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Chemical Structure| 354812-17-2 Chemical Structure| 354812-17-2

Structure of SC-514
CAS No.: 354812-17-2

Chemical Structure| 354812-17-2

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SC514 is a potent, reversible, ATP-competitive and highly selective IKK-β(IKK-2) inhibitor with IC50 value ranging in 3-12 µM.

Synonyms: GK 01140

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Product Details of SC-514

CAS No. :354812-17-2
Formula : C9H8N2OS2
M.W : 224.30
SMILES Code : O=C(C1=C(N)C=C(C2=CSC=C2)S1)N
Synonyms :
GK 01140
MDL No. :MFCD00206459
InChI Key :BMUACLADCKCNKZ-UHFFFAOYSA-N
Pubchem ID :2807869

Safety of SC-514

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P280-P301+P312-P302+P352-P305+P351+P338

Related Pathways of SC-514

pyroptosis
TLR

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
RAW Blue cells 1 µM 16 hours Measure NF-κB activity, assess tolerance Biomaterials. 2022 Jul;286:121571.
BMDCs 1 µM 16 hours Generate tolerogenic DC phenotype, increase IL-10 secretion Biomaterials. 2022 Jul;286:121571.
Human myometrial cells 100 µM 1 hour Inhibition of IL1β-induced COX2 protein expression Front Immunol. 2018 Dec 20;9:2966.
Human myometrial cells 50 µM 1 hour Inhibition of IL1β-induced COX2 protein expression Front Immunol. 2018 Dec 20;9:2966.
Human myometrial cells 50 µM and 100 µM 1 hour Inhibition of IL1β-induced COX2 protein expression Front Immunol. 2018 Dec 20;9:2966.
Human Aortic Vascular Smooth Muscle Cells (HVSMCs) 30 µM 15 minutes SC-514 markedly attenuated the basal MLC phosphorylation in HVSMCs. Circ Res. 2013 Aug 16;113(5):562-70.
Mouse Embryonic Fibroblasts (MEFs) 30 µM 15 minutes SC-514 markedly decreased MLC phosphorylation levels in wild-type but not IKK2−/− MEFs. Circ Res. 2013 Aug 16;113(5):562-70.
Human chondrocytes 20 µM 24 hours To test whether SC-514 can suppress Postn-induced MMP-13 expression. The results showed that SC-514 significantly suppressed Postn-induced MMP-13 expression, indicating a link between Postn and the NF-κB signaling pathway. Arthritis Rheumatol. 2021 Dec;73(12):2249-2260.
Vascular smooth muscle (VSM) cells 10 µM 24 hours SC-514 inhibited NOS2 activity and protein expression induced by FK565 Br J Pharmacol. 2010 Aug;160(8):1997-2007.
J774.2 macrophages 10 µM 24 hours SC-514 inhibited NOS2 activity and protein expression induced by LPS Br J Pharmacol. 2010 Aug;160(8):1997-2007.
Vascular smooth muscle cells 10 µM 24 hours SC-514 inhibited NOS2 activity and protein expression induced by FK565 Br J Pharmacol. 2010 Aug;160(8):1997-2007.
Macrophages 10 µM 24 hours SC-514 inhibited NOS2 activity and protein expression induced by LPS Br J Pharmacol. 2010 Aug;160(8):1997-2007.
A375 50 µM 48 hours To evaluate the effect of SC-514 combined with fotemustine on melanoma cell proliferation, results showed that co-treatment significantly enhanced fotemustine-induced cytotoxicity Redox Biol. 2017 Apr;11:562-576.
G361 50 µM 48 hours To evaluate the effect of SC-514 combined with fotemustine on melanoma cell proliferation, results showed that co-treatment significantly enhanced fotemustine-induced cytotoxicity Redox Biol. 2017 Apr;11:562-576.
INS-1 cells 20 µM 48 hours SC-514 significantly reduced AngII-induced dedifferentiation and restored insulin expression. Mol Med. 2018 Aug 14;24(1):43.
Min6 cells 20 µM 48 hours SC-514 significantly reduced AngII-induced dedifferentiation and restored insulin expression. Mol Med. 2018 Aug 14;24(1):43.
Human biliary epithelial cells 100 µM Inhibition of NF-κB activation, blocking LPS-induced up-regulation of pri-miRNAs Nucleic Acids Res. 2010 Jun;38(10):3222-32.
SiHa cells 100 µM SC-514 completely reversed the upregulation of IKKb and downregulation of p53 and p21 by LPS in SiHa cells. Chin Med J (Engl). 2016 Nov 20;129(22):2703-2707.
C33A cells 100 µM SC-514 had no effects on the expressions of p53 proteins in C33A cells before and after LPS treatment. Chin Med J (Engl). 2016 Nov 20;129(22):2703-2707.

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
C57BL/6 mice EAE model Intraperitoneal injection 10 μmol/mouse Once daily for 2 days Generate tolerogenic DCs and reduce EAE symptoms Biomaterials. 2022 Jul;286:121571.
Mice Smooth Muscle-Specific IKK2 Deficient Mice (IKK2smKo) Intravascular Administration 100 µM Single Dose SC-514 significantly reduced the vascular contractile responses in IKK2smKo mice. Circ Res. 2013 Aug 16;113(5):562-70.
Nude mice Melanoma xenograft model Intraperitoneal injection 25 mg/kg Daily for 13–15 consecutive days To evaluate the effect of SC-514 combined with fotemustine on melanoma xenograft model, results showed that the combination significantly reduced tumor size Redox Biol. 2017 Apr;11:562-576.
Db/db mice Type 2 diabetes model Oral gavage 30 mg/kg Once daily for 4 weeks SC-514 reversed the AngII-induced β-cell dedifferentiation and dysfunction in db/db mice, reducing the NGN3-positive cell ratio. Mol Med. 2018 Aug 14;24(1):43.

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

4.46mL

0.89mL

0.45mL

22.29mL

4.46mL

2.23mL

44.58mL

8.92mL

4.46mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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