2. Epigenetics Metabolic Enzyme/Protease
  3. Histone Methyltransferase Aminotransferases (Transaminases) Lactate Dehydrogenase
  4. WQQ-345

WQQ-345 is an orally active BCAT1 inhibitor with an IC50 values of 10.8 mM. WQQ-345 reduces cellular α-KG levels, upregulating H3K27me3 expression, decreasing glycolytic enzyme expression, and impairing glycolysis activity. WQQ-345 reduces colony formation, suppresses growth of BCAT1-high TKI-resistant lung cancer cells. WQQ-345 exerts in vitro and in vivo antitumor activity. WQQ-345 can be used for the research of TKI-resistant non-small cell lung cancer and TKI-resistant lung cancer.

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

WQQ-345

WQQ-345 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.

WQQ-345 Related Antibodies

Top Publications Citing Use of Products

View All Histone Methyltransferase Isoform Specific Products:

View All Isoforms
EZH1 EZH2 DOT1L SMYD2 SMYD3 SUV39H2/KMT1B EHMT2/G9a/KMT1C EHMT1/GLP/KMT1D ASH1L/KMT2H SETDB1/KMT2G SETD2/KMT3A NSD2/MMSET/WHSC1 NSD3/WHSC1L1 SETD7/KMT7 SETD8/KMT5A PRMT1 PRMT3 PRMT4 PRMT5 PRMT6 PRMT7 PRMT8

View All Aminotransferases (Transaminases) Isoform Specific Products:

View All Isoforms
GPT/ALT GOT/AST

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

WQQ-345 is an orally active BCAT1 inhibitor with an IC50 values of 10.8 mM. WQQ-345 reduces cellular α-KG levels, upregulating H3K27me3 expression, decreasing glycolytic enzyme expression, and impairing glycolysis activity. WQQ-345 reduces colony formation, suppresses growth of BCAT1-high TKI-resistant lung cancer cells. WQQ-345 exerts in vitro and in vivo antitumor activity. WQQ-345 can be used for the research of TKI-resistant non-small cell lung cancer and TKI-resistant lung cancer[1][2].

In Vitro

WQQ-345 (2.5-5 mM; 7-10 days) dose-dependently inhibits colony formation of 67R NSCLC cells[1].
WQQ-345 (5-10 mM; 3 days) dose-dependently reduces intracellular α-KG levels, upregulates H3K27me3 protein expression, and downregulates PFKP and LDHA protein expression in 67R NSCLC cells after 3 days of treatment at 5 mM or 10 mM[1].
WQQ-345 (5 mM; 3 days) impairs glycolytic activity (lowered ECAR) in 67R NSCLC cells[1].

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

WQQ-345 Related Antibodies

Cell Proliferation Assay[1]

Cell Line: ASK120067-resistant NCI-H1975 (67R) NSCLC cells
Concentration: 2.5, 5 mM
Incubation Time: 7-10 days
Result: Dose-dependently reduced colony formation of 67R cells, with significant inhibition observed at both 2.5 mM and 5 mM.
Resulted in stronger growth inhibition when co-treated with 1 μM ASK120067 (HY-138751) than either monotherapy.
Lost growth-inhibitory effects in 67R cells with BCAT1 knockdown, confirming on-target activity.

Western Blot Analysis[1]

Cell Line: ASK120067-resistant NCI-H1975 (67R) NSCLC cells
Concentration: 5, 10 mM
Incubation Time: 3 days
Result: Dose-dependently upregulated H3K27me3 protein expression in 67R cells.
Left BCAT1 protein expression unchanged in 67R cells.\n
Dose-dependently reduced protein levels of glycolytic enzymes PFKP and LDHA in 67R cells.
In Vivo

WQQ-345 (80-120 mg/kg; p.o.; twice daily; 43 days) exerts potent antitumor activity in mouse 67R NSCLC xenografts[1].

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

Animal Model: BALB/c nude (4-week-old) subcutaneously injected with 67R cells[1]
Dosage: 80; 120 mg/kg
Administration: p.o.; twice daily; 43 days
Result: Achieved robust tumor regression at 120 mg/kg, with significantly smaller tumor volumes compared to vehicle control by day 43.
Increased H3K27me3 protein expression significantly in tumors treated with 120 mg/kg relative to vehicle control tumors.
Decreased protein levels of glycolytic enzymes PFKP, LDHA, and PKM1/2 significantly in tumors treated with 120 mg/kg relative to vehicle control tumors.
Molecular Weight

183.25

Formula

C10H17NO2
SMILES

O=C(O)C[C@]1(CN)[C@](C2)([H])CC[C@]2([H])C1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
  • 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.

WQQ-345 Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2
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:

WQQ-345WQQ345WQQ 345Histone MethyltransferaseAminotransferases (Transaminases)Lactate DehydrogenaseAminotransferases (Transaminases) LDHEGFR TKI-resistant NSCLC cellsH3K27me3lung cancernon-small cell lung cancerBCAT1LDHA67R NSCLC cellsbranched-chain amino acid catabolismPFKPNSCLC xenograft modelsInhibitorinhibitorinhibit

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:
WQQ-345
Cat. No.:
HY-169061
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.