2. Others PROTAC
  3. Drug Isomer Molecular Glues
  4. (Rac)-TNG961

(Rac)-TNG961 is the rac isomer of TNG961 (HY-183115). TNG961 is a selective and orally active CRBN-mediated HBS1L molecular glue degrader. TNG961 induces formation of an HBS1L-TNG961-CRBN ternary complex, leading to potent degradation of HBS1L and secondary destabilization of its binding partner PELO. TNG961 can reduce HBS1L protein levels, thereby disrupting the PELO region involved in ribosome rescue. TNG961 can be used for the study of FOCAD-deficient cancers, such as pancreatic cancer.

For research use only. We do not sell to patients.

(Rac)-TNG961

(Rac)-TNG961 Chemical Structure

Size Stock
50 mg   Get quote  
100 mg   Get quote  
250 mg   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Other Forms of (Rac)-TNG961:

(Rac)-TNG961 Related Antibodies

Top Publications Citing Use of Products

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

(Rac)-TNG961 is the rac isomer of TNG961 (HY-183115). TNG961 is a selective and orally active CRBN-mediated HBS1L molecular glue degrader. TNG961 induces formation of an HBS1L-TNG961-CRBN ternary complex, leading to potent degradation of HBS1L and secondary destabilization of its binding partner PELO. TNG961 can reduce HBS1L protein levels, thereby disrupting the PELO region involved in ribosome rescue. TNG961 can be used for the study of FOCAD-deficient cancers, such as pancreatic cancer[1].

In Vitro

In vitro, TNG961 leads to a dose-dependent decrease in HBS1L protein levels, which in turn destabilizes the portion of PELO involved in ribosome rescue. TNG961 displays proteome-wide selectivity for HBS1L, with no change in SALL4 protein level as determined by western blot. TNG961-induced HBS1L degradation and PELO destabilization can both be rescued by inactivation of CRBN confirming mechanism[1].
In engineered HiBiT knock-in cells, treatment with TNG961 induces maximal HBS1L degradation within 4 hours, without affecting GSPT1 protein levels[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

(Rac)-TNG961 Related Antibodies
In Vivo

TNG961 (Oral administration) induces dose-dependent degradation of HBS1L and subsequent destabilization of PELO protein in FOCAD-deleted xenograft models, resulting in tumor stasis or regression across multiple lineages[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Molecular Weight

539.57

Formula

C28H24F3N3O3S
SMILES

O=C(NC1=O)CCC1C(C=C2)=CC3=C2C(NC(NC(C)(C)C4=CC(C=CC(C(F)(F)F)=C5)=C5S4)=O)=CC=C3
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (185.33 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.8533 mL 9.2666 mL 18.5333 mL
5 mM 0.3707 mL 1.8533 mL 3.7067 mL
View the Complete Stock Solution Preparation Table

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
References

Complete Stock Solution Preparation Table

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.8533 mL 9.2666 mL 18.5333 mL 46.3332 mL
5 mM 0.3707 mL 1.8533 mL 3.7067 mL 9.2666 mL
10 mM 0.1853 mL 0.9267 mL 1.8533 mL 4.6333 mL
15 mM 0.1236 mL 0.6178 mL 1.2356 mL 3.0889 mL
20 mM 0.0927 mL 0.4633 mL 0.9267 mL 2.3167 mL
25 mM 0.0741 mL 0.3707 mL 0.7413 mL 1.8533 mL
30 mM 0.0618 mL 0.3089 mL 0.6178 mL 1.5444 mL
40 mM 0.0463 mL 0.2317 mL 0.4633 mL 1.1583 mL
50 mM 0.0371 mL 0.1853 mL 0.3707 mL 0.9267 mL
60 mM 0.0309 mL 0.1544 mL 0.3089 mL 0.7722 mL
80 mM 0.0232 mL 0.1158 mL 0.2317 mL 0.5792 mL
100 mM 0.0185 mL 0.0927 mL 0.1853 mL 0.4633 mL
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.

(Rac)-TNG961 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

(Rac)-TNG961Drug IsomerMolecular GluesInhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

  

Requested Quantity *

Applicant Name *

 

Salutation

Email Address *

 

Phone Number *

Department

 

Organization Name *

City

State

Country or Region *

      

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
(Rac)-TNG961
Cat. No.:
HY-183115A
Quantity:
MCE Japan Authorized Agent:

Customer Review

Thank You for Your Feedback!

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

Product Name

  

Lot #

Applicant Name *

 

Email Address *

Phone Number

 

Department *

Organization Name *

 

Country or Region *

Remarks

SAFETY DATA SHEET (SDS)

Request for HNMR Report

We have received your request and will respond to you as soon as possible.