞提取液中PARP活性的理想方案,操作简单,重复性高。其通过检测96孔板上生物素标记的多聚ADP核糖聚合到邻近组蛋白的反应,从而确定已知的或可能的PARP抑制剂。试剂盒中的依托泊苷(Etoposide)是拓扑异构酶Ⅱ抑制剂,在拓扑异构酶Ⅱ切割完DNA后能够稳定该酶。在试剂盒中,依托泊苷作为凋亡诱导的对照参与检测。
通量PARP/凋亡分析试剂盒可广泛应用于1)检测原代、肿瘤等细胞的PARP活性;2)检测凋亡前后的PARP活性;3)利用细胞裂解液筛选PARP抑制剂。
试剂盒特色比色法/化学发光法,无放射性输出。96well,高通量检测。极大地节省了分析时间,提高了使用效率。高敏感性。能够检测到500个细胞中低至0.1mU的PARP。检测范围广。0.1-10mU。样本用量少。仅仅需要10-100ng的提取物。检测时间短。仅需要3h即可完成检测。
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A.优点:
多重分析——一次分析可以检测16种干细胞相关的TF
定量比较——二个样本的差异可以定量分析和比较
步骤简单——探针温育、柱分离、板杂交和HRP检测
无需贵重仪器——无需如Luminex那样的贵重仪器
B.原理:
干细胞转录因子活性多重检测阵列试剂用于同时检测多种TF活性。该技术中,基于TFDNA结合位点的一致性序列,制备一系列生物素标记的探针。当探针混合物与核提取物一起温育时,每个探针寻找相应的TF,形成TF/探针复合物,通过柱离心纯化可以很容易与游离探针分开。结合的探针从混合物中分离出来,通过板杂交分析。板孔中预包被上与探针互补的特异序列,捕获的DNA探针进一步用链酶亲和素-HRP检测,化学发光检测仪测定发光强度(RLUs)。

