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MedKoo Cat#: 562577 | Name: SP-100030
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

SP-100030 is a dual inhibitor of NF-κB and AP-1 transcriptional activity. SP 100030 displayed no activity in non-T-cell lines, including monocytes, epithelial cells, fibroblasts, synoviocytes, osteoblasts and endothelial cells.

Chemical Structure

SP-100030
SP-100030
CAS#154563-54-9

Theoretical Analysis

MedKoo Cat#: 562577

Name: SP-100030

CAS#: 154563-54-9

Chemical Formula: C14H5ClF9N3O

Exact Mass: 436.9977

Molecular Weight: 437.64

Elemental Analysis: C, 38.42; H, 1.15; Cl, 8.10; F, 39.07; N, 9.60; O, 3.66

Price and Availability

Size Price Availability Quantity
5mg USD 350.00 2 Weeks
10mg USD 575.00 2 Weeks
25mg USD 1,050.00 2 Weeks
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Related CAS #
No Data
Synonym
SP-100030; SP 100030; SP100030;
IUPAC/Chemical Name
N-[3,5-Bis(trifluoromethyl)phenyl]-2-chloro-4-(trifluoromethyl)-5-pyrimidinecarboxamide
InChi Key
GHMKQBWHPQMXSH-UHFFFAOYSA-N
InChi Code
InChI=1S/C14H5ClF9N3O/c15-11-25-4-8(9(27-11)14(22,23)24)10(28)26-7-2-5(12(16,17)18)1-6(3-7)13(19,20)21/h1-4H,(H,26,28)
SMILES Code
O=C(C1=CN=C(Cl)N=C1C(F)(F)F)NC2=CC(C(F)(F)F)=CC(C(F)(F)F)=C2
Appearance
Solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO and ethanol
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info
Product Data
Product Data
Instruction
View handling instruction
Biological target:
SP-100030 is a potent dual inhibitor of NF-κB and AP-1 transcriptional activity (IC50 = 50 nM).
In vitro activity:
NF-kappa B is crucial in cytokine production for inflammatory diseases. SP-100030 effectively inhibited NF-kappa B activation in Jurkat cells and reduced luciferase production (IC50 = 30 nM). SP-100030 blocked IL-2, IL-8, and TNF-alpha production in T cells but not in other cell types. SP-100030 selectively targets T cells, potentially offering potent immunosuppression with reduced toxicity compared to other NF-kappa B inhibitors. Reference: J Immunol. 2000 Aug 1;165(3):1652-8. https://pubmed.ncbi.nlm.nih.gov/10903776/
In vivo activity:
The specific inhibition of NF-kappaB by SP-100030 could be useful for the treatment of lung fibrosis. In a mouse model of chronic lung fibrosis, mice treated with SP-100030 had significantly less cachexia and lung injury. SP-100030 treated mice also had decreased levels of inflammatory cytokines and growth factors, activation of coagulation activation, and collagen deposition in the lung. The inhibitory activity of SP-100030 was dose dependent and was effective in acute and chronic phases of lung fibrosis. Reference: Am J Respir Crit Care Med. 2007 Dec 15;176(12):1251-60. https://pubmed.ncbi.nlm.nih.gov/17901412/
Solvent mg/mL mM comments
Solubility
DMSO 43.8 100.00
Ethanol 43.8 100.00
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 437.64 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
1. Gerlag DM, Ransone L, Tak PP, Han Z, Palanki M, Barbosa MS, Boyle D, Manning AM, Firestein GS. The effect of a T cell-specific NF-kappa B inhibitor on in vitro cytokine production and collagen-induced arthritis. J Immunol. 2000 Aug 1;165(3):1652-8. doi: 10.4049/jimmunol.165.3.1652. PMID: 10903776. 2. Sullivan RW, Bigam CG, Erdman PE, Palanki MS, Anderson DW, Goldman ME, Ransone LJ, Suto MJ. 2-Chloro-4-(trifluoromethyl)pyrimidine-5-N-(3',5'- bis(trifluoromethyl)phenyl)-carboxamide: a potent inhibitor of NF-kappa B- and AP-1-mediated gene expression identified using solution-phase combinatorial chemistry. J Med Chem. 1998 Feb 12;41(4):413-9. doi: 10.1021/jm970671g. PMID: 9484492. 3. Moore-Carrasco R, Busquets S, Figueras M, Palanki M, López-Soriano FJ, Argilés JM. Both AP-1 and NF-kappaB seem to be involved in tumour growth in an experimental rat hepatoma. Anticancer Res. 2009 Apr;29(4):1315-7. PMID: 19414381. 4. Fujimoto H, D'Alessandro-Gabazza CN, Palanki MS, Erdman PE, Takagi T, Gabazza EC, Bruno NE, Yano Y, Hayashi T, Tamaki S, Sumida Y, Adachi Y, Suzuki K, Taguchi O. Inhibition of nuclear factor-kappaB in T cells suppresses lung fibrosis. Am J Respir Crit Care Med. 2007 Dec 15;176(12):1251-60. doi: 10.1164/rccm.200609-1288OC. Epub 2007 Sep 27. PMID: 17901412.
In vitro protocol:
1. Gerlag DM, Ransone L, Tak PP, Han Z, Palanki M, Barbosa MS, Boyle D, Manning AM, Firestein GS. The effect of a T cell-specific NF-kappa B inhibitor on in vitro cytokine production and collagen-induced arthritis. J Immunol. 2000 Aug 1;165(3):1652-8. doi: 10.4049/jimmunol.165.3.1652. PMID: 10903776. 2. Sullivan RW, Bigam CG, Erdman PE, Palanki MS, Anderson DW, Goldman ME, Ransone LJ, Suto MJ. 2-Chloro-4-(trifluoromethyl)pyrimidine-5-N-(3',5'- bis(trifluoromethyl)phenyl)-carboxamide: a potent inhibitor of NF-kappa B- and AP-1-mediated gene expression identified using solution-phase combinatorial chemistry. J Med Chem. 1998 Feb 12;41(4):413-9. doi: 10.1021/jm970671g. PMID: 9484492.
In vivo protocol:
1. Moore-Carrasco R, Busquets S, Figueras M, Palanki M, López-Soriano FJ, Argilés JM. Both AP-1 and NF-kappaB seem to be involved in tumour growth in an experimental rat hepatoma. Anticancer Res. 2009 Apr;29(4):1315-7. PMID: 19414381. 2. Fujimoto H, D'Alessandro-Gabazza CN, Palanki MS, Erdman PE, Takagi T, Gabazza EC, Bruno NE, Yano Y, Hayashi T, Tamaki S, Sumida Y, Adachi Y, Suzuki K, Taguchi O. Inhibition of nuclear factor-kappaB in T cells suppresses lung fibrosis. Am J Respir Crit Care Med. 2007 Dec 15;176(12):1251-60. doi: 10.1164/rccm.200609-1288OC. Epub 2007 Sep 27. PMID: 17901412.
1: Ye N, Ding Y, Wild C, Shen Q, Zhou J. Small molecule inhibitors targeting activator protein 1 (AP-1). J Med Chem. 2014 Aug 28;57(16):6930-48. doi: 10.1021/jm5004733. Epub 2014 May 27. PubMed PMID: 24831826; PubMed Central PMCID: PMC4148154. 2: Moore-Carrasco R, Busquets S, Figueras M, Palanki M, López-Soriano FJ, Argilés JM. Both AP-1 and NF-kappaB seem to be involved in tumour growth in an experimental rat hepatoma. Anticancer Res. 2009 Apr;29(4):1315-7. PubMed PMID: 19414381. 3: Fujimoto H, D'Alessandro-Gabazza CN, Palanki MS, Erdman PE, Takagi T, Gabazza EC, Bruno NE, Yano Y, Hayashi T, Tamaki S, Sumida Y, Adachi Y, Suzuki K, Taguchi O. Inhibition of nuclear factor-kappaB in T cells suppresses lung fibrosis. Am J Respir Crit Care Med. 2007 Dec 15;176(12):1251-60. Epub 2007 Sep 27. PubMed PMID: 17901412. 4: Moore-Carrasco R, Busquets S, Almendro V, Palanki M, López-Soriano FJ, Argilés JM. The AP-1/NF-kappaB double inhibitor SP100030 can revert muscle wasting during experimental cancer cachexia. Int J Oncol. 2007 May;30(5):1239-45. PubMed PMID: 17390027. 5: Phippard D, Manning AM. Screening for inhibitors of transcription factors using luciferase reporter gene expression in transfected cells. Methods Mol Biol. 2003;225:19-23. Review. PubMed PMID: 12769470. 6: Huang TJ, Adcock IM, Chung KF. A novel transcription factor inhibitor, SP100030, inhibits cytokine gene expression, but not airway eosinophilia or hyperresponsiveness in sensitized and allergen-exposed rat. Br J Pharmacol. 2001 Nov;134(5):1029-36. PubMed PMID: 11682451; PubMed Central PMCID: PMC1573037. 7: Infante JM, Mauchamp A, Fernández-Alé R, Joffre R, Rambal S. Within-tree variation in transpiration in isolated evergreen oak trees: evidence in support of the pipe model theory. Tree Physiol. 2001 Apr;21(6):409-14. PubMed PMID: 11282581. 8: Gerlag DM, Ransone L, Tak PP, Han Z, Palanki M, Barbosa MS, Boyle D, Manning AM, Firestein GS. The effect of a T cell-specific NF-kappa B inhibitor on in vitro cytokine production and collagen-induced arthritis. J Immunol. 2000 Aug 1;165(3):1652-8. PubMed PMID: 10903776. 9: Morikawa M, Shorthouse RA, Suto MJ, Goldman ME, Morris RE. A novel inhibitor of nuclear factor-kappa B and activator protein-1 transcription factors in T cells suppresses host-versus-graft alloreactivity in vivo. Transplant Proc. 1997 Feb-Mar;29(1-2):1269-70. PubMed PMID: 9123300. 10: Goldman ME, Ransone LJ, Anderson DW, Gaarde WA, Suto MJ, Sullivan RW, Shorthouse R, Morikawa M, Morris RE. SP100030 is a novel T-cell-specific transcription factor inhibitor that possesses immunosuppressive activity in vivo. Transplant Proc. 1996 Dec;28(6):3106-9. PubMed PMID: 8962204. 11: Manning, A. M., & Mercurio, F. (1997). Transcription inhibitors in inflammation. Expert Opinion on Investigational Drugs, 6(5), 555-567.