Subasumstat
Based on 34 publication(s) in Google Scholar
Subasumstat (TAK-981) is a first in class and selective inhibitor of the SUMOylation enzymatic cascade, with potential immune-activating and antineoplastic activities.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Pureté: 98.38%
- CAS No.: 1858276-04-6
- Formule: C25H28ClN5O5S2
- Masse moléculaire:578.10
-
Stockage:Powder -20°C, 3 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]
-
Activité biologique
-
Chemical Information
-
Solvant et solubilité
- Pureté et documentation
- Références
-
Help & FAQs
-
Immunology/Inflammation Compound Library
HY-L007
-
Metabolism/Protease Compound Library
HY-L012
-
Anti-Cancer Compound Library
HY-L025
-
Clinical Compound Library
HY-L026
-
Drug Repurposing Compound Library
HY-L035
-
Oxygen Sensing Compound Library
HY-L045
-
Ubiquitination Compound Library
HY-L050
-
Chemical Probe Library
HY-L063
-
Anti-Liver Cancer Compound Library
HY-L101
-
Heterocyclic Compound Library
HY-L138
-
Mitochondrial Protection Compound Library
HY-L144
-
Metabolic Enzyme Compound Library
HY-L146
-
Highly Selective Inhibitors Library
HY-L158
-
Mitophagy Compound Library
HY-L180
-
Bioactive Compound Library Max
HY-L181
-
MCE Bioactive Compound Library
HY-L001V
-
Drug Repurposing Compound Library Plus
HY-L035P
-
Clinical Compound Library Plus
HY-L026P
-
Bioactive Compound Library
HY-L001
-
Amino Acid Metabolism Compound Library
HY-L189
-
Protein Kinase Compound Library
HY-L196
-
Cell Proliferation Compound Library
HY-L201
-
High-Throughput Bioactive Compound Library
HY-L205
-
Posttranslational Modification Library
HY-L226
Publications Citing Use of MedChemExpress (MCE) Subasumstat
More- Nat Microbiol. 2022 Dec;7(12):2101-2113. [Abstract]
- Nat Cell Biol. 2026 Mar 13. [Abstract]
- Nat Commun. 2026 Feb 12;17(1):1214. [Abstract]
- J Clin Invest. 2022 May 2;132(9):e152383. [Abstract]
- Gut Microbes. 2025 Dec;17(1):2446392. [Abstract]
- Cell Death Dis. 2023 Feb 21;14(2):147. [Abstract]
- EMBO J. 2025 Aug 13. [Abstract]
- EMBO Mol Med. 2023 Sep 11;15(9):e16431. [Abstract]
- Cell Rep. 2026 Mar 13;45(3):117102. [Abstract]
- Antioxidants (Basel). 2026 Apr 11;15(4):478. [Abstract]
- Int J Oncol. 2024 Oct;65(4):98. [Abstract]
- Cell Oncol (Dordr). 2024 Apr;47(2):513-532. [Abstract]
- Eur J Cell Biol. 2025 Feb 20;104(2):151480. [Abstract]
- iScience. 2024 Oct 11;27(11):111133. [Abstract]
- J Biol Chem. 2025 Oct 8:110807. [Abstract]
- J Biol Chem. 2023 Nov;299(11):105280. [Abstract]
- Chem Res Toxicol. 2025 Apr 17. [Abstract]
- J Virol. 2024 Dec 5:e0122424. [Abstract]
- Mol Cell Biochem. 2025 Jun 23. [Abstract]
- J Cell Sci. 2023 Aug 1;136(15):jcs261119. [Abstract]
- Adipocyte. 2025 Dec;14(1):2474107. [Abstract]
- J Gen Physiol. 2025 Nov 3;157(6):e202513837. [Abstract]
- Neuroscience. 2025 Jan 29:568:433-443. [Abstract]
- Biochem Biophys Res Commun. 2025 May 12:770:152000. [Abstract]
- bioRxiv. 2026 Mar 13.
- bioRxiv. 2026 Jan 5.
- medRxiv. 2025 Aug 28:2025.08.25.25333715. [Abstract]
- Temple University. 2025.
- bioRxiv. 2025 April 29.
- bioRxiv. 2025 March 26.
- bioRxiv. 2025 March 25.
- bioRxiv. 2025 January 19.
- bioRxiv. 2024 November 23.
- Res Sq. 2024 Apr 2:rs.3.rs-4201913. [Abstract]
Customer Validation & Images
-
WB
-
In Vivo Efficacy Study
-
Cell Migration/Invasion Assay
-
Cell Proliferation/Viability Assay
-
RT-PCR
Activité biologique
SUMOylation[1].
