ITD 1 |
Catalog No.GC12108
One-Click Copy Product Info
|
ITD 1은 선택적 TGFβ 수용체 억제제(IC50 = 460nM)이다.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1099644-42-4
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');)
ITD 1은 선택적 TGFβ 수용체 억제제(IC50 = 460nM)이다. ITD 1은 Wnt/β-catenin 신호전달 경로를 억제해서 줄기세포의 심근세포 분화를 촉진한다[2]. ITD 1은 심장 재생 등 기초연구에 사용된다[3-4].
U87과 U251 세포에서 ITD 1(5µM; 24시간) 처리 후 세포 증식이 억제되었다[5]. 인간 섬유아세포에서 ITD 1(5µM; 24시간)은 저산소 조건에서 TβRII를 억제해서 p-Smad2/3 수준과 콜라겐 침착을 줄인다[6]. 인간 각막 내피세포에서 ITD 1(10µM; 48시간)은 세포 증식을 억제하고 노화를 가속하고 내피세포 표지자의 발현을 줄인다[7].
C57BL/6J 쥐에서 ITD 1(20㎕; 2000ng; 근육 주사; 4일)은 근육에서 TGF-β 활성을 감소시켰다[8]. 루이스 세포 피하 종양 쥐 모델에서 ITD 1(5mg/kg; 복강 주사; 5일)은 Smad2/3 신호를 억제해서 SAHA 유도 항종양 면역과 CD8+ T 세포 활성을 약화시켰다[9].
References:
[1]. Willems E, Cabral-Teixeira J, Schade D, et al. Small molecule-mediated TGF-β type II receptor degradation promotes cardiomyogenesis in embryonic stem cells[J]. Cell stem cell, 2012, 11(2): 242-252.
[2]. Zhong Q, Laco F, Liao M C, et al. Influencing the fate of cardiac and neural stem cell differentiation using small molecule inhibitors of alk5[J]. Stem cells translational medicine, 2018, 7(10): 709-720.
[3]. Plowright A T, Engkvist O, Gill A, et al. Heart regeneration: opportunities and challenges for drug discovery with novel chemical and therapeutic methods or agents[J]. Angewandte Chemie International Edition, 2014, 53(16): 4056-4075.
[4]. Lin Y H, Kang L, Feng W H, et al. Effects of lipids and lipoproteins on mesenchymal stem cells used in cardiac tissue regeneration[J]. International journal of molecular sciences, 2020, 21(13): 4770.
[5]. Sun Z, Yan T, Jiang H, et al. Claudin-3 facilitates the progression and mediates the tumorigenic effects of TGF-β in glioblastoma multiforme[J]. Medical Oncology, 2023, 40(9): 268.
[6]. Mingyuan X, Qianqian P, Shengquan X, et al. Hypoxia-inducible factor-1α activates transforming growth factor-β1/Smad signaling and increases collagen deposition in dermal fibroblasts[J]. Oncotarget, 2017, 9(3): 3188.
[7]. Ozen E A, Toprak E K, Donmez A Ç, et al. Investigation of the Effects of TGF-β and TGF-β Inhibitors on Cell Proliferation and Senescence in Human Corneal Endothelial Cells[J]. Acta Physiologica, 2023, 237.
[8]. Mázala D A G, Novak J S, Hogarth M W, et al. TGF-β–driven muscle degeneration and failed regeneration underlie disease onset in a DMD mouse model[J]. Jci Insight, 2020, 5(6): e135703.
[9]. Dong W, He B, Cao Y, et al. Low-dose SAHA enhances CD8+ T cell-mediated antitumor immunity by boosting MHC I expression in non-small cell lung cancer[J]. Cellular Oncology, 2025, 48(1): 249-264.
| 세포 실험 [1]: | |
세포 라인 | U87 및 U251 세포 |
제조 방법 | U87과 U251 세포를 96웰 판에 각각 5,000개의 세포 밀도로 파종하고 DMSO, TGF-β1(10ng/mL) 또는 ITD 1(5µM)로 처리하기 전에 37℃에서 24시간 동안 배양하였습니다. 처리 후 각 웰에 CCK-8 시약 10µL을 추가하고 24시간 동안 배양하였습니다. 그리고 세포 생존력을 평가하였습니다. |
반응 조건 | 5μM; 24시간 동안 |
응용 분야 | ITD 1 처리 후 세포 증식이 억제되었습니다. |
| 동물 실험 [2]: | |
동물 모형 | C57BL/6J 쥐 |
제조 방법 | 24일령 쥐는 이소플루란으로 마취하고 앞쪽 뒷다리의 털을 깎았습니다. 이 후에 28규의 인슐린 주사기로 비복근(TA) 근육에 NTX(10㎍/㎖) 40㎕를 주사하였습니다. 주사바늘은 먼저 녹색 문신 염료에 담가 손상 부위를 표시하였습니다. ITD 1 처리 그룹의 경우 ITD 1 2000ng을 NTX(10㎍/㎖) 30㎕에 추가해서 한쪽 TA 근육에 주사하였고 반대쪽 TA 근육은 NTX 30㎕만을 투여받았습니다. 최초 주사 후 2일과 4일째에는 ITD 1 투여 측의 TA 근육에 ITD 1(2000ng) 20㎕를 주사하였고 반대쪽 TA 근육은 동일한 부피의 생리식염수를 투여받았습니다. |
제형 | 20μL; 2000ng; im; 4 일 동안 |
응용 분야 | ITD 1은 근육에서 TGF-β 활성을 감소시켰습니다. |
References: | |
| Cas No. | 1099644-42-4 | SDF | |
| Chemical Name | (Z)-1-(5-(tert-butyl)isoxazol-3(2H)-ylidene)-3-(4-(7-(2-morpholinoethoxy)benzo[d]imidazo[2,1-b]thiazol-2-yl)phenyl)urea | ||
| Canonical SMILES | CC(C)(C1=C/C(NO1)=N/C(NC2=CC=C(C3=CN(C4=N3)C5=C(S4)C=C(OCCN6CCOCC6)C=C5)C=C2)=O)C | ||
| Formula | C29H32N6O4S | M.Wt | 560.67 |
| Solubility | ≥ 28.05mg/mL in DMSO | 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. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 1.7836 mL | 8.9179 mL | 17.8358 mL |
| 5 mM | 356.7 μL | 1.7836 mL | 3.5672 mL |
| 10 mM | 178.4 μL | 891.8 μL | 1.7836 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: >99.50% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 38 reference(s) in Google Scholar.)