Incyclinide (CMT-3)是一种非抗生素，由四环素衍生的基质金属蛋白酶（MMP）抑制剂。
Cas No.:15866-90-7
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');)
Incyclinide (CMT-3) is a non-antibiotic matrix metalloproteinase (MMP) inhibitor derived from tetracycline[1]. Incyclinide inhibits tumor growth, metastasis, and angiogenesis by inducing apoptosis in cancer cells and degrading the extracellular matrix, without exhibiting antimicrobial activity[2]. Incyclinide is commonly used in research on Kaposi's sarcoma, solid tumors, and neurodegenerative diseases such as Parkinson's disease[3,4].
In vitro, Incyclinide (10, 20μM) treatment of HeLa cells for 24h inhibited the expression of NF-κB and Bcl-2 proteins and induced the cleavage of procaspase-9, caspase-3, and PARP[5]. Incyclinide (25μM) pretreatment of human CD34+ stem cell-derived mast cells for 1h, followed by anti-IgE stimulation for 1h, showed an inhibitory trend on IgE-mediated histamine release (inhibition rate of 31.1%)[6].
In vivo, Incyclinide (30mg/kg; once daily) was administered by oral gavage to Wistar rats fitted with orthodontic appliances for 14 days, significantly inhibiting orthodontic tooth displacement[7]. Incyclinide (200mg/kg; once daily) was administered by oral gavage to C3H/HeN mice intravaginally infected with Chlamydia muridarum for 21 days (from day 1 to day 21 post-infection), significantly reducing the incidence of pyosalpinx on days 14 and 21 post-infection[8].
References:
[1] Islam M M, Franco C D, Courtman D W, et al. A nonantibiotic chemically modified tetracycline (CMT-3) inhibits intimal thickening[J]. The American Journal of Pathology, 2003, 163(4): 1557-1566.
[2] Lokeshwar B L. MMP inhibition in prostate cancer[J]. Annals of the New York Academy of Sciences, 1999, 878(1): 271-289.
[3] Richards C, Pantanowitz L, Dezube B J. Antimicrobial and non-antimicrobial tetracyclines in human cancer trials[J]. Pharmacological Research, 2011, 63(2): 151-156.
[4] González-Lizárraga F, Ploper D, Ávila C L, et al. CMT-3 targets different α-synuclein aggregates mitigating their toxic and inflammogenic effects[J]. Scientific Reports, 2020, 10(1): 20258.
[5] Zhao L, Xu J, Yang Y, et al. Inhibitory impacts of chemically modified tetracycline-3 and underlying mechanism in human cervical cancer cells[J]. Anti-Cancer Drugs, 2013, 24(8): 799-809.
[6] Sandler C, Ekokoski E, Lindstedt K A, et al. Chemically modified tetracycline (CMT)-3 inhibits histamine release and cytokine production in mast cells: possible involvement of protein kinase C[J]. Inflammation Research, 2005, 54(7): 304-312.
[7] Bildt M M, Henneman S, Maltha J C, et al. CMT-3 inhibits orthodontic tooth displacement in the rat[J]. Archives of Oral Biology, 2007, 52(6): 571-578.
[8] Imtiaz M T, Schripsema J H, Sigar I M, et al. Inhibition of matrix metalloproteinases protects mice from ascending infection and chronic disease manifestations resulting from urogenital Chlamydia muridarum infection[J]. Infection and Immunity, 2006, 74(10): 5513-5521.
Incyclinide (CMT-3)是一种非抗生素，由四环素衍生的基质金属蛋白酶（MMP）抑制剂[1]。Incyclinide通过诱导癌细胞细胞凋亡和基质降解，可抑制肿瘤生长、转移和血管新生，且不具抗菌活性[2]。Incyclinide通常用于卡波西肉瘤和实体肿瘤，以及帕金森病等神经退行性疾病的研究[3,4]。
在体外，Incyclinide（10, 20μM）处理HeLa细胞24h，抑制了NF-κB和Bcl-2蛋白表达，激活了procaspase-9、caspase-3和PARP的裂解[5]。Incyclinide（25μM）预处理人CD34+干细胞来源的肥大细胞1h，再用anti-lgE刺激1h，对lgE介导的组胺释放显示出抑制趋势（抑制率31.1%）[6]。
在体内，Incyclinide（30mg/kg; once daily）通过口服灌胃给药佩戴正畸装置的Wistar大鼠14天，显著抑制了正畸牙齿的移动[7]。Incyclinide（200mg/kg; once daily）通过灌胃给药于Chlamydia muridarum阴道感染的C3H/HeN小鼠21天（感染后第1天至第21天连续给药），在感染后第14天和第21天显著减少了输卵管积脓的发生率[8]。
| Cell experiment [1]: | |
Cell lines | HeLa cells |
Preparation Method | HeLa cells were treated with 10 and 20μM Incyclinide for 24h, and protein expression levels of NF-κB, Bcl-2, caspase-9, caspase-3, and PARP were analyzed by western blotting with β-actin as a loading control. |
Reaction Conditions | 10, 20μM; 24h |
Applications | Treatment of Incyclinide inhibits the expression of NF-κB and Bcl-2 proteins and activates the cleavage of procaspase-9, caspase-3, and PARP. |
| Animal experiment [2]: | |
Animal models | C3H/HeN mice infected with C. muridarum vaginally |
Preparation Method | C3H/HeN mice were used to establish an infection model by vaginal inoculation with C. muridarum. From day 1 to day 21 post-infection, mice were administered Incyclinide (200mg/kg) daily by gavage. Dissections were performed on days 7, 14, and 21 post-infection, and the incidence of pyosalpinx was observed visually. |
Dosage form | 200mg/kg; once daily; 21 days; i.g. |
Applications | Incyclinide treatment significantly reduced the incidence of pyosalpinx in mice on days 14 and 21 post-infection. |
References: | |
| Cas No. | 15866-90-7 | SDF | |
| 别名 | CMT-3; COL-3 | ||
| Canonical SMILES | O=C(C(C1=O)=C(O)C[C@]2([H])C[C@]3([H])CC4=C(C(C3=C(O)[C@@]21O)=O)C(O)=CC=C4)N | ||
| 分子式 | C19H17NO7 | 分子量 | 371.34 |
| 溶解度 | DMSO : ≥ 100 mg/mL (269.29 mM) | 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 | 2.6929 mL | 13.4647 mL | 26.9295 mL |
| 5 mM | 538.6 μL | 2.6929 mL | 5.3859 mL |
| 10 mM | 269.3 μL | 1.3465 mL | 2.6929 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: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet