Home Ubiquitin SUMO inhibitor Subasumstat (TAK-981) For research use only.

Subasumstat (TAK-981)

Subasumstat (TAK-981) is a novel, selective inhibitor of the SUMOylation enzymatic cascade with potential immune-activating and antineoplastic activities.

Subasumstat (TAK-981) Chemical Structure

Subasumstat (TAK-981) Chemical Structure

CAS No. 1858276-04-6

Purity & Quality Control

Subasumstat (TAK-981) Related Products

Biological Activity

Description Subasumstat (TAK-981) is a novel, selective inhibitor of the SUMOylation enzymatic cascade with potential immune-activating and antineoplastic activities.
Targets
SUMOylation enzymatic cascade [1]
In vitro
In vitro

In both mouse bone-marrow and human peripheral blood mononuclear cell derived dendritic cells (DCs), TAK-981 treatment ex vivo induced markers of activation and maturation including CD40, CD80 and CD86, as well as increased secretion of inflammatory cytokines like IP-10, MCP1, MIP-1α, MIP1β, IFNα and IFNβ.[1]
Cell Research Cell lines mouse bone-marrow and human peripheral blood mononuclear cell derived dendritic cells (DCs)
Concentrations --
Incubation Time --
Method

--
In Vivo
In vivo

In vivo, a single sub-cutaneous injection of TAK-981 in naïve Balb/c mice at the brachial lymph nodes induced activation of DCs, measured as significant increases in CD40 and CD86 expression.[1] TAK-981 demonstrates antitumor activity, including complete regression (CR) of some tumors, in immune-competent BALB/c mice bearing syngeneic A20 lymphoma tumors.[2]
Animal Research Animal Models immune-competent BALB/c mice
Dosages 7.5 mg/kg
Administration IV
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT04381650 Active not recruiting
Advanced or Metastatic Solid Tumors
Takeda|Takeda Development Center Americas Inc.
 August 17 2020 Phase 1|Phase 2
NCT04074330 Terminated
Lymphoma Non-Hodgkin
Takeda
 October 15 2019 Phase 1|Phase 2
NCT03648372 Terminated
Neoplasms|Lymphoma|Hematologic Neoplasms
Takeda
 October 1 2018 Phase 1|Phase 2

Chemical Information & Solubility

Molecular Weight 578.10 Formula

C25H28ClN5O5S2
CAS No. 1858276-04-6 SDF --
Smiles CC1=C(C=C(S1)C(=O)C2=CN=CN=C2NC3CC(C(C3)O)COS(=O)(=O)N)C4C5=C(CCN4)C=CC(=C5)Cl
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 100 mg/mL ( (172.98 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
Batch:

Add solvents to the product individually and in order.


In vivo Formulation Calculator

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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 ddH2O, 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.

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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