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SKU | Size | Availability | Price | Qty |
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T126861-5mg | 5mg | Available within 4-8 weeks(?) Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience! | $75.90 | |
T126861-25mg | 25mg | Available within 4-8 weeks(?) Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience! | $342.90 | |
T126861-100mg | 100mg | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $532.90 |
Potent, selective IκB kinase inhibitor
Synonyms | TPCA-1|507475-17-4|5-(4-Fluorophenyl)-2-ureidothiophene-3-carboxamide|IKK-2 Inhibitor IV|TPCA1|2-(carbamoylamino)-5-(4-fluorophenyl)thiophene-3-carboxamide|[5-(p-Fluorophenyl)-2-ureido]thiophene-3-carboxamide|IKK2 Inhibitor IV|IKK 2 Inhibitor IV|TPCA 1|CH |
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Specifications & Purity | Moligand™, ≥98% |
Biochemical and Physiological Mechanisms | TPCA-1 is potent, selective inhibitor of IκB kinase-2 (IKK-2) (IC50 = 17.9 nM) that displays > 22-fold selectivity over IKK-1 and > 550-fold selectivity over other kinases and enzymes. TPCA-1 inhibits production of pro-inflammatory cytokines i |
Storage Temp | Store at -20°C |
Shipped In | Ice chest + Ice pads |
Grade | Moligand™ |
Action Type | INHIBITOR |
Mechanism of action | Inhibitor of inhibitor of nuclear factor kappa B kinase subunit beta |
Note | Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour. Need more advice on solubility, usage and handling? Please visit our frequently asked questions (FAQ) page for more details. |
Product Description | TPCA-1 is potent, selective inhibitor of IKK-2 (IC50 = 17.9 nM) that displays > 22-fold selectivity over IKK-1 and > 550-fold selectivity over other kinases and enzymes. |
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IUPAC Name | 2-(carbamoylamino)-5-(4-fluorophenyl)thiophene-3-carboxamide |
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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 |
Canonical SMILES | C1=CC(=CC=C1C2=CC(=C(S2)NC(=O)N)C(=O)N)F |
Isomeric SMILES | C1=CC(=CC=C1C2=CC(=C(S2)NC(=O)N)C(=O)N)F |
WGK Germany | 3 |
PubChem CID | 9903786 |
Molecular Weight | 279.29 |
PubChem CID | 9903786 |
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ChEMBL Ligand | CHEMBL257167 |
CAS Registry No. | 507475-17-4 |
RCSB PDB Ligand | NM7 |
Enter Lot Number to search for COA:
To view the certificate results,please click on a Lot number.For Lot numbers from past orders,please use our order status section
Lot Number | Certificate Type | Date | Item |
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E1718001 | Certificate of Analysis | Jan 12, 2023 | T126861 |
Solubility | DMSO 56 mg/mL Water <1 mg/mL Ethanol <1 mg/mL |
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Pictogram(s) | GHS07 |
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Signal | Warning |
Hazard Statements | H319:Causes serious eye irritation H302:Harmful if swallowed |
Precautionary Statements | P305+P351+P338:IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses if present and easy to do - continue rinsing. P280:Wear protective gloves/protective clothing/eye protection/face protection. P501:Dispose of contents/container to ... P264:Wash hands [and …] thoroughly after handling. P270:Do not eat, drink or smoke when using this product. P330:Rinse mouth. P264+P265:Wash hands [and …] thoroughly after handling. Do not touch eyes. P301+P317:IF SWALLOWED: Get medical help. P337+P317:If eye irritation persists: Get medical help. |
WGK Germany | 3 |
1. Podolin PL, Callahan JF, Bolognese BJ, Li YH, Carlson K, Davis TG, Mellor GW, Evans C, Roshak AK. (2005) Attenuation of murine collagen-induced arthritis by a novel, potent, selective small molecule inhibitor of IkappaB Kinase 2, TPCA-1 (2-[(aminocarbonyl)amino]-5-(4-fluorophenyl)-3-thiophenecarboxamide), occurs via reduction of proinflammatory cytokines and antigen-induced T cell Proliferation.. J Pharmacol Exp Ther, 312 (1): (373-81). [PMID:15316093] |
2. Llona-Minguez S, Baiget J, Mackay SP. (2013) Small-molecule inhibitors of IκB kinase (IKK) and IKK-related kinases.. Pharm Pat Anal, 2 (4): (481-98). [PMID:24237125] |
3. Lim J et al.. (2022) Induction of natural IgE by glucocorticoids.. J Exp Med, 219 (10): [PMID:36098746] |
4. Nakamura K et al.. (2020) IFNT-independent effects of intrauterine extracellular vesicles (EVs) in cattle.. Reproduction, 159 (5): (503-511). [PMID:32103820] |