AC-4-130
Based on 8 publication(s) in Google Scholar
AC-4-130 is a potent STAT5 SH2 domain inhibitor. AC-4-130 directly binds to STAT5 and disrupts STAT5 activation, dimerization, nuclear translocation, and STAT5-dependent gene transcription. AC-4-130 induces cell cycle arrest and apoptosis in FLT3-ITD-driven leukemic cells. AC-4-130 has anti-cancer activity and can efficiently block pathological levels of STAT5 activity in acute myeloid leukemia (AML).
For research use only. We do not sell to patients.
- Purity : 99.93%
- CAS No.: 1834571-82-2
- Formula: C37H36ClF5N2O5S
- Molecular Weight:751.20
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocols
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) AC-4-130
More- Nat Cancer. 2023 Aug;4(8):1193-1209. [Abstract]
- Cell Stem Cell. 2026 May 7;33(5):800-819.e9. [Abstract]
- Nat Chem Biol. 2025 Sep 1. [Abstract]
- Pharmacol Res. 2024 Dec:210:107499. [Abstract]
- Cell Rep. 2026 Jun 4;45(6):117519. [Abstract]
- PLoS Pathog. 2022 Oct 25;18(10):e1010913. [Abstract]
- Iran J Immunol. 2024 Sep 25;21(3). [Abstract]
- Research Square Print. 2022 Aug.
Customer Validation & Images
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Others
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Histological Imaging/Staining
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Others
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WB
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RT-PCR
Biological Activity
Description
IC50 & Target
[1]|
STAT5 |
In Vitro
AC-4-130 (0.1-100 μM; 72 hours) leads to a significant increase in apoptosis in a dose-dependent and time-dependent manner in MV4-11 or MOLM-13 cells[1].
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AC-4-130 (2, 5 μM; 72 hours) induces cell cycle arrest with an increase in G0/G1 arrested cells and a concomitant reduction in cells in S or G2/M[1].
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AC-4-130 (0.5-2; 24 hours) reveals reduced pY-STAT5 levels both in the cytoplasm and nucleus[1].
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AC-4-130-mediated STAT5 inhibition efficiently blocks the proliferation and clonogenic growth of primary human AML cells, while healthy CD34+ cells are less sensitive[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
Chemical Information
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CAS No. 1834571-82-2
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Appearance Solid
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Molecular Weight 751.20
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Formula C37H36ClF5N2O5S
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Color Off-white to brown
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SMILES
FC1=C(C(F)=C(C(F)=C1F)S(=O)(N(CC2=CC=C(C=C2)Cl)CC(N(C3=CC=C(C=C3)C(O)=O)CC4=CC(C(C)(C)C)=CC(C(C)(C)C)=C4)=O)=O)F
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (8)
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Journal Impact Factor
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Most Recent
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Nat Cancer
Different niches for stem cells carrying the same oncogenic driver affect pathogenesis and therapy response in myeloproliferative neoplasms. [Abstract]2023 Aug;4(8):1193-1209. PMID: 37550517
AC-4-130 purchased from MedChemExpress. Usage Cited in: Nat Cancer. 2023 Aug;4(8):1193-1209. [Abstract]
HSCs were sorted from 10–13-week-old WT mice and cultured for 16 h with STAT1 (NSC 118218 phosphate, 10 µM), STAT3 (BP-1-102, 5 µM) or STAT5 (AC-4-130, 5 µM) inhibitor, or vehicle.
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Cell Stem Cell
2026 May 7;33(5):800-819.e9. PMID: 42030946 -
Nat Chem Biol
Real-time visualization of STAT activation in live cells using genetically encoded biosensors. [Abstract]2025 Sep 1. PMID: 40890507
AC-4-130 purchased from MedChemExpress. Usage Cited in: Nat Chem Biol. 2025 Sep 1. [Abstract]
HEK-BlueTM IL-2 cells were transfected with STATeLight5A and incubated with indicated STAT5 inhibitors (10 μM AC-4-130) for 2 hours. Subsequently, cells were stimulated with 3.5 µg of IL-2 for 30 min. mNG fluorescence lifetime was measured.