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| HCT-116 | EC50 |
0.063 μM
Compound: TAK-981
|
Cytotoxicity against human HCT116 cells assessed as reduction in cell viability after 72 hrs by CellTiter-Glo luminescent assay
Cytotoxicity against human HCT116 cells assessed as reduction in cell viability after 72 hrs by CellTiter-Glo luminescent assay
|
[PMID: 33631934] |
| OCI-Ly10 | EC50 |
0.004 μM
Compound: TAK-981
|
Cytotoxicity against human OCI-LY10 cells assessed as reduction in cell viability after 72 hrs by CellTiter-Glo luminescent assay
Cytotoxicity against human OCI-LY10 cells assessed as reduction in cell viability after 72 hrs by CellTiter-Glo luminescent assay
|
[PMID: 33631934] |
Subasumstat (TAK-981) is able to increase the production of type 1 IFN, thereby increasing type 1 IFN-mediated signaling, activating innate effector cells and enhancing the antitumor innate immune responses[1].
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.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
-
CAS No. 1858276-04-6
-
Appearance Solid
-
Masse moléculaire 578.10
-
Formule C25H28ClN5O5S2
-
Color White to light yellow
-
SMILES
O=S(OC[C@@H]1[C@@H](O)C[C@H](NC2=NC=NC=C2C(C3=CC([C@@H]4NCCC5=C4C=C(Cl)C=C5)=C(C)S3)=O)C1)(N)=O
-
Synonyms
TAK-981
-
Livraison
Room temperature in continental US; may vary elsewhere.
-
Stockage
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Publications (34)
-
Journal Impact Factor
-
Most Recent
-
Nat Microbiol
2022 Dec;7(12):2101-2113. PMID: 36376394
Subasumstat purchased from MedChemExpress. Usage Cited in: Nat Microbiol. 2022 Dec;7(12):2101-2113. [Abstract]
Subasumstat (TAK-981) boosts NLuc expression from unintegrated HIV-1 DNA, reaching a plateau at ~75 nM. Subasumstat is added to CEM-SS Cas9 and ΔSMC5 cells infected with NL-NLuc at 0, 5, 15, 30, 75, 150, 500 and 1,000 nM concentrations, and the cells are collected for an NLuc assay after 2 dpi.
-
Nat Cell Biol
An SP110-SP100 axis is a critical regulator of promyelocytic leukaemia body dynamics and mitotic fidelity. [Abstract]2026 Mar 13. PMID: 41826696 -
Nat Commun
Human iPSC-based Modeling of Pulmonary Fibrosis Reveals p300/CBP Inhibition Suppresses Alveolar Transitional Cell State. [Abstract]2026 Feb 12;17(1):1214. PMID: 41680175 -
J Clin Invest
Activated SUMOylation restricts MHC class I antigen presentation to confer immune evasion in cancer. [Abstract]2022 May 2;132(9):e152383. PMID: 35499080 -
Gut Microbes
2025 Dec;17(1):2446392. PMID: 39819277 -
Cell Death Dis
Glioblastoma upregulates SUMOylation of hnRNP A2/B1 to eliminate the tumor suppressor miR-204-3p, accelerating angiogenesis under hypoxia. [Abstract]2023 Feb 21;14(2):147. PMID: 36810326
Subasumstat purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2023 Feb 21;14(2):147. [Abstract]
Subasumstat (TAK-981; 25 mg/kg; every 3 days for 21 days) suppresses the growth of glioblastoma in mice.
-
EMBO J
Targeting SUMO2 reverses aberrant epigenetic rewiring driven by SS18::SSX fusion oncoproteins and impairs sarcomagenesis. [Abstract]2025 Aug 13. PMID: 40804185 -
EMBO Mol Med
Actionable loss of SLF2 drives B-cell lymphomagenesis and impairs the DNA damage response. [Abstract]2023 Sep 11;15(9):e16431. PMID: 37485814 -
Cell Rep
TCR-NF-κB signaling activates the SENP1-NR4A1 axis to fine-tune effector activation of CD8+ T cells. [Abstract]2026 Mar 13;45(3):117102. PMID: 41831233 -
Antioxidants (Basel)
SUMOylation Inhibitor TAK-981 Alleviates Hallmark Features of Preeclampsia Related to High Glucocorticoid Exposure by Inhibiting Placental Oxidative Stress in Rats. [Abstract]2026 Apr 11;15(4):478. PMID: 42072120 -
Int J Oncol
Transcription factor E2F4 facilitates SUMOylation to promote HCC progression through interaction with LIN9. [Abstract]2024 Oct;65(4):98. PMID: 39239750 -
Cell Oncol (Dordr)
SUMOylation inhibitors activate anti-tumor immunity by reshaping the immune microenvironment in a preclinical model of hepatocellular carcinoma. [Abstract]2024 Apr;47(2):513-532. PMID: 38055116 -
Eur J Cell Biol
Transient pharmacological inhibition of SUMOylation during pregnancy induces craniofacial malformations in offspring mice. [Abstract]2025 Feb 20;104(2):151480. PMID: 39985830 -
iScience
Intra-tumoral YAP and TAZ heterogeneity drives collective NSCLC invasion that is targeted by SUMOylation inhibitor TAK-981. [Abstract]2024 Oct 11;27(11):111133. PMID: 39524367
Subasumstat purchased from MedChemExpress. Usage Cited in: iScience. 2024 Oct 11;27(11):111133. [Abstract]
Leader and follower cells treated with indicated doses of TAK-981 for 72 h were evaluated for YAP and TAZ.
