2. Immunology/Inflammation
  3. SphK
  4. SLM6031434

SLM6031434 is a highly selective sphingosine kinase 2 (SphK2) inhibitor with an IC50 value of 0.4 μM for SphK2. SLM6031434 exerts anti-fibrotic effects by increasing sphingosine accumulation and Smad7 expression. SLM6031434 demonstrates effective anti-fibrotic efficacy in a unilateral ureteral obstruction (UUO)-induced tubulointerstitial fibrosis mouse model. SLM6031434 can be used for the study of proteinuric kidney diseases or chronic kidney disease (CKD).

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SLM6031434

SLM6031434 Chemical Structure

CAS No. : 1897379-33-7

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Based on 1 publication(s) in Google Scholar

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SphK1 SphK2

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Description

SLM6031434 is a highly selective sphingosine kinase 2 (SphK2) inhibitor with an IC50 value of 0.4 μM for SphK2. SLM6031434 exerts anti-fibrotic effects by increasing sphingosine accumulation and Smad7 expression. SLM6031434 demonstrates effective anti-fibrotic efficacy in a unilateral ureteral obstruction (UUO)-induced tubulointerstitial fibrosis mouse model. SLM6031434 can be used for the study of proteinuric kidney diseases or chronic kidney disease (CKD)[1][2].

IC50 & Target[1]

SphK2

0.4 μM (IC50)

SphK1

16 μM (IC50)

In Vitro

SLM6031434 (3 μM, 16 h) reduces TGFβ-induced expression of profibrotic markers (Col1, FN-1, CTGF) in primary mouse renal fibroblasts[1].
SLM6031434 (0.3-10 μM, 16 h) dose-dependently increases Smad7 protein expression in primary mouse renal fibroblasts[1].
SLM6031434 (1 μM, 20 h) significantly increases cellular sphingosine levels in human podocytes[2].
SLM6031434 (1 μM, 24 h) upregulates nephrin and Wilm’s tumor suppressor gene 1 (WT1) protein expressions and mRNA expressions in wildtype human podocytes[2].

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

SLM6031434 Related Antibodies
In Vivo

SLM6031434 (5 mg/kg, i.p., daily, 9 days) attenuates unilateral ureteral obstruction (UUO)-induced renal interstitial fibrosis in mice[1].

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

Animal Model: UUO-induced renal interstitial fibrosis mouse models were established by performing unilateral ureteral ligation surgery on 10-12 week-old adult male mice[1]
Dosage: 5 mg/kg
Administration: i.p., daily, 9 days
Result: Reduced collagen accumulation and ECM deposition.
Decreased α-SMA expression to reduce myofibroblast activation.
Downregulated mRNA and protein levels of Col1, FN-1, CTGF.
Increased sphingosine accumulation and Smad7 expression, while reduced Smad2 phosphorylation.
Reduced F4/80-positive macrophage infiltration and downregulated iNOS, Mcr1 mRNA.
Molecular Weight

453.50

Formula

C22H30F3N5O2
CAS No.
SMILES

N=C(N1[C@H](C2=NC(C3=CC=C(OCCCCCCCC)C(C(F)(F)F)=C3)=NO2)CCC1)N
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Storage

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Purity & Documentation
References
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SLM6031434 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:

SLM60314341897379-33-7SLM 6031434SLM-6031434SphKSphingosine kinasesphingosine kinaseSphK2mSphK2rSphK2mSphK1rSphK1Sphingosine 1-phosphateS1PU937renal fibrosisInhibitorinhibitorinhibit

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