SLx-2119
(Synonyms: 2-[3-[4-[(1H-吲唑-5-基)氨基]喹唑啉-2-基]苯氧基]-N-异丙基乙酰胺,SLx 2119;SLx2119;ROCK inhibitor;KD-025) 目录号 : GC12827
SLx-2119是一种高效的Rho kinase (ROCK) 2抑制剂，IC50值为105nM。
Cas No.:911417-87-3
Sample solution is provided at 25 µL, 10mM.
_1-3.$$$39978408@51.jpg');)
_1-9.$$$38538795@65.jpg');)
_1-9.$$$39112701@51.jpg');)
_1-7.$$$37316672@70.jpg');)
_366-372.$$$36198801@70.jpg');)
.$$$38565142@65.jpg');)
_1867-1883.$$$33248023@67.jpg');)
_eads6055.$$$39977546@45.jpg');)
_eadm9805.$$$40080571@45.jpg');)
_eadj3020.$$$39666821@45.jpg');)
_1-20.$$$39757301@28.jpg');)
_1-24.$$$38898113@28.jpg');)
_273-287.$$$36806353@46.jpg');)
_1-16.$$$37156877@44.jpg');)
_1-19.$$$37460805@44.jpg');)
_1291-1307.$$$34518654@46.jpg');)
SLx-2119 potent inhibits activity of Rho kinase (ROCK) 2, with an IC50 value of 105nM [1]. SLx-2119 binds to ROCK2 and suppresses aberrant pro-fibrotic signalling via downregulation of pro-fibrotic gene transcription, stress fiber formation, myofibroblast activation and collagen deposition[2]. SLx-2119 has been widely used in animal models to inhibit inflammatory responses[3].
In vitro, SLx-2119 treatment for 24 hours significantly inhibited the growth of human prostate epithelial cells (PrECs) and prostate cancer PC-3 cells, with IC50 values of 2028nM and 422nM, respectively[4]. Treatment with 3μM SLx-2119 for 24 days significantly inhibited the adipocyte differentiation of human adipose-derived stem cells (hADSCs) and downregulated the protein and mRNA expressions of various adipogenesis-related and adipogenesis markers, including PPARγ, C/EBPα, SREBP-1c, Glut4 and FABP4[5]. Treatment of CD4+ T cells with 10μM SLx-2119 for 1 hour significantly reduced the intracellular levels of IL-17 and IL-21, and inhibited the phosphorylation of STAT3[6].
In vivo, SLx-2119 treatment via oral administration at a dose of 100mg/kg/day for 1 weeks significantly inhibited the liver fibrosis induced by thiocarbamide (TAA) in C57BL/6 mice [7]. Continuous intraperitoneal injection of SLx-2119 (50mg/kg/day) for 28 consecutive days can reduce the body weight of obese mice induced by high-fat diet, improve lipid metabolism, and decrease the mass of white adipose tissue[8].
References:
[1] Boerma M, Fu Q, Wang J, et al. Comparative gene expression profiling in three primary human cell lines after treatment with a novel inhibitor of Rho kinase or atorvastatin[J]. Blood coagulation & fibrinolysis, 2008, 19(7): 709-718.
[2] Blair H A. Belumosudil: first approval[J]. Drugs, 2021, 81(14): 1677-1682.
[3] Yoon J H, Nguyen T T L, Duong V A, et al. Determination of KD025 (SLx-2119), a selective ROCK2 inhibitor, in rat plasma by high-performance liquid chromatography-tandem mass spectrometry and its pharmacokinetic application[J]. Molecules, 2020, 25(6): 1369.
[4] Hossain A, Yamamura A, Nayeem M J, et al. Rho kinase 2 promotes epithelial-mesenchymal transition and proliferation in human prostate cancer PC-3 cells[J]. Journal of Pharmacological Sciences, 2025.
[5] Diep D T V, Duong K H M, Choi H, et al. KD025 (SLx-2119) suppresses adipogenesis at intermediate stage in human adipose-derived stem cells[J]. Adipocyte, 2019, 8(1): 114-124.
[6] Zanin-Zhorov A, Weiss J M, Nyuydzefe M S, et al. Selective oral ROCK2 inhibitor down-regulates IL-21 and IL-17 secretion in human T cells via STAT3-dependent mechanism[J]. Proceedings of the National Academy of Sciences, 2014, 111(47): 16814-16819.
[7] Nalkurthi C, Schroder W A, Melino M, et al. ROCK2 inhibition attenuates profibrogenic immune cell function to reverse thioacetamide-induced liver fibrosis[J]. JHEP Reports, 2022, 4(1): 100386.
