SC-514
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    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 526794

CAS#: 354812-17-2

Description: SC-514 is a selective and reversible inhibitor of IκB kinase 2 (IKK2) that may target osteoclastogenesis. SC-514 dose-dependently inhibits RANKL-induced osteoclastogenesis and induced apoptosis and caspase 3 activation in RAW264.7 cells. Targeting IKKβ by SC-514 may be a potential treatment for osteoclast-related disorders such as osteoporosis and cancer-induced bone loss.

Chemical Structure

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SC-514
CAS# 354812-17-2
Product data Instruction

Theoretical Analysis

MedKoo Cat#: 526794
Name: SC-514
CAS#: 354812-17-2
Chemical Formula: C9H8N2OS2
Exact Mass: 224.01
Molecular Weight: 224.300
Elemental Analysis: C, 48.19; H, 3.60; N, 12.49; O, 7.13; S, 28.59

Price and Availability

Size Price Availability Quantity
5mg USD 350 2 Weeks
10mg USD 500 2 Weeks
25mg USD 750 2 Weeks
50mg USD 1100 2 Weeks
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Synonym: SC-514; SC 514; SC514.

IUPAC/Chemical Name: 4-amino-[2,3'-bithiophene]-5-carboxamide

InChi Key: BMUACLADCKCNKZ-UHFFFAOYSA-N

InChi Code: InChI=1S/C9H8N2OS2/c10-6-3-7(5-1-2-13-4-5)14-8(6)9(11)12/h1-4H,10H2,(H2,11,12)

SMILES Code: NC(=O)c1sc(cc1N)c1cscc1

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

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: SC-514 is a selective IKK-2 inhibitor (IC50=11.2 μM), which does not inhibit other IKK isoforms or other serine-threonine and tyrosine kinases.
In vitro activity: SC-514 is a potential treatment for osteoclast-related disorders, such as osteoporosis. SC-514 dose-dependently inhibits RANKL-induced osteoclastogenesis. At high concentrations, SC-514 induced apoptosis and caspase 3 activation in RAW264.7 cells. SC-514 impairs RANKL-induced osteoclastogenesis and NF-κB activation. Reference: Biochem Pharmacol. 2013 Dec 15;86(12):1775-83. https://pubmed.ncbi.nlm.nih.gov/24091016/
In vivo activity: The combination of SC-514 with nitrosoureas has potential for melanoma therapy. In a xenograft mouse model, SC-514 cooperated with nitrosourea to reduce metastatic melanoma tumor size and malignancy in vivo. Reference: Redox Biol. 2017 Apr;11:562-576. https://pubmed.ncbi.nlm.nih.gov/28107677/