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Pharmacol Res
ARID1A is a coactivator of STAT5 that contributes to CD8+ T cell dysfunction and anti-PD-1 resistance in gastric cancer. [Abstract]2024 Dec:210:107499. PMID: 39549895
AC-4-130 purchased from MedChemExpress. Usage Cited in: Pharmacol Res. 2024 Dec:210:107499. [Abstract]
Ten⁶ MFC cells were subcutaneously injected into 615 mice (n=6 per group), followed by intraperitoneal injection of AC-4-130 (25 mg/kg), anti-PD-1 (10 mg/kg), or AC-4-130 + anti-mPD-1, for a total of 5 treatment cycles, each lasting 21 days (AC-4-130 administered daily, anti-PD-1 administered every 4 days). Ki67 staining was performed on the subcutaneous gastric cancer model.
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Cell Rep
IL-33/TGF-β/IL-4-induced bone marrow-derived DC9 subset promotes Th9 differentiation and allergic airway inflammation. [Abstract]2026 Jun 4;45(6):117519. PMID: 42247295 -
PLoS Pathog
IL-2-mTORC1 signaling coordinates the STAT1/T-bet axis to ensure Th1 cell differentiation and anti-bacterial immune response in fish. [Abstract]2022 Oct 25;18(10):e1010913. PMID: 36282845
AC-4-130 purchased from MedChemExpress. Usage Cited in: PLoS Pathog. 2022 Oct 25;18(10):e1010913. [Abstract]
Splenic leukocytes were stimulated with recombinant IL-2 for 12 hours in the presence of the STAT5 inhibitor AC-4-130 (5 mM). The expression levels of the molecules were detected by Western blotting.
AC-4-130 purchased from MedChemExpress. Usage Cited in: PLoS Pathog. 2022 Oct 25;18(10):e1010913. [Abstract]
Splenic leukocytes were stimulated with recombinant IL-2 for 12 hours in the presence of the STAT5 inhibitor AC-4-130 (5 mM). The expression levels of the molecules were detected by qPCR.
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Iran J Immunol
2024 Sep 25;21(3). PMID: 39319693 -
Solvent & Solubility
In Vitro:
DMSO : 100 mg/mL (133.12 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : < 0.1 mg/mL (insoluble)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocols
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Cytoplasmic-Nuclear Fractionated Protein Extraction
Cytoplasmic-nuclear fractionated protein extraction separates soluble cytoplasmic proteins from nuclear-enriched proteins by mild plasma-membrane permeabilization, differential centrifugation, washing of nuclei, and extraction of nuclear proteins for downstream immunoblotting or related molecular analysis. The readout is the relative abundance of a protein in cytoplasmic and nuclear fractions, commonly assessed by western blotting together with compartment markers such as tubulin or pyruvate kinase for cytoplasm and lamin, nucleoporin, hnRNP, H2AX, or Lamin B for nuclear fractions.
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Apoptosis
Apoptosis, also called programmed cell death, is generally characterized by distinct morphological characteristics.
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TUNEL staining for apoptotic DNA fragmentation
TUNEL staining detects DNA strand breaks by using terminal deoxynucleotidyl transferase to add labeled nucleotides to exposed 3′-OH DNA termini, generating either microscopic staining in fixed cells or tissue sections, or fluorescence/cytometric signal in cell suspensions. TUNEL positivity reflects DNA fragmentation but should not be interpreted alone as definitive apoptosis, because TUNEL can also label necrotic, autolytic, mechanically damaged, or DNA-repair-associated DNA breaks.
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Flow cytometric DNA-content cell-cycle staining
Flow cytometric DNA-content cell-cycle staining measures the fluorescence intensity of DNA-bound fluorochromes in single cells or nuclei to estimate DNA content distributions, allowing assignment of populations to G0/G1, S, and G2/M phases by DNA histogram deconvolution. Propidium iodide (PI) intercalates into DNA, and PI fluorescence is proportional to cellular DNA content when staining is performed under conditions that make DNA accessible and minimize non-DNA signal. Cells with G2/M DNA content are expected to show approximately twice the fluorescence intensity of G0/G1 cells, while S-phase cells occupy intermediate fluorescence values. PI-based DNA-content analysis can also detect cells with fractional DNA content, often reported as sub-G1, when DNA fragmentation and extraction during staining reduce retained DNA signal in apoptotic cells. DAPI is an alternative DNA fluorochrome for univariate DNA-content analysis, while bivariate approaches combining DNA content with proliferation
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Annexin V plus membrane-impermeant dye apoptosis staining
Annexin V-based apoptosis assays rely on the detection of phosphatidylserine (PS) externalization from the inner leaflet of the plasma membrane to the outer leaflet, an early biochemical hallmark of apoptosis. Fluorescently labeled Annexin V binds PS in a calcium-dependent manner, enabling identification of early apoptotic cells by flow cytometry or fluorescence microscopy. When combined with a membrane-impermeant DNA-binding dye (e. g. , propidium iodide), this approach allows discrimination between viable (Annexin V−/dye−), early apoptotic (Annexin V+/dye−), and late apoptotic or necrotic (Annexin V+/dye+) cell populations by assessing membrane integrity and PS exposure.
