2. Cell Cycle/DNA Damage Epigenetics Protein Tyrosine Kinase/RTK JAK/STAT Signaling Stem Cell/Wnt Immunology/Inflammation
  3. Sirtuin JAK STAT Interleukin Related
  4. SIRT5-IN-10

SIRT5-IN-10 is a competitive SIRT5 inhibitor. SIRT5-IN-10 improves renal function and reduces histopathological damage in septic acute kidney injury (AKI) mice. SIRT5-IN-10 can be used for the research of sepsis-associated AKI.

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SIRT5-IN-10

SIRT5-IN-10 Chemical Structure

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SIRT5-IN-10 Related Antibodies

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STAT3 STAT5 STAT6 STAT1

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IL-1 IL-2 IL-3 IL-4 IL-5 IL-6 IL-8 IL-10 IL-12 IL-13 IL-15 IL-17 IL-23 IL-7 IL-33 IL-22 IL-18

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Description

SIRT5-IN-10 is a competitive SIRT5 inhibitor. SIRT5-IN-10 improves renal function and reduces histopathological damage in septic acute kidney injury (AKI) mice. SIRT5-IN-10 can be used for the research of sepsis-associated AKI[1].

IC50 & Target[1]

SIRT5

 

In Vitro

SIRT5-IN-10 (compound 56) (0.03-600 μM; 2 h) potently inhibits recombinant human SIRT5 catalytic domain with an IC50 of 0.29 μM at 100 μM NAD+ and 0.79 μM at 400 μM NAD+[1].
SIRT5-IN-10 acts as a dual competitive inhibitor of recombinant human SIRT5, competing for binding with both the NAD+ cofactor and the P16 substrate[1].

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

SIRT5-IN-10 Related Antibodies
Parmacokinetics
Species Dose Route AUC0-∞ Cmax Tmax T1/2 Vz CL AUC0-24
Rat[1] 10 mg/kg i.p. 1601.71 ng/mL·h 417.39 ng/mL 0.69 h 2.75 h 73560 mL/kg 6330 mL/h/kg 1487.85 ng·h/mL
In Vivo

SIRT5-IN-10 (compound 56) (20-40 mg/kg; i.p.; two doses (1 h pre-surgery and 8 h post-surgery)) protects against cecal ligation and punctu (CLP)-induced septic AKI in mice[1].
SIRT5-IN-10 (40 mg/kg; i.p.; two doses (1 h pre-LPS injection and 8 h post-LPS (HY-D1056) injection)) significantly protects against LPS-induced septic AKI in mice[1].

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

Animal Model: C57BL/6J mice (male, 8 weeks old) with CLP-induced septic AKI[1]
Dosage: 20; 40 mg/kg
Administration: i.p.; two doses (1 h pre-surgery and 8 h post-surgery)
Result: Reduced serum blood urea nitrogen (BUN) and serum creatinine (Scr) levels at 40 mg/kg dose.
Mitigated tubular dilation and damage via H&E staining and tubular injury scoring at 40 mg/kg dose.
Downregulated renal mRNA expression of injury markers Havcr1 (KIM-1) and Lcn2 (NGAL) at 40 mg/kg dose.
Exhibited renoprotective effects at both doses, with 40 mg/kg being more potent.
Showed no statistically significant differences in serum ALT, AST, Scr, or BUN levels between compound-treated mice and normal controls.
Caused no notable histopathological changes in heart, liver, lung, spleen, or testis tissues.
Animal Model: C57BL/6J mice (male, 8 weeks old) with LPS-induced septic AKI[1]
Dosage: 40 mg/kg
Administration: i.p.; two doses (1 h pre-LPS injection and 8 h post-LPS injection)
Result: Attenuated LPS-induced elevations in serum Scr and BUN levels.
Downregulated renal mRNA expression of KIM-1 and NGAL.
Ameliorated histopathological renal damage.
Partially normalized aberrant renal succinylation profiles.
Suppressed pro-inflammatory JAK-STAT signaling by reducing renal mRNA expression of Il6, Jak1, Jak2, and Stat3.
Lowered plasma CRP levels.
Decreased renal mRNA levels of inflammatory mediators Il6, Mcp1, and Tnf-α.
Molecular Weight

610.64

Formula

C27H30N8O7S
SMILES

O=C(C1=C(N=C(N=C1)C2=CC=C(S2)C(C)=O)NCCCN/C(NCCC(O)=O)=C\[N+]([O-])=O)NC3=CC=CC(NC(C)=O)=C3
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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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SIRT5-IN-10 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:

SIRT5-IN-10SirtuinJAKSTATInterleukin RelatedJanus kinaseILacyl-lysine substrateJAK-STAT signalingP16 substrateSIRT5NAD+recombinant human SIRT5 catalytic domainrenal inflammationseptic AKILPS-induced septic AKICLP-induced septic AKI miceInhibitorinhibitorinhibit

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