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 100.0 445.83

Preparing Stock Solutions

The following data is based on the product molecular weight 224.30 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. Liu Q, Wu H, Chim SM, Zhou L, Zhao J, Feng H, Wei Q, Wang Q, Zheng MH, Tan RX, Gu Q, Xu J, Pavlos N, Tickner J, Xu J. SC-514, a selective inhibitor of IKKβ attenuates RANKL-induced osteoclastogenesis and NF-κB activation. Biochem Pharmacol. 2013 Dec 15;86(12):1775-83. doi: 10.1016/j.bcp.2013.09.017. Epub 2013 Sep 30. PMID: 24091016. 2. Kishore N, Sommers C, Mathialagan S, Guzova J, Yao M, Hauser S, Huynh K, Bonar S, Mielke C, Albee L, Weier R, Graneto M, Hanau C, Perry T, Tripp CS. A selective IKK-2 inhibitor blocks NF-kappa B-dependent gene expression in interleukin-1 beta-stimulated synovial fibroblasts. J Biol Chem. 2003 Aug 29;278(35):32861-71. doi: 10.1074/jbc.M211439200. Epub 2003 Jun 17. PMID: 12813046. 3. Tse AK, Chen YJ, Fu XQ, Su T, Li T, Guo H, Zhu PL, Kwan HY, Cheng BC, Cao HH, Lee SK, Fong WF, Yu ZL. Sensitization of melanoma cells to alkylating agent-induced DNA damage and cell death via orchestrating oxidative stress and IKKβ inhibition. Redox Biol. 2017 Apr;11:562-576. doi: 10.1016/j.redox.2017.01.010. Epub 2017 Jan 12. PMID: 28107677; PMCID: PMC5247288. 4. Johnson J, Shi Z, Liu Y, Stack MS. Inhibitors of NF-kappaB reverse cellular invasion and target gene upregulation in an experimental model of aggressive oral squamous cell carcinoma. Oral Oncol. 2014 May;50(5):468-77. doi: 10.1016/j.oraloncology.2014.02.004. Epub 2014 Feb 28. PMID: 24582884; PMCID: PMC4001858.
In vitro protocol: 1. Liu Q, Wu H, Chim SM, Zhou L, Zhao J, Feng H, Wei Q, Wang Q, Zheng MH, Tan RX, Gu Q, Xu J, Pavlos N, Tickner J, Xu J. SC-514, a selective inhibitor of IKKβ attenuates RANKL-induced osteoclastogenesis and NF-κB activation. Biochem Pharmacol. 2013 Dec 15;86(12):1775-83. doi: 10.1016/j.bcp.2013.09.017. Epub 2013 Sep 30. PMID: 24091016. 2. Kishore N, Sommers C, Mathialagan S, Guzova J, Yao M, Hauser S, Huynh K, Bonar S, Mielke C, Albee L, Weier R, Graneto M, Hanau C, Perry T, Tripp CS. A selective IKK-2 inhibitor blocks NF-kappa B-dependent gene expression in interleukin-1 beta-stimulated synovial fibroblasts. J Biol Chem. 2003 Aug 29;278(35):32861-71. doi: 10.1074/jbc.M211439200. Epub 2003 Jun 17. PMID: 12813046.
In vivo protocol: 1. Tse AK, Chen YJ, Fu XQ, Su T, Li T, Guo H, Zhu PL, Kwan HY, Cheng BC, Cao HH, Lee SK, Fong WF, Yu ZL. Sensitization of melanoma cells to alkylating agent-induced DNA damage and cell death via orchestrating oxidative stress and IKKβ inhibition. Redox Biol. 2017 Apr;11:562-576. doi: 10.1016/j.redox.2017.01.010. Epub 2017 Jan 12. PMID: 28107677; PMCID: PMC5247288. 2. Johnson J, Shi Z, Liu Y, Stack MS. Inhibitors of NF-kappaB reverse cellular invasion and target gene upregulation in an experimental model of aggressive oral squamous cell carcinoma. Oral Oncol. 2014 May;50(5):468-77. doi: 10.1016/j.oraloncology.2014.02.004. Epub 2014 Feb 28. PMID: 24582884; PMCID: PMC4001858.

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1. Kishore, N., Sommers, C., Mathialagan, S., et al. A selective IKK-2 inhibitor blocks NF- k B-dependent gene expression in interleukin-1ß-stimulated synovial fibroblasts. The Journal of Biological Chemisty 278(35), 32861-32871 (2003).

2. Baxter, A., Brough, S., Cooper, A., et al. Hit-to-lead studies: The discovery of potent, orally active, thiophenecarboxamide IKK-2 inhibitors. Bioorganic & Medicinal Chemistry Letters 14, 2817-2822 (2004).

3. Gomez, A.B., MacKenzie, C., Paul, A., et al. Selective inhibition of inhibitory kappa B kinase-b abrogates induction of nitric oxide synthase in lipopolysaccharide-stimulated rat aortic smooth muscle cells. British Journal of Pharmacology 146, 217-225 (2005).

4. Phulwani, N.K., Esen, N., Syed, M.M., et al. TLR2 expression in astrocytes is induced by TNF-α-and NF- k B-dependent pathways. Journal of Immunology 181, 3841-3849 (2008).