STAT5-IN-1 (Synonyms: Signal Transducers and Activators of Transcription 5) |
Catalog No.GC13647
One-Click Copy Product Info
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STAT5 억제제는 IC50이 47 μ인 STAT5 억제제입니다. 아이소폼.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 285986-31-4
Sample solution is provided at 25 µL, 10mM.
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STAT5-IN-1 is a cell-permeable STAT5 inhibitor with an IC50 value of 47μM against the STAT5β isoform. STAT5-IN-1 blocks STAT5 signaling and STAT5-DNA binding by interacting with the SH2 domain of STAT5. STAT5-IN-1 selectively inhibits STAT5 and downregulates C/EBPβ and Acod1 expression. STAT5-IN-1 can be used in studies related to tumors, hematological diseases, and immunology[1-4].
In vitro, treatment of CD103+ cDC1 cells with 0-50μM STAT5-IN-1 for 9 days increased the proportion of Annexin V+7AAD- cells[5]. Treatment of TF-1(R140Q) cells with 25-100μM STAT5-IN-1 for 3 days blocked cytokine-independent proliferation in a concentration-dependent manner[6]. Treatment of NK cells with 100μM STAT5-IN-1 for 6 hours reduced p-S6Ser235/236 levels[7].
In vivo, oral administration of 10mg/kg STAT5-IN-1 every other day to high-fat diet-fed ApoE-/- mice for 12 weeks reduced atherosclerotic plaque area in the aortic arch and aortic root. STAT5-IN-1 decreased aortic ICAM-1, VCAM-1, TNF-α, and IL-6 mRNA levels and reduced aortic TNF-α and IL-6 protein levels[8]. Intraperitoneal injection of 20mg/kg STAT5-IN-1 every three days to MC38 colon adenocarcinoma-bearing Rig-I-/- mice for 22 consecutive days restored tumor growth[9].
References:
[1] Fanti M, Brandhorst S, Navarrete G, et al. Methionine-supplemented longevity diet increases growth hormone, GLP-1, and FGF21; reduces frailty; and promotes healthspan. Cell Metab. 2026 Aug 4;38(8):1579-1598.e6.
[2] Chen S, Lu H, Ying Y, et al. IL2RG knockout mitigates polycystic ovary syndrome pathogenesis by transitioning pyroptosis to apoptosis through the GSDME pathway. Journal of Ovarian Research. 2025 Aug 19;18:189.
[3] Zhu F, Chen H, Xu M, et al. Cryptotanshinone possesses therapeutic effects on ischaemic stroke through regulating STAT5 in a rat model. Pharmaceutical Biology. 2021;59(1):465-471.
[4] Yovas A, Stanely SP, Issac R, et al. β-caryophyllene blocks reactive oxygen species-mediated hyperlipidemia in isoproterenol-induced myocardial infarcted rats. Eur J Pharmacol. 2023 Dec 5;960:176102.
[5] Xu F, Liu C, Dong Y, et al. Ablation of Cbl-b and c-Cbl in dendritic cells causes spontaneous liver cirrhosis via altering multiple properties of CD103+ cDC1s. Cell Death Discovery. 2022;8:142.
[6] Yang J, Chen J, Chang J, et al. IDH2/R140Q mutation confers cytokine-independent proliferation of TF-1 cells by activating constitutive STAT3/5 phosphorylation. Cell Commun Signal. 2024 Feb 12;22:116.
[7] Wang F, Meng M, Mo B, et al. Crosstalks between mTORC1 and mTORC2 variagate cytokine signaling to control NK maturation and effector function. Nat Commun. 2018 Nov 19;9:4874.
[8] Wang X, Ding X, Yan J, et al. STAT5 inhibitor attenuates atherosclerosis via inhibition of inflammation: the role of STAT5 in atherosclerosis. Am J Transl Res. 2021;13(3):1422-1431.
[9] Jiang X, Lin J, Shangguan C, et al. Intrinsic RIG-I restrains STAT5 activation to modulate antitumor activity of CD8+ T cells. J Clin Invest. 2023;133(9):e160790.
| Cell experiment [1]: | |
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Cell lines |
TF-1(R140Q) cells (human erythroleukemia isogenic cell line with IDH2/R140Q mutation) |
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Preparation Method |
TF-1(R140Q) cells were cultured in RPMI-1640 medium supplemented with 10% FBS at 37°C, 5% CO2. TF-1(R140Q) cells were treated with STAT5-IN-1 at increasing concentrations for 3 days in the absence of GM-CSF, followed by MTT assay for cell viability evaluation. |
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Reaction Conditions |
25-100μM; 3 days |
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Applications |
STAT5-IN-1 blocked cytokine-independent proliferation of TF-1(R140Q) cells in a concentration-dependent manner with IC50 of 308.1μM. |
| Animal experiment [2]: | |
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Animal models |
ApoE-/- mice (male, 16-22g, 10 weeks) |
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Preparation Method |
ApoE-/- mice were fed a high-fat diet (0.2% cholesterol) for 12 weeks and orally administered STAT5-IN-1 (10mg/kg every other day) by gavage for 12 weeks. After treatment, arterial tissues were collected for histological, immunofluorescence, qPCR and western blot analysis, and serum was collected for lipid measurement. |
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Dosage form |
10mg/kg; p.o.; every other day; 12 weeks |
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Applications |
STAT5-IN-1 inhibited phosphorylation of STAT5 in arterial tissue. STAT5-IN-1 reduced atherosclerotic lesion area in aortic arch and aortic root. STAT5-IN-1 decreased mRNA levels of ICAM-1, VCAM-1, TNF-α and IL-6 and protein levels of TNF-α and IL-6 in atherosclerotic aortas. STAT5-IN-1 did not change body weight or serum TG, TCH, HDL-C and LDL-C levels. |
References: [1] Yang J, Chen J, Chang J, et al. IDH2/R140Q mutation confers cytokine-independent proliferation of TF-1 cells by activating constitutive STAT3/5 phosphorylation. Cell Commun Signal. 2024 Feb 12;22:116. [2] Wang X, Ding X, Yan J, et al. STAT5 inhibitor attenuates atherosclerosis via inhibition of inflammation: the role of STAT5 in atherosclerosis. Am J Transl Res. 2021;13(3):1422-1431. | |
| Cas No. | 285986-31-4 | SDF | |
| Synonyms | Signal Transducers and Activators of Transcription 5 | ||
| Chemical Name | 2-[(4-oxo-4H-1-benzopyran-3-yl)methylene]hydrazide 3-pyridinecarboxylic acid | ||
| Canonical SMILES | O=C(N/N=C/C1=COC(C=CC=C2)=C2C1=O)C3=CC=CN=C3 | ||
| Formula | C16H11N3O3 | M.Wt | 293.3 |
| Solubility | ≤5mg/ml in DMSO;2mg/ml in dimethyl formamide | 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 | 3.4095 mL | 17.0474 mL | 34.0948 mL |
| 5 mM | 681.9 μL | 3.4095 mL | 6.819 mL |
| 10 mM | 340.9 μL | 1.7047 mL | 3.4095 mL |
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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.
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Quality Control & SDS
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- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 37 reference(s) in Google Scholar.)