ISA-2011B
Based on 21 publication(s) in Google Scholar
ISA-2011B is a PIP5K1α inhibitor with promising anticancer effects .
For research use only. We do not sell to patients.
- Purity: 99.85%
- CAS No.: 1395347-24-6
- Formula: C22H18ClN3O4
- Molecular Weight:423.85
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocol
- Purity & Documentation
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) ISA-2011B
More- Nat Commun. 2025 Oct 15;16(1):9160. [Abstract]
- Adv Sci (Weinh). 2026 Jun;13(34):e01083. [Abstract]
- Adv Sci (Weinh). 2025 May 23:e04372. [Abstract]
- Cell Discov. 2024 Nov 5;10(1):112. [Abstract]
- Sci Adv. 2022 Jul 22;8(29):eabn1440. [Abstract]
- Sci Adv. 2019 Mar 27;5(3):eaat4872. [Abstract]
- J Hazard Mater. 2025 Jun 15:490:137792. [Abstract]
- J Allergy Clin Immunol. 2025 May;155(5):1607-1622. [Abstract]
- Biomed Pharmacother. 2024 Jun 4:176:116826. [Abstract]
- Cell Rep. 2023 Jan 31;42(1):111905. [Abstract]
- Int Immunopharmacol. 2026 Aug 1:182:116808. [Abstract]
- Molecules. 2024 Jun 1;29(11):2602. [Abstract]
- FEBS J. 2020 Jul;287(14):3042-3064. [Abstract]
- J Cell Mol Med. 2018 Sep;22(9):4117-4129. [Abstract]
- Cell Signal. 2022 Dec:100:110475. [Abstract]
- Bioorg Med Chem. 2024 May 1:105:117727. [Abstract]
- Biochem Biophys Res Commun. 2024 Aug 29:734:150619. [Abstract]
- bioRxiv. 2025 January 29.
- bioRxiv. 2024 June 17.
- bioRxiv. 2023 Feb 23.
- Patent. US20220062379A1.
Customer Validation & Images
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Cell Imaging/Staining
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Cell Proliferation/Viability Assay
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In Vivo Efficacy Study
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Histological Imaging/Staining
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Bio/Physico-chemical Assay
Biological Activity
The proliferation rate of PC-3 cells after treatment with ISA-2011B at 10, 20, and 50 μM is significantly reduced to 58.77%, 48.65%, and 21.62% of vehicle-treated controls, respectively. ISA-2011B exhibits the highest binding affinity to PIP5K1α, and to MAP/microtubule affinity-regulating kinase 1 and 4 (MARK1 and MARK4) across 460 kinases. ISA-2011B treatment inhibits PIP5K1α expression by 78.6% in PC-3 cells[1]. ISA-2011B leads to a remarkable reduction in AR-V7 and CDK1 in both nucleus and cytoplasm of 22Rv1 cells. ISA-2011B treatment also abolishes AR expression in the nucleus, without depleting the cytoplasmic AR[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1395347-24-6
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Appearance Solid
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Molecular Weight 423.85
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Formula C22H18ClN3O4
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Color White to off-white
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SMILES
O=C(N1[C@H](C2=CNC3=C2C=C(Cl)C=C3)C4=C(C=C5C(OCO5)=C4)C[C@]16[H])CN(C)C6=O
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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 2 years -20°C 1 year
Publications (21)
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Journal Impact Factor
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Most Recent
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Nat Commun
The formation of the 'footprint of death' as a mechanism for generating large substrate-bound extracellular vesicles that mark the site of cell death. [Abstract]2025 Oct 15;16(1):9160. PMID: 41093830
ISA-2011B purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Oct 15;16(1):9160. [Abstract]
Confocal laser scanning microscopy (CLSM) imaging of apoptotic MEFs treated with a BH3-mimetic cocktail (5 μM ABТ-737, 10 µM S63845) with and without migrasome inhibitors SMS2-IN-1 (30 uM) and, ISA-2011B (20 µM). MEFs were stained with SiR-actin, A5-FITC, and Hoechst 33342, to visualise F-actin, the nucleus, and exposed phosphatidylserine, respectively.
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Adv Sci (Weinh)
Cell Cycle Control of Nuclear Metabolism Couples Phosphatidylinositol Signaling to Histone Methylation. [Abstract]2026 Jun;13(34):e01083. PMID: 42011901 -
Adv Sci (Weinh)
PIP5K1A Suppresses Ferroptosis and Induces Sorafenib Resistance by Stabilizing NRF2 in Hepatocellular Carcinoma. [Abstract]2025 May 23:e04372. PMID: 40405713
ISA-2011B purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2025 May 23:e04372. [Abstract]
HCC cells (PLC, Hep3B, 97L, 97H, LM3, and SK‐HEP‐1) were treated with increasing doses of ISA-2011B (6.25, 12.5, 25, 50, and 100 µM) for 24 h, and the cell viability was measured by CCK8 assay (n = 3). IC50 values of each cell line are summarized in the top‐right corner.
ISA-2011B purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2025 May 23:e04372. [Abstract]
Representative image of subcutaneous xenografts models inoculated with SK-Hep-1 cells. Seven days post-inoculation, mice received either control or ISA-2011B (40 mg/kg) through injection intraperitoneally once every other day for 14 days (n=6).
ISA-2011B purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2025 May 23:e04372. [Abstract]
Representative H&E staining of heart, kidney and lung tissues form all treatment groups. The results showed that no obvious toxicity was observed in the major organs (liver, lung or kidney) of mice treated with ISA-2011B (40 mg/kg; i.p.; once every other day for 14 days). Scale bar: 200 μm.
ISA-2011B purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2025 May 23:e04372. [Abstract]
Serum levels of ALT were detected in all treatment groups. The results showed that serum liver function indicators remained unchanged in mice treated with ISA-2011B (40 mg/kg;i.p.; once every other day for 14 days).
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Cell Discov
2024 Nov 5;10(1):112. PMID: 39500876 -
Sci Adv
2022 Jul 22;8(29):eabn1440. PMID: 35857835 -
Sci Adv
2019 Mar 27;5(3):eaat4872. PMID: 30944849 -
J Hazard Mater
2025 Jun 15:490:137792. PMID: 40048781 -
J Allergy Clin Immunol
Allergen-induced activation of epithelial P2Y2 receptors promotes ATP exocytosis and type 2 immunity in airways. [Abstract]2025 May;155(5):1607-1622. PMID: 39863058 -
Biomed Pharmacother
Rupatadine inhibits colorectal cancer cell proliferation through the PIP5K1A/Akt/CDK2 pathway. [Abstract]2024 Jun 4:176:116826. PMID: 38838507 -
Cell Rep
Tryptophan-dependent and -independent secretions of tryptophanyl- tRNA synthetase mediate innate inflammatory responses. [Abstract]2023 Jan 31;42(1):111905. PMID: 36640342 -
Int Immunopharmacol
IITZ01 attenuates fructose aggravated ulcerative colitis via prevention of macrophage activation and decrease in cytokine release via inhibition of PIP5 kinase. [Abstract]2026 Aug 1:182:116808. PMID: 42140165 -
Molecules
Signal Transduction of Transient Receptor Potential TRPM8 Channels: Role of PIP5K, Gq-Proteins, and c-Jun. [Abstract]2024 Jun 1;29(11):2602. PMID: 38893478 -
FEBS J
Development of an in vitro screening assay for PIP5K1α lipid kinase and identification of potent inhibitors. [Abstract]2020 Jul;287(14):3042-3064. PMID: 31876381 -
J Cell Mol Med
NEDD4-induced degradative ubiquitination of phosphatidylinositol 4-phosphate 5-kinase α and its implication in breast cancer cell proliferation. [Abstract]2018 Sep;22(9):4117-4129. PMID: 29851245
ISA-2011B purchased from MedChemExpress. Usage Cited in: J Cell Mol Med. 2018 Sep;22(9):4117-4129. [Abstract]
Effect of ISA-2011B or its gene knockout on cancer cell proliferation. Colony formation assays are performed in SKBR3 cells treated with ISA-2011B (20 μM) or DMSO as a control.
