Y-33075
(Synonyms: (R)-4-(1-氨基乙基)-N-1H-吡咯并[2,3-B]吡啶-4-基苯甲酰胺,Y 39983) 目录号 : GC37947
Y-33075是一种有效的ROCK（Rho相关蛋白激酶）抑制剂，IC50值为3.6nM。
Cas No.:199433-58-4
Sample solution is provided at 25 µL, 10mM.
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Y-33075 is a potent ROCK (Rho-associated protein kinase) inhibitor with an IC50 value of 3.6nM[1]. ROCK is a serine-threonine kinase belonging to the AGC (PKA/PKG/PKC) family of kinases and is present in mammals, zebrafish, Xenopus laevis, invertebrates, and chickens[2]. Y-33075 exhibits neuroprotective effects on retinal ganglion cells (RGCs)[3]. Treatment of Xenopus laevis with Y-33075 can disrupt the homeostasis of ciliated epithelial tissues, leading to abnormal epithelial growth at the tail margins[4].
In vitro, treatment of primary hepatic stellate cells (HSCs) isolated from FVB/NJ mice and the immortalized human hepatic stellate cell line (TWNT-4 cells) with Y-33075 (10nM-10µM) for 24h significantly reduced the contraction, fibrosis, and proliferation of activated mouse HSCs and TWNT-4 cells, while significantly increasing the migration of mouse HSCs[5]. Treatment of activated LX-2 cells with Y-33075 (10nM) downregulated the expression of ROCK and p-MLC and upregulated the expression of cAMP and PKA[6].
References:
[1] Vercammen H, Ondra M, Kotulova J, et al. “Keep on ROCKIn”: Repurposed ROCK inhibitors to boost corneal endothelial regeneration[J]. Biomedicine & Pharmacotherapy, 2024, 174: 116435.
[2] Amin F, Ahmed A, Feroz A, et al. An update on the association of protein kinases with cardiovascular diseases[J]. Current Pharmaceutical Design, 2019, 25(2): 174-183.
[3] Reboussin É, Bastelica P, Benmessabih I, et al. Evaluation of Rho kinase inhibitor effects on neuroprotection and neuroinflammation in an ex-vivo retinal explant model[J]. Acta Neuropathologica Communications, 2024, 12(1): 150.
[4] Khan F, Pitstick L, Lara J, et al. Rho-Associated protein kinase activity is required for tissue homeostasis in the Xenopus laevis ciliated epithelium[J]. Journal of Developmental Biology, 2024, 12(2): 17.
[5] Bachtler N, Torres S, Ortiz C, et al. The non-selective Rho-kinase inhibitors Y-27632 and Y-33075 decrease contraction but increase migration in murine and human hepatic stellate cells[J]. PLoS One, 2023, 18(1): e0270288.
[6] Zeng R, Guo Y, Qi J, et al. Dantao formula alleviates hepatic fibrosis and portal hypertension via modulation of the cAMP/PKA/ROCK signaling pathway in hepatic stellate cells[J]. Journal of Ethnopharmacology, 2025: 120650.
Y-33075是一种有效的ROCK（Rho相关蛋白激酶）抑制剂，IC50值为3.6nM[1]。ROCK是一种属于丝氨酸-苏氨酸激酶AGC（PKA/PKG/PKC）家族的激酶，存在于哺乳动物、斑马鱼、非洲爪蟾、无脊椎动物和鸡中[2]。Y-33075对视网膜神经节细胞（RGCs）具有神经保护作用[3]。Y-33075处理非洲爪蟾，能够破坏纤毛上皮组织稳态，导致尾部边缘出现异常上皮生长[4]。
在体外，Y-33075（10nM-10µM）处理从FVB/NJ小鼠分离的原代肝星状细胞（HSC）和永生化人肝星状细胞系（TWNT-4细胞）24h，显著降低了激活的小鼠HSC和TWNT-4细胞的收缩、纤维化和增殖，显著增加了小鼠HSC的迁移显著增加[5]。Y-33075（10nM）处理激活的LX-2细胞，下调了ROCK和p-MLC的表达，上调了cAMP和PKA的表达[6]。
| Cell experiment [1]: | |
Cell lines | Primary isolated HSC from FVB/NJ mice、the immortalized human HSC line TWNT-4 |
Preparation Method | Primary isolated HSC from FVB/NJ mice and the immortalized human HSC line TWNT-4 were culture-activated and incubated with Y-27632 and Y-33075 (10nM to 10μM) for 24h. Protein expression levels were analyzed by Western Blots and transcriptional levels of profibrotic markers and proliferative markers were evaluated using real-time qPCR. Migration was investigated by wound-healing assay. Proliferation was assessed by BrdU assay. |
Reaction Conditions | 10nM-10µM; 24h |
Applications | Both Rho-kinase inhibitors, Y-27632 and Y-33075, reduced contraction, fibrogenesis and proliferation in activated primary mouse HSC (FVB/NJ) and human HSC line (TWNT-4) significantly. Y-33075 demonstrated a 10-times increased potency compared to Y-27632. Both inhibitors mediated a substantial and unexpected increase in migration of HSC in FVB/NJ. |
References: | |
| Cas No. | 199433-58-4 | SDF | |
| 别名 | (R)-4-(1-氨基乙基)-N-1H-吡咯并[2,3-B]吡啶-4-基苯甲酰胺,Y 39983 | ||
| Canonical SMILES | O=C(NC1=C2C(NC=C2)=NC=C1)C3=CC=C(C=C3)[C@H](N)C | ||
| 分子式 | C16H16N4O | 分子量 | 280.32 |
| 溶解度 | DMSO: 50 mg/mL (178.37 mM and warming); Water: < 0.1 mg/mL (insoluble) | 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。 |
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| 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 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.5674 mL | 17.8368 mL | 35.6735 mL |
| 5 mM | 713.5 μL | 3.5674 mL | 7.1347 mL |
| 10 mM | 356.7 μL | 1.7837 mL | 3.5674 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
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet