SC-514 | CAS# 354812-17-2 | IKK2 inhibitor

MedKoo Cat#: 526794 | Name: SC-514

Description:

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

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

SC-514

CAS#354812-17-2

Theoretical Analysis

MedKoo Cat#: 526794

Name: SC-514

CAS#: 354812-17-2

Chemical Formula: C9H8N2OS2

Exact Mass: 224.0078

Molecular Weight: 224.30

Elemental Analysis: C, 48.19; H, 3.60; N, 12.49; O, 7.13; S, 28.59

Price and Availability

Size	Price	Availability
5mg	USD 350.00	Ready to ship
100mg	USD 450.00	Ready to ship
200mg	USD 750.00	Ready to ship
500mg	USD 1,550.00	Ready to ship
1g	USD 2,450.00	Ready to ship
2g	USD 4,050.00	Ready to ship

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Related CAS #

354812-17-2

Synonym

SC-514; SC 514; SC514; GK 01140; GK-01140; GK01140;

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

Certificate of Analysis

View CoA: current batch, Lot#A24T05K23

QC Data

View QC data: current batch, Lot#A24T05K23

Safety Data Sheet (SDS)

View Safety Data Sheet (SDS)

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/

	Solvent	mg/mL	mM
Solubility
	DMSO	100.0	445.83

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 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.

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:

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.