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Cell Signal
2022 Dec:100:110475. PMID: 36150420 -
Bioorg Med Chem
2024 May 1:105:117727. PMID: 38669736 -
Biochem Biophys Res Commun
Polystyrene nanoplastics enhance poxvirus preference for migrasome-mediated transmission. [Abstract]2024 Aug 29:734:150619. PMID: 39232458 -
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Solvent & Solubility
DMSO : 100 mg/mL (235.93 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.90 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (5.90 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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.
Add each solvent one by one: 0.5% CMC-Na/saline water
Solubility: 4 mg/mL (9.44 mM); Suspended solution; Need ultrasonic
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.
Protocol
Cells are grown in phenol red-free RPMI-1640 medium 24 hours and then are treated with drugs alone or in combination for 24 hours or 48 hours. MDV3100 at 5 μM or ISA-2011B at 20 μM or 50 μM final concentrations or solvent DMSO 1% is used. For treatment of 22Rv1 cells with MG132, a proteasome inhibitor, cells are treated with MG132 at 1 μM. For combination treatment of MG132 and ISA-2011B, cells are pre-treated with MG132 for 30 min at 1 μM prior to treatment of ISA-2011B[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Mice: BALB/c nude mice aged 8 to 12 wk are used in the experiments. Tumor cells are implanted into the mice. Tumor xenografts are treated with vehicle (control), RP-56976 (10 mg/kg), ISA-2011B (40 mg/kg), and RP-56976 (10 mg/kg) in combination with ISA-2011B (40 mg/kg) every second day[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (286 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. Semenas J, et al. The role of PI3K/AKT-related PIP5K1α and the discovery of its selective inhibitor for treatment of advanced prostate cancer. Proc Natl Acad Sci U S A. 2014 Sep 2;111(35):E3689-98. [Content Brief]
[2]. Sarwar M, et al. Targeted suppression of AR-V7 using PIP5K1α inhibitor overcomes MDV3100 resistance in prostate cancer cells. Oncotarget. 2016 Sep 27;7(39):63065-63081. [Content Brief]
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.3593 mL | 11.7966 mL | 23.5933 mL | 58.9831 mL |
| 5 mM | 0.4719 mL | 2.3593 mL | 4.7187 mL | 11.7966 mL | |
| 10 mM | 0.2359 mL | 1.1797 mL | 2.3593 mL | 5.8983 mL | |
| 15 mM | 0.1573 mL | 0.7864 mL | 1.5729 mL | 3.9322 mL | |
| 20 mM | 0.1180 mL | 0.5898 mL | 1.1797 mL | 2.9492 mL | |
| 25 mM | 0.0944 mL | 0.4719 mL | 0.9437 mL | 2.3593 mL | |
| 30 mM | 0.0786 mL | 0.3932 mL | 0.7864 mL | 1.9661 mL | |
| 40 mM | 0.0590 mL | 0.2949 mL | 0.5898 mL | 1.4746 mL | |
| 50 mM | 0.0472 mL | 0.2359 mL | 0.4719 mL | 1.1797 mL | |
| 60 mM | 0.0393 mL | 0.1966 mL | 0.3932 mL | 0.9831 mL | |
| 80 mM | 0.0295 mL | 0.1475 mL | 0.2949 mL | 0.7373 mL | |
| 100 mM | 0.0236 mL | 0.1180 mL | 0.2359 mL | 0.5898 mL |
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