Home Cart Sign in  
Chemical Structure| 507475-17-4 Chemical Structure| 507475-17-4

Structure of TPCA-1
CAS No.: 507475-17-4

Chemical Structure| 507475-17-4

*Storage: {[sel_prStorage]}

*Shipping: {[sel_prShipping]}

,{[proInfo.pro_purity]}

TPCA-1 is a potent and selective inhibitor of IKK-2 with an IC50 of 17.9 nM, effectively inhibiting STAT3 phosphorylation, DNA binding, and transactivation.

Synonyms: IKK2 Inhibitor IV; GW683965

4.5 *For Research Use Only !

{[proInfo.pro_purity]}
Cat. No.: {[proInfo.prAm]} Purity: {[proInfo.pro_purity]}

Change View

Size Price VIP Price

US Stock

Global Stock

In Stock
{[ item.pr_size ]} Inquiry {[ getRatePrice(item.pr_usd,item.pr_rate,item.mem_rate,item.pr_is_large_size_no_price, item.vip_usd) ]}

US Stock: ship in 0-1 business day
Global Stock: ship in 5-7 days

  • {[ item.pr_size ]}

In Stock

- +

Please Login or Create an Account to: See VIP prices and availability

US Stock: ship in 0-1 business day
Global Stock: ship in 2 weeks

  • 1-2 Day Shipping
  • High Quality
  • Technical Support
Product Citations

Alternative Products

Product Details of TPCA-1

CAS No. :507475-17-4
Formula : C12H10FN3O2S
M.W : 279.29
SMILES Code : FC1=CC=C(C=C1)C2=CC(C(N)=O)=C(S2)NC(N)=O
Synonyms :
IKK2 Inhibitor IV; GW683965
MDL No. :MFCD09037541
InChI Key :SAYGKHKXGCPTLX-UHFFFAOYSA-N
Pubchem ID :9903786

Safety of TPCA-1

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H319
Precautionary Statements:P301+P312+P330-P305+P351+P338

Related Pathways of TPCA-1

pyroptosis
TLR

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
MPAEpiC cells 150, 300, 600 nM 6 h To evaluate the inhibitory effect of TPCA-1 on LPS-induced inflammatory response, results showed that TPCA-1 significantly suppressed the expression of IL-1B, IL-6, IL-8, IL-15, TNFA, MIP2, CCR5, GM-CSF, VEGF, COX2, and iNOS. PMC11191317
RAW264.7 cells 150, 300, 600 nM 6 h To evaluate the inhibitory effect of TPCA-1 on LPS-induced inflammatory response, results showed that TPCA-1 significantly suppressed the expression of IL-1B, IL-6, IL-8, IL-15, TNFA, MIP2, CCR5, GM-CSF, VEGF, COX2, and iNOS. PMC11191317
mammary epithelial cells 25 μM 24 h To test the effect of TPCA-1 on Bcl11b expression, it was found that TPCA-1 significantly upregulated Bcl11b expression PMC11183265
human umbilical vein endothelial cells (HUVECs) 3 μM 1 h TPCA-1 inhibits NF-κB signaling, reducing the expression of lncRNA-CCL2 and CCL2 PMC6697820
BMDCs 10 µM 1 h Inhibition of IKK-2-dependent phosphorylation of SNAP23, blocking MHC-I delivery to phagosomes, but TPCA-1 had no effect on MHC-I delivery and cross-presentation in Tap−/− DCs. PMC8981674
BUMPT cells 50 μM 24 h TPCA1 significantly reduced the levels of P65 phosphorylation and cleavage of caspase 3 in BUMPT cells treated with cisplatin and sTim-3. PMC10314935

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mice Palb2 mutant mice Intraperitoneal injection 20 mg/kg Twice, 12 hours apart Inhibit NFκB, restore radiation-induced apoptosis, and delay tumor development PMC6050088
nude mice SW620 and HCT116 xenograft models intraperitoneal injection 15 mg/kg once every two days, until the end of the experiment The combination of TPCA-1 with trametinib significantly inhibited the growth of PPP6C-deficient tumors and restored their sensitivity to MAPK pathway inhibitors. PMC11238902
C57BL/6 mice ARDS mouse model Not specified 10 mg/kg Once daily for two days To evaluate the inhibitory effect of TPCA-1 on inflammatory response in ARDS mice, results showed that TPCA-1 significantly reduced serum concentrations of IL-1β, IL-6, and TNF-α, but did not affect concentrations of IL-15, IL-18, and IFN-γ. PMC11191317
mice aged mice intraperitoneal injection 10 mg/kg once daily for 30 days To test the effect of TPCA-1 on mammary cell aging, it was found that TPCA-1 significantly reduced the number of senescent cells and increased the number of young cells PMC11183265
CD-1 mice Acute lung inflammation mouse model Intravenous injection 2 mg/kg Single dose, lasting 20 hours To evaluate the therapeutic effect of TPCA-1-NPs-Abs in the acute lung inflammation mouse model, results showed that anti-ICAM-1 decorated NPs significantly reduced lung inflammation. PMC6542597
Mice Cisplatin-induced acute kidney injury model Tail vein injection 1 mg/kg Single injection, lasting 3 days TPCA1 significantly reduced serum creatinine and BUN levels in cisplatin-treated Tim-3 knockout mice and alleviated renal tubular injury. PMC10314935

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.58mL

0.72mL

0.36mL

17.90mL

3.58mL

1.79mL

35.81mL

7.16mL

3.58mL

References

 

Historical Records

Categories