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: Pan D, Li Y, Yang F, Lv Z, Zhu S, Shao Y, Huang Y, Ning G, Feng S. Increasing toll-like receptor 2 on astrocytes induced by Schwann cell-derived exosomes promotes recovery by inhibiting CSPGs deposition after spinal cord injury. J Neuroinflammation. 2021 Aug 9;18(1):172. doi: 10.1186/s12974-021-02215-x. PMID: 34372877; PMCID: PMC8353762. 3: Han R, Gao J, Wang L, Hao P, Chen X, Wang Y, Jiang Z, Jiang L, Wang T, Zhu L, Li X. MicroRNA-146a negatively regulates inflammation via the IRAK1/TRAF6/NF-κB signaling pathway in dry eye. Sci Rep. 2023 Jul 11;13(1):11192. doi: 10.1038/s41598-023-38367-4. PMID: 37433841; PMCID: PMC10336050. 4: Dumler JS, Lichay M, Chen WH, Rennoll-Bankert KE, Park JH. Anaplasma phagocytophilum Activates NF-κB Signaling via Redundant Pathways. Front Public Health. 2020 Oct 30;8:558283. doi: 10.3389/fpubh.2020.558283. PMID: 33194960; PMCID: PMC7661751. 5: Spivack K, Muzzelo C, Hall M, Warga E, Neely C, Slepian H, Cunningham A, Tucker M, Elmer J. Enhancement of transgene expression by the β-catenin inhibitor iCRT14. Plasmid. 2021 Mar;114:102556. doi: 10.1016/j.plasmid.2021.102556. Epub 2021 Jan 17. PMID: 33472046. 6: Deak P, Knight HR, Esser-Kahn A. Robust tolerogenic dendritic cells via push/pull pairing of toll-like-receptor agonists and immunomodulators reduces EAE. Biomaterials. 2022 Jul;286:121571. doi: 10.1016/j.biomaterials.2022.121571. Epub 2022 May 11. PMID: 35597168; PMCID: PMC10152544. 7: Ma L, Zhen J, Sorisky A. Regulators of thymic stromal lymphopoietin production by human adipocytes. Cytokine. 2020 Dec;136:155284. doi: 10.1016/j.cyto.2020.155284. Epub 2020 Sep 16. PMID: 32950025. 8: You W, Hong Y, He H, Huang X, Tao W, Liang X, Zhang Y, Li X. TGF-β mediates aortic smooth muscle cell senescence in Marfan syndrome. Aging (Albany NY). 2019 May 30;11(11):3574-3584. doi: 10.18632/aging.101998. PMID: 31147528; PMCID: PMC6594817. 9: Kwon Y, Choi SK, Byeon S, Lee YH. Involvement of inhibitor kappa B kinase 2 (IKK2) in the regulation of vascular tone. Lab Invest. 2018 Oct;98(10):1311-1319. doi: 10.1038/s41374-018-0061-4. Epub 2018 May 21. PMID: 29785049. 10: Huang X, Zeng Y, Jiang Y, Qin Y, Luo W, Xiang S, Sooranna SR, Pinhu L. Lipopolysaccharide-Binding Protein Downregulates Fractalkine through Activation of p38 MAPK and NF-κB. Mediators Inflamm. 2017;2017:9734837. doi: 10.1155/2017/9734837. Epub 2017 May 29. PMID: 28634422; PMCID: PMC5467387. 11: Negi G, Sharma SS. Inhibition of IκB kinase (IKK) protects against peripheral nerve dysfunction of experimental diabetes. Mol Neurobiol. 2015 Apr;51(2):591-8. doi: 10.1007/s12035-014-8784-8. Epub 2014 Jun 20. PMID: 24946751. 12: Ferrao Blanco MN, Bastiaansen-Jenniskens YM, Chambers MG, Pitsillides AA, Narcisi R, van Osch GJVM. Effect of Inflammatory Signaling on Human Articular Chondrocyte Hypertrophy: Potential Involvement of Tissue Repair Macrophages. Cartilage. 2021 Dec;13(2_suppl):168S-174S. doi: 10.1177/19476035211021907. Epub 2021 Jun 24. PMID: 34165367; PMCID: PMC8739598. 13: Duan X, Cai L, Pham CTN, Abu-Amer Y, Pan H, Brophy RH, Wickline SA, Rai MF. Amelioration of Posttraumatic Osteoarthritis in Mice Using Intraarticular Silencing of Periostin via Nanoparticle-Based Small Interfering RNA. Arthritis Rheumatol. 2021 Dec;73(12):2249-2260. doi: 10.1002/art.41794. Epub 2021 Oct 28. PMID: 33982891; PMCID: PMC8589880. 14: Kotnik P, Keuper M, Wabitsch M, Fischer-Posovszky P. Interleukin-1β downregulates RBP4 secretion in human adipocytes. PLoS One. 2013;8(2):e57796. doi: 10.1371/journal.pone.0057796. Epub 2013 Feb 27. PMID: 23460908; PMCID: PMC3584036. 15: Li Y, Li P, Lin SH, Zheng YQ, Zheng XX. Paeonol inhibited TNFα-induced GM- CSF expression in fibroblast-like synoviocytes. Int J Clin Pharmacol Ther. 2014 Nov;52(11):986-96. doi: 10.5414/CP202127. PMID: 25161157. 16: Chen H, Zhou W, Ruan Y, Yang L, Xu N, Chen R, Yang R, Sun J, Zhang Z. Reversal of angiotensin ll-induced β-cell dedifferentiation via inhibition of NF-κb signaling. Mol Med. 2018 Aug 14;24(1):43. doi: 10.1186/s10020-018-0044-3. PMID: 30134927; PMCID: PMC6092859. 17: You Y, Qin Y, Lin X, Yang F, Li J, Sooranna SR, Pinhu L. Methylprednisolone attenuates lipopolysaccharide-induced Fractalkine expression in kidney of Lupus- prone MRL/lpr mice through the NF-kappaB pathway. BMC Nephrol. 2015 Aug 27;16:148. doi: 10.1186/s12882-015-0145-y. PMID: 26310926; PMCID: PMC4551515. 18: 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. 19: Bloom MJ, Saksena SD, Swain GP, Behar MS, Yankeelov TE, Sorace AG. The effects of IKK-beta inhibition on early NF-kappa-B activation and transcription of downstream genes. Cell Signal. 2019 Mar;55:17-25. doi: 10.1016/j.cellsig.2018.12.004. Epub 2018 Dec 10. PMID: 30543861; PMCID: PMC6348059. 20: 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.