2. Metabolic Enzyme/Protease
  3. Aldose Reductase
  4. SG-55

SG-55 is a selective, noncompetitive and orally active AKR1C3 inhibitor with an IC50 of 5 nM and a Ki of 10 nM. SG-55 shows >2000-fold selectivity for AKR1C3 over AKR1C1, AKR1C2, and AKR1C4 (> 10 μM). SG-55 increases the ratio of reduced/oxidized nicotinamide adenine dinucleotide phosphate (NADPH/NADP+), decreases the ratio of reduced/oxidized glutathione (GSH/GSSG), and induces DNA double-strand breaks. SG-55 can overcome Osimertinib (HY-15772) resistance mediated by EGFR C797S triple mutation in non-small cell lung cancer (NSCLC).

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SG-55

SG-55 Chemical Structure

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SG-55 Related Antibodies

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Description

SG-55 is a selective, noncompetitive and orally active AKR1C3 inhibitor with an IC50 of 5 nM and a Ki of 10 nM. SG-55 shows >2000-fold selectivity for AKR1C3 over AKR1C1, AKR1C2, and AKR1C4 (> 10 μM). SG-55 increases the ratio of reduced/oxidized nicotinamide adenine dinucleotide phosphate (NADPH/NADP+), decreases the ratio of reduced/oxidized glutathione (GSH/GSSG), and induces DNA double-strand breaks. SG-55 can overcome Osimertinib (HY-15772) resistance mediated by EGFR C797S triple mutation in non-small cell lung cancer (NSCLC)[1].

IC50 & Target[1]

AKR1C3

5 nM (IC50)

AKR1C3

10 nM (Ki)

In Vitro

SG-55 (0.5-100 μM; 72 h) does not inhibits the cell growth of AKR1C3-overexpressing PC-9/OR cell line (PC-9 EGFR 19Del/T790M/C797S cells)[1].
SG-55 (72 h) at 10 μM, 20 μM and 50 μM decreased the IC50 of Osimertinib (100-500 nM) in PC-9/OR cells from 2.59 μM to 1.30 μM, 0.43 μM and 0.23 μM, respectively, corresponding to resistance-reversal factors of 2, 6 and 11-fold[1].
SG-55 (10 μM) cooperates with Osimertinib to suppress clonogenicity (14 days), curtail migration (24 h), and amplify cycle arrest (24 h) and apoptosis (72 h), thereby conferring significant sensitization in PC-9/OR cells[1].
SG-55 (10 μM; 72 h)-mediated AKR1C3 inhibition elevates the NADPH/NADP+ ratio, disrupts the GSH cycle, breaks redox balance, and amplifies oxidative damage, thereby overcoming EGFR mutation-driven Osimertinib resistance in PC-9/OR cells[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

SG-55 Related Antibodies

Apoptosis Analysis[1]

Cell Line: AKR1C3-overexpressing PC-9/OR cell lines
Concentration: 10 μM plus Osimertinib (100 nM)
Incubation Time: 72 h
Result: AKR1C3 Inhibition enhanced Osimertinib-induced apoptosis.

Cell Cycle Analysis[1]

Cell Line: AKR1C3-overexpressing PC-9/OR cell lines
Concentration: 10 μM plus Osimertinib (100 nM)
Incubation Time: 24 h
Result: Osimertinib alone imposed a G0/G1 arrest, whereas the addition of the compound shifted the cycle distribution to G2/M accumulation.
Parmacokinetics
Species Dose Route Cmax
Rat[1] 10 mg/kg p.o. 280011.39 μg/L
Rat[1] 2 mg/kg i.v. 22371.51 μg/L
In Vivo

SG-55 (10 mg/kg; p.o.; every 1 days; for 21 days) significantly densitizes Osimertinib-resistant EGFR C797S tumors in mice[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male BALB/c nude mice (6 weeks old) were inoculated subcutaneously in the right flank with 3 × 107 PC-9/OR cells (100 μL) to establish xenografts[1].
Dosage: 10 mg/kg plus Osimertinib (5 mg/kg p.o.)
Administration: p.o.; every 1 days; for 21 days
Result: The tumor-growth inhibition (TGI) values of 15.6%.
When used in combination with osimertinib, the TGI was 93.1%.
No significant body-weight loss was observe.
Molecular Weight

319.36

Formula

C19H17N3O2
SMILES

N#CC1=CC2=C(C=C1)CN(C(C3=CC(C(C4CC4)=O)=CN3)=O)CC2
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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SG-55 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

SG-55SG55SG 55Aldose ReductaseAKR1C3 inhibitornoncompetitiveNADPH/NADP+GSH/GSSGOsimertinib resistancenon-small cell lung cancer (NSCLC)EGFR 19Del/T790M/C797SInhibitorinhibitorinhibit

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