SIS3 HCl |
Catalog No.GC17191
One-Click Copy Product Info
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SIS3 HCl은 Smad3 억제제로 IC50 3 μM로 Smad3의 인산화를 억제한다.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 521984-48-5
Sample solution is provided at 25 µL, 10mM.
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SIS3 HCl은 Smad3 억제제로 IC50 3 μM로 Smad3의 인산화를 억제한다.
SIS3 HCl은 농도에 따라 증가된 p3TP-lux 루시퍼아제 활동을 제거하고 변화 성장 인자(TGF-1)에 의해 유도된 Smad3의 인산화와 Smad3과 Smad4 간의 상호작용을 완화시킬 수 있고 SIS3 HCl은 Smad2의 인산화에 영향을 미치지 않는다. SIS3 HCl은 전사활성성을 감소시키는 방식으로 TGF-1의 효과를 완화시키고 TGF-1을 통해 성체 근섬유아세포의 분화를 억제한다 [1]. ML-12 세포에서 10 μM의 SIS3 HCl은 TGF-β를 통한 Smad3의 인산화를 차단했고 Smad2/3의 총량은 변하지 않았다 [2].
Tie2-Cre; Loxp-EGFP 쥐 연구에서 SIS3 HCl(2.5 mg/kg/일)은 스트레포토시신(STZ) 유발 당뇨병성 신증에서 Smad3 활성을 억제했다. SIS3 HCl은 엔도테리얼 메센치멀 전환을 제거하고, 신장섬유증을 줄이고 신장질환의 진행을 늦추었다[3]. 고지식 식이로 유도된 2형 다이어벳(T2DM) 모델 쥐에서 SIS3 HCl(5 mg/kg)은 체중, 지방량, 그리고 빵먹은 혈당을 현저하게 낮추었고 쥐의 인슐린 민감도와 구강 내당능도 개선했다[4].
References:
[1] Jinnin M et al. Characterization of SIS3, a novel specific inhibitor of Smad3, and its effect on transforming growth factor-beta1-induced extracellular matrix expression. Mol Pharmacol. 2006 Feb;69(2):597-607.
[2] Leiting S, Seidl S, Martinez-Palacian A, Muhl L, Kanse SM. Transforming Growth Factor-β (TGF-β) Inhibits the Expression of Factor VII-activating Protease (FSAP) in Hepatocytes. J Biol Chem. 2016 Sep 30;291(40):21020-21028.
[3] Li J et al. Blockade of endothelial-mesenchymal transition by a Smad3 inhibitor delays the early development of streptozotocin-induced diabetic nephropathy. Diabetes.2010 Oct;59(10):2612-24.
[4] Wang D C, Yan T T, Chen B, et al. SIS3, a good candidate for the reverse of type 2 diabetes mellitus in mice[J]. Fundamental & Clinical Pharmacology, 2021, 35(2): 389-396.
| 세포 실험 [1]: | |
세포 라인 | HK-2세포 |
제조 방법 | 세포는 0.1% DMSO로 처리하거나 5 μM SIS3 HCl로 1시간 처리한 후 25 μM CdCl2(Cd)를 포함하거나 포함하지 않는 조건에서 추가 30시간 더 배양했습니다. 세포의 생존성을 타이판 블루 배제 실험으로 결정했습니다. |
반응 조건 | 5 μM, 1 시간 동안 |
응용 분야 | SIS3 HCl은 카드뮴으로 유도된 HK-2세포 사멸을 억제했습니다. |
| 동물 실험 [2]: | |
동물 모형 | T2DM 쥐 모델 |
제조 방법 | 2형 당뇨병 진단된 쥐는 T2DM+식염수 투여 그룹, T2DM+차량 그룹, T2DM+SIS3 HCl 치료 그룹으로 무작위로 나뉘어졌습니다. 지속적인 약물 관리 45일 후에 빵먹은 혈당, 구강내당능, 인슐린 내성 자료를 측정했습니다. |
제형 | 5 mg/kg, 45일 동안, i.p. |
응용 분야 | SIS3 HCl은 쥐의 체중, 지방량, 빵먹은 혈당을 현저하게 낮추었고 인슐린 민감도와 구강 내당능도 개선했습니다. |
References: | |
| Cas No. | 521984-48-5 | SDF | |
| Chemical Name | (E)-1-(6,7-dimethoxy-3,4-dihydroisoquinolin-2(1H)-yl)-3-(1-methyl-2-phenyl-1H-pyrrolo[2,3-b]pyridin-3-yl)prop-2-en-1-one hydrochloride | ||
| Canonical SMILES | CN1C(C2=CC=CC=C2)=C(C3=C1N=CC=C3)/C([H])=C([H])/C(N4CCC5=CC(OC)=C(OC)C=C5C4)=O.Cl | ||
| Formula | C28H28ClN3O3 | M.Wt | 489.99 |
| Solubility | ≥ 49 mg/mL in DMSO, ≥ 11 mg/mL in EtOH with ultrasonic and warming | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.0409 mL | 10.2043 mL | 20.4086 mL |
| 5 mM | 408.2 μL | 2.0409 mL | 4.0817 mL |
| 10 mM | 204.1 μL | 1.0204 mL | 2.0409 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 3 reference(s) in Google Scholar.)