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BrdU Incorporation Assay
Bromodeoxyuridine (BrdU) incorporation assay is based on the principle that BrdU, a thymidine analog, is incorporated into newly synthesized DNA during the S phase of the cell cycle, thereby serving as a marker of DNA replication and cellular proliferation. Incorporated BrdU can be detected using anti-BrdU antibodies following DNA denaturation, enabling visualization or quantification of proliferating cells through immunochemical detection methods such as immunofluorescence or immunohistochemistry.
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Apoptosis Solutions
Apoptosis is a regulated, generally non-lytic cell-death pathway that removes unwanted, damaged, infected, or abnormal cells through coordinated morphological changes, caspase activation, DNA fragmentation, and membrane remodeling. The intrinsic apoptosis pathway is controlled mainly by mitochondrial outer membrane permeabilization, BCL-2 family proteins, cytochrome c release, apoptosome formation, caspase-9 activation, and downstream executioner caspase-3/7 activation. The extrinsic apoptosis pathway is initiated by death receptors such as Fas, TNFR, and TRAIL receptors, which recruit adaptor proteins and activate caspase-8 before engaging executioner caspases or mitochondrial amplification through BID cleavage. Apoptosis is linked to many phenotypes, including cancer cell killing, tissue homeostasis, immune regulation, neurodegeneration, infection response, and treatment-induced cytotoxicity; unresolved questions include how apoptosis interacts with necroptosis, pyroptosis, ferroptos
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Protocol for Cell Cycle
Cell-cycle analysis by flow cytometry measures DNA content in single cells to estimate the fraction of cells in G0/G1, S, and G2/M phases. Propidium iodide intercalates into DNA, and after RNA removal with RNase, fluorescence intensity reflects cellular DNA content: 2N cells are assigned to G0/G1, cells between 2N and 4N to S phase, and 4N cells to G2/M. DNA-content analysis alone cannot reliably separate G0 from G1 or G2 from M. Ki-67 can distinguish quiescent G0 cells from cycling cells, EdU or BrdU incorporation marks active DNA synthesis in S phase, and phospho-histone H3 staining identifies mitotic cells within the 4N population.
Purity & Documentation
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Data Sheet (278 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 1.3312 mL | 6.6560 mL | 13.3120 mL | 33.2801 mL |
| 5 mM | 0.2662 mL | 1.3312 mL | 2.6624 mL | 6.6560 mL | |
| 10 mM | 0.1331 mL | 0.6656 mL | 1.3312 mL | 3.3280 mL | |
| 15 mM | 0.0887 mL | 0.4437 mL | 0.8875 mL | 2.2187 mL | |
| 20 mM | 0.0666 mL | 0.3328 mL | 0.6656 mL | 1.6640 mL | |
| 25 mM | 0.0532 mL | 0.2662 mL | 0.5325 mL | 1.3312 mL | |
| 30 mM | 0.0444 mL | 0.2219 mL | 0.4437 mL | 1.1093 mL | |
| 40 mM | 0.0333 mL | 0.1664 mL | 0.3328 mL | 0.8320 mL | |
| 50 mM | 0.0266 mL | 0.1331 mL | 0.2662 mL | 0.6656 mL | |
| 60 mM | 0.0222 mL | 0.1109 mL | 0.2219 mL | 0.5547 mL | |
| 80 mM | 0.0166 mL | 0.0832 mL | 0.1664 mL | 0.4160 mL | |
| 100 mM | 0.0133 mL | 0.0666 mL | 0.1331 mL | 0.3328 mL |
AC-4-130 Related Classifications
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