2. Apoptosis PI3K/Akt/mTOR NF-κB Immunology/Inflammation
  3. RIP kinase Akt PI3K NF-κB Interleukin Related Necroptosis
  4. LT-1339-553

LT-1339-553 is a selective, orally active RIPK1 inhibitor with IC50 values of 4.32, 95.74 and 84.33 nM against RIPK1, RIPK2 and RIPK3, respectively. LT-1339-553 exerts anti-necroptotic activity by inhibiting the AKT/PI3K/NF-κB pathway and the IL-17 pathway. LT-1339-553 reduces liver injury, inflammatory responses and collagen deposition. LT-1339-553 can be used in studies related to schistosomiasis-induced liver fibrosis.

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

LT-1339-553

LT-1339-553 Chemical Structure

CAS No. : 3078683-57-2

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.

LT-1339-553 Related Antibodies

Top Publications Citing Use of Products

View All RIP kinase Isoform Specific Products:

View All Isoforms
RIPK1 RIPK2 RIPK3

View All Akt Isoform Specific Products:

View All Isoforms
Akt Akt1 Akt2 Akt3

View All PI3K Isoform Specific Products:

View All Isoforms
PI3Kα PI3Kβ PI3Kγ PI3Kδ PI3KC2α PI3KC2β PI3KC2γ Vps34 PI3K PI3KC3 p120γ

View All NF-κB Isoform Specific Products:

View All Isoforms
NF-κB NF-κB1/p50 RelA/p65 RelB c-Rel

View All Interleukin Related Isoform Specific Products:

View All Isoforms
IL-1 IL-2 IL-3 IL-4 IL-5 IL-6 IL-8 IL-10 IL-12 IL-13 IL-15 IL-17 IL-23 IL-7 IL-33 IL-22 IL-18

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

LT-1339-553 is a selective, orally active RIPK1 inhibitor with IC50 values of 4.32, 95.74 and 84.33 nM against RIPK1, RIPK2 and RIPK3, respectively. LT-1339-553 exerts anti-necroptotic activity by inhibiting the AKT/PI3K/NF-κB pathway and the IL-17 pathway. LT-1339-553 reduces liver injury, inflammatory responses and collagen deposition. LT-1339-553 can be used in studies related to schistosomiasis-induced liver fibrosis[1].

IC50 & Target[1]

RIPK1

4.32 nM (IC50)

RIPK2

95.74 nM (IC50)

RIPK3

84.33 nM (IC50)

IL-17

 

In Vitro

LT-1339-553 potently protects human HT29 cells from necroptosis induced by TNFα/Smac-mimetic/z-VAD-FMK (HY-16658B) (TSZ), with an EC50 of 14.43 nM; meanwhile, this compound exhibits cytotoxicity at high concentrations, with an IC50 of 1760 nM[1].
LT-1339-553 potently protects mouse L929 cells from TSZ-induced necroptosis with an EC50 of 5.33 nM, and inhibits the phosphorylation of mouse RIPK1 in a dose-dependent manner[1].

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

LT-1339-553 Related Antibodies
Parmacokinetics
Species Dose Route Cmax Tmax AUClast T1/2 Vz CL MRTlast F
Rat[1] 1 mg/kg i.v. 3237.5 ng/mL 0.083 h 2070.5 ng·h/mL 3.06 h 2.25 L/kg 8.59 mL/min/kg 1.80 h /
Rat[1] 10 mg/kg p.o. 1920.0 ng/mL 1.25 h 8128.4 ng·h/mL 3.63 h 6.54 L/kg 21.32 mL/min/kg 3.90 h 39.3 %
In Vivo

LT-1339-553 (5-10 mg/kg; i.p.; daily; 4 weeks) significantly alleviates schistosomiasis-induced hepatic fibrosis in C57BL/6 mice[1].
LT-1339-553 (50-100 mg/kg; p.o.; daily; 4 weeks) significantly alleviates schistosomiasis-induced hepatic fibrosis in C57BL/6 mice, with the 100 mg/kg dose suppressing pro-inflammatory and profibrotic signaling pathways including AKT/PI3K/NF-κB and IL-17[1].
LT-1339-553 (400 mg/kg; p.o.; single dose) exhibits a favorable safety profile in ICR mice with no observed toxicity or organ damage over 14 days[1].

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

Animal Model: C57BL/6 (infected percutaneously with S. japonicum cercariae, treated with praziquantel at 5 weeks postinfection to clear parasites)[1]
Dosage: 5 mg/kg; 10 mg/kg
Administration: i.p.; daily; 4 weeks
Result: Significantly improved body weight recovery at weeks 8 and 9 postinfection compared to infected controls.
Reduced liver index from 8.67% to 6.14% and spleen index from 1.60% to 0.76% at 10 mg/kg.
Reduced serum ALT and AST levels, hepatic egg granuloma area, collagen deposition, liver hydroxyproline content, and liver ROS levels compared to infected controls, with significant effects at 10 mg/kg.
Decreased hepatic protein levels of Collagen I and α-SMA, with the 10 mg/kg dose showing more pronounced reduction.
Animal Model: C57BL/6 (infected percutaneously with S. japonicum cercariae, treated with praziquantel at 5 weeks postinfection to clear parasites)[1]
Dosage: 50 mg/kg; 100 mg/kg
Administration: p.o.; daily; 4 weeks
Result: Significantly improved body weight recovery at weeks 8 and 9 postinfection compared to infected controls.
Reduced liver index, spleen index, serum ALT and AST levels, hepatic egg granuloma area, collagen deposition, liver hydroxyproline content, and liver ROS levels compared to infected controls, with significant effects at both doses.
Decreased hepatic protein levels of Collagen I and α-SMA, with the 100 mg/kg dose showing more pronounced reduction.
Downregulated hepatic expression of inflammatory factors (TNF-α, IL-17, IL-1β) and chemokines (CXCL5/9/10/16, CCL2/4/5/7/11/22), and suppressed activation of the AKT/PI3K/NF-κB signaling pathway and necroptosis-related proteins (RIPK1, RIPK3, MLKL, and their phosphorylated forms) at 100 mg/kg.
Molecular Weight

464.34

Formula

C21H13F5N4O3
CAS No.
SMILES

NC1=NOC2=C1C(C3=C(C(F)=C(C=C3)NC(NC4=CC(OC(F)(F)F)=CC=C4)=O)F)=CC=C2
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.

LT-1339-553 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:

LT-1339-5533078683-57-2RIP kinaseAktPI3KNF-κBInterleukin RelatedNecroptosisReceptor-interacting protein kinasesRIPKPKBProtein kinase BPhosphoinositide 3-kinaseNuclear factor-κBNuclear factor-kappaBILschistosomiasis-induced hepatic fibrosisAKT/PI3K/NF-κBC57BL/6 micenecroptosisL929 cellsRIPK3RIPK2RIPK1IL-17HT29 cellsInhibitorinhibitorinhibit

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:
LT-1339-553
Cat. No.:
HY-184001
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.