Subasumstat purchased from MedChemExpress. Usage Cited in: iScience. 2024 Oct 11;27(11):111133. [Abstract]
Mice were treated with vehicle or 25 mg/kg TAK-981 thrice weekly. Bright-field images of tumors isolated from vehicle- and TAK-981-treated mice were captured.
Subasumstat purchased from MedChemExpress. Usage Cited in: iScience. 2024 Oct 11;27(11):111133. [Abstract]
Spheroids generated with leader cells, follower cells, or mixes of 90% follower cells and 10% leader cells (L:F, 1:9) treated with either DMSO or 250 nM TAK-981 (72 h) were evaluated for invasive area with quantification of invasive area.
-
J Biol Chem
2025 Oct 8:110807. PMID: 41072767 -
J Biol Chem
SUMOylation indirectly suppresses activity of the HIF-1α pathway in intestinal epithelial cells. [Abstract]2023 Nov;299(11):105280. PMID: 37742924 -
Chem Res Toxicol
Nuclear SUMOylation and Proteotoxic Stress Responses to Metals with Different Ligand Preferences. [Abstract]2025 Apr 17. PMID: 40243484 -
J Virol
Analysis of the ubiquitin-modified proteome identifies novel host factors in Kaposi's sarcoma herpesvirus lytic reactivation. [Abstract]2024 Dec 5:e0122424. PMID: 39636148 -
Mol Cell Biochem
Synthetic inhibition of the SUMO pathway by targeting the SAE1 component via TAK-981 compound impairs growth and chemosensitizes embryonal and alveolar rhabdomyosarcoma cell lines. [Abstract]2025 Jun 23. PMID: 40549307 -
J Cell Sci
B cell receptor-induced protein dynamics and the emerging role of SUMOylation revealed by proximity proteomics. [Abstract]2023 Aug 1;136(15):jcs261119. PMID: 37417469 -
Adipocyte
Pharmacological inhibition of SUMOylation with TAK-981 mimics genetic HypoSUMOylation in murine perigonadal white adipose tissue. [Abstract]2025 Dec;14(1):2474107. PMID: 40047287 -
J Gen Physiol
2025 Nov 3;157(6):e202513837. PMID: 41085580 -
Neuroscience
Inhibition of SUMOylation exacerbates neurological dysfunction and delays hematoma clearance after intracerebral hemorrhage in mice. [Abstract]2025 Jan 29:568:433-443. PMID: 39890052 -
Biochem Biophys Res Commun
TAK-981 enhances antitumor activity in ELT3 uterine leiomyoma cells through the modulation of apoptosis, cell cycle arrest, and autophagy. [Abstract]2025 May 12:770:152000. PMID: 40373381 -
-
-
medRxiv
Integration of cell-type resolved spatial proteomics and transcriptomics reveals novel mechanisms in early ovarian cancer. [Abstract]2025 Aug 28:2025.08.25.25333715. PMID: 40909841 -
-
-
-
-
-
-
Res Sq
Regulation of Enhancers by SUMOylation Through TFAP2C Binding and Recruitment of HDAC Complex to the Chromatin. [Abstract]2024 Apr 2:rs.3.rs-4201913. PMID: 38645262
Solvant et solubilité
DMSO : 100 mg/mL (172.98 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, 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)
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: ≥ 5 mg/mL (8.65 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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.
Please enter the basic information of animal experiments:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
-
%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
-
%+
-
+%Tween-80 + +
-
%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.
Pureté et documentation
-
Fiche technique (276 KB)
-
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)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
-
Instruction de manipulation (2659 KB)
Références
[1]. Sumoylation inhibitor TAK-981.
[2]. TAK-981.
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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.7298 mL | 8.6490 mL | 17.2980 mL | 43.2451 mL |
| 5 mM | 0.3460 mL | 1.7298 mL | 3.4596 mL | 8.6490 mL | |
| 10 mM | 0.1730 mL | 0.8649 mL | 1.7298 mL | 4.3245 mL | |
| 15 mM | 0.1153 mL | 0.5766 mL | 1.1532 mL | 2.8830 mL | |
| 20 mM | 0.0865 mL | 0.4325 mL | 0.8649 mL | 2.1623 mL | |
| 25 mM | 0.0692 mL | 0.3460 mL | 0.6919 mL | 1.7298 mL | |
| 30 mM | 0.0577 mL | 0.2883 mL | 0.5766 mL | 1.4415 mL | |
| 40 mM | 0.0432 mL | 0.2162 mL | 0.4325 mL | 1.0811 mL | |
| 50 mM | 0.0346 mL | 0.1730 mL | 0.3460 mL | 0.8649 mL | |
| 60 mM | 0.0288 mL | 0.1442 mL | 0.2883 mL | 0.7208 mL | |
| 80 mM | 0.0216 mL | 0.1081 mL | 0.2162 mL | 0.5406 mL | |
| 100 mM | 0.0173 mL | 0.0865 mL | 0.1730 mL | 0.4325 mL |
Subasumstat Related Classifications
HY-111789 Related Classifications
Powered by Bioz