[8] Tran N N Q, Choi H, Sactivel B, et al. The dual targeting effects of KD025 on casein kinase 2 and ROCK2 in a mouse model of diet-induced obesity[J]. Biochemical Pharmacology, 2025, 237: 116933.
SLx-2119是一种高效的Rho kinase (ROCK) 2抑制剂，IC50值为105nM[1]。SLx-2119通过结合ROCK2，下调促纤维化基因转录、抑制应力纤维形成、肌成纤维细胞活化及胶原沉积，从而抑制异常的促纤维化信号传导[2]。SLx-2119已广泛应用于动物模型中以抑制炎症反应[3]。
在体外，SLx-2119处理24小时能显著抑制人前列腺上皮细胞(PrECs)和前列腺癌PC-3细胞的生长，IC50值分别为2028nM和422nM[4]。使用3μM的SLx-2119处理人脂肪来源干细胞(hADSCs) 24天，可显著抑制hADSCs向脂肪细胞分化，并下调多种脂肪生成相关标志物的蛋白和mRNA表达水平，包括PPARγ、C/EBPα、SREBP-1c、Glut4和FABP4 [5]。用10μM的SLx-2119处理CD4+T细胞1小时，能显著降低细胞内IL-17和IL-21水平，并抑制STAT3的磷酸化[6]。
在体内，通过每日口服100mg/kg剂量的SLx-2119，连续1周，可显著抑制硫代乙酰胺诱导的C57BL/6小鼠肝纤维化[7]。连续28天每日腹腔注射SLx-2119（50mg/kg/day），能够减轻高脂饮食诱导的肥胖小鼠体重、改善脂质代谢，并减少白色脂肪组织质量[8]。
| Cell experiment [1]: | |
Cell lines | Human adipose-derived stem cells (hADSCs) |
Preparation Method | The hADSCs were cultured in MesenPro RS medium, which was supplemented with 100units/ml penicillin and 100μg/ml streptomycin. The medium was placed in a humidified incubator at 37°C and 5% CO2. To differentiate into adipocytes, the cells were cultured for 2 days after confluence, and then the medium was replaced with StemPro adipocyte differentiation medium. During the specific culture period, the medium was changed every 3 days. During the entire experiment, the cells were treated with different concentrations (0.3, 0.5, 1, and 3μM) of SLx-2119, and stained with Oil Red O method on the 15th day. |
Reaction Conditions | 0.3, 0.5, 1, and 3μM; 15 days |
Applications | SLx-2119 significantly dose-dependently inhibited the lipid accumulation in hADSCs. |
| Animal experiment [2]: | |
Animal models | Male Sprague-Dawley rats |
Preparation Method | Male Sprague-Dawley rats (4 weeks old, 100-120g) were given a single subcutaneous injection of the vector (DMSO) or monocrotaline (MCT) (60mg/kg) on day 1. From day 8 to day 21, the rats were intraperitoneally injected with the vector (normal saline) or SLx-2119 (1mg/kg/day). On day 21, the rats were intraperitoneally injected with ketamine (100mg/kg) and sevoflurane (26mg/kg) for anesthesia, and the right ventricular pressure was measured. |
Dosage form | 1mg/kg/day for 14 days; i.p. |
Applications | SLx-2119 treatment attenuated right ventricular systolic pressure (RVSP) in rats with pulmonary hypertension (PH) caused by MCT. |
References: | |
| Cas No. | 911417-87-3 | SDF | |
| 别名 | 2-[3-[4-[(1H-吲唑-5-基)氨基]喹唑啉-2-基]苯氧基]-N-异丙基乙酰胺,SLx 2119;SLx2119;ROCK inhibitor;KD-025 | ||
| 化学名 | 2-(3-(4-((1H-indazol-5-yl)amino)quinazolin-2-yl)phenoxy)-N-isopropylacetamide | ||
| Canonical SMILES | O=C(C([H])([H])OC1=C([H])C([H])=C([H])C(C2=NC3=C([H])C([H])=C([H])C([H])=C3C(N([H])C(C([H])=C4[H])=C([H])C5=C4N([H])N=C5[H])=N2)=C1[H])N([H])C(C([H])([H])[H])([H])C([H])([H])[H] | ||
| 分子式 | C26H24N6O2 | 分子量 | 452.51 |
| 溶解度 | ≥ 22.65 mg/mL in DMSO, ≥ 26.4 mg/mL in EtOH with ultrasonic and warming | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
||
| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 2.2099 mL | 11.0495 mL | 22.099 mL |
| 5 mM | 442 μL | 2.2099 mL | 4.4198 mL |
| 10 mM | 221 μL | 1.1049 mL | 2.2099 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet