TPCA-1

Alternative_name

2-[(Aminocarbonyl)amino]-5-(4-fluorophenyl)-3-thiophenecarboxamide
Description

A potent and selective inhibitor of IκB kinase-2 (IKK-2) (IC₅₀ = 17.9 nM). Displays > 22-fold selectivity over IKK-1 and > 550-fold selectivity over other kinases and enzymes. TPCA-1 inhibits production of pro-inflammatory cytokines in vitro and in vivo and inhibits NF-κB nuclear localization. It has been used to study inhibition of IKK-2 to prevent inflammatory mediator release in animal models of arthritis and airway inflammation.
CAS Number

507475-17-4
Structure Available

Yes
Salt Form

No
Molecular Formula

C₁₂H₁₀FN₃O₂S
Molecular Weight

279.29
Cell Permeable

Yes
Purity

≥95% by HPLC
Solubilities

DMSO (~25 mg/ml) or EtOH (~3 mg/ml)
Handling

Protect from light and air
Tag Line

A potent and selective IκB kinase-2 (IKK-2) inhibitor
Storage Condition

-20 ̊C
Shipping Condition

gel pack
Shelf Life

36 months
MDL Number

MFCD09037541
PubChem CID

9903786
PubChem CID Link
SMILES

C1=CC(=CC=C1C2=CC(=C(S2)NC(=O)N)C(=O)N)F
InChi

InChI=1S/C12H10FN3O2S/c13-7-3-1-6(2-4-7)9-5-8(10(14)17)11(19-9)16-12(15)18/h1-5H,(H2,14,17)(H3,15,16,18)
InChi Key

SAYGKHKXGCPTLX-UHFFFAOYSA-N
Data Sheet Link
MSDS Available

Yes

Gene target

TPCA-1
Gene symbol

IGHVII-1-1, MIR1-1, TRUND-NNN8-1, TRUND-NNN7-1, IGKV1OR2-1, MIR1289-1, MIR101-1, MIR16-1, PIRC1
Short name

TPCA-1
Alternative name

TPCA-1

Identity

HGNC:5670
Gene

IGHVII-1-1
Long gene name

immunoglobulin heavy variable (II)-1-1 (pseudogene)
Synonyms gene name
- immunoglobulin heavy variable (II)-1-1
- immunoglobulin heavy variable (II)-1-1 pseudogene
Synonyms
- IGHV(II)-1-1
GenBank acession
- AB019441
Locus

14q32.33
Discovery year

2000-04-17
Entrez gene record

28377
RefSeq identity
- NG_001019
Classification
- Immunoglobulin heavy locus at 14q32.33
VEGA ID

OTTHUMG00000152325

Identity

HGNC:5760
Gene

IGKV1OR2-1
Long gene name

immunoglobulin kappa variable 1/OR2-1 (pseudogene)
Synonyms gene
- IGKVPZ1
- IGKV1OR-1
Synonyms gene name
- immunoglobulin kappa variable 1/OR-1
- immunoglobulin kappa variable 1/OR-1 pseudogene
- immunoglobulin kappa variable 1/OR-1 (pseudogene)
Synonyms
- IGKV1/OR-1
- IGKV1/OR2-1
GenBank acession
- Z12367
Locus

2p11.1
Discovery year

2000-04-18
Entrez gene record

3531
Pubmed identfication
- 2853098
Classification
- Immunoglobulin kappa (IGK) orphons
VEGA ID

OTTHUMG00000155081