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Chemical Structure| 1262888-28-7 Chemical Structure| 1262888-28-7

Structure of Spautin-1
CAS No.: 1262888-28-7

Chemical Structure| 1262888-28-7

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Spautin-1 is inhibitor of USP10 and USP13 with IC50 of ∼0.6 and 0.7 μM respectively, it's also a potent and specific autophagy inhibitor.

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Product Details of Spautin-1

CAS No. :1262888-28-7
Formula : C15H11F2N3
M.W : 271.26
SMILES Code : FC1=CC=C(C=C1)CNC2=C3C=C(F)C=CC3=NC=N2
MDL No. :MFCD16962292
InChI Key :AWIVHRPYFSSVOG-UHFFFAOYSA-N
Pubchem ID :51037431

Safety of Spautin-1

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H332-H335
Precautionary Statements:P280-P305+P351+P338-P310

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
H4-LC3-GFP cells 5 µM 2 hours MBCQ reduced the spot numbers, spot size, and spot intensity of LC3-GFP+ puncta, indicating inhibition of autophagy. PMC3441147
MEF cells 10 µM 4 hours Spautin-1 reduced the levels of PtdIns3P, indicating that it inhibits autophagy by promoting the degradation of Vps34 complexes. PMC3441147
SW-1573 cells 10 µM 6 hours Spautin-1 reduces MCL1 protein levels by inhibiting USP13 activity and enhances tumor cell sensitivity to ABT-263 PMC5768685
TOV-21G cells 10 µM 6 hours Spautin-1 reduces MCL1 protein levels by inhibiting USP13 activity and enhances tumor cell sensitivity to ABT-263 PMC5768685
Rat aortic smooth muscle cells (RASMs) 10 μM 3 days Spautin-1 inhibited autophagy and induced cellular senescence, evidenced by increased SA-GLB1 activity and upregulated CDKN1A expression PMC7469683
Mouse aortic smooth muscle cells (MASMs) 10 μM 3 days Spautin-1 significantly increased SA-GLB1 activity in WT MASMs, indicating that autophagy inhibition leads to cellular senescence PMC7469683
BPK maμMary tumor cells 2.5 µM 24 hours To evaluate the effect of Spautin-1 on the oxidative respiratory capacity of BPK cells, results showed that Spautin-1 significantly reduced the spare respiratory capacity of the cells. PMC6103709
BPK maμMary tumor cells 2.5 µM 7 days To evaluate the effect of Spautin-1 on the colony-forming ability of BPK cells, results showed that the combination of Spautin-1 and Metformin significantly reduced the colony-forming ability of the cells. PMC6103709
293THK cells 10 μmol/L 12 hours Induced CMA activity, leading to a significant decrease in HK2-GFP fluorescence and protein levels, demonstrating that Spautin-1 can induce CMA. PMC8464644
SKOV-3 cells 10 μM 48 hours Treatment with Spautin-1 reduced MDC puncta, indicating autophagy was blocked at the early stage. PMC8628289
MKN-1 cells 10 μM 48 hours Treatment with Spautin-1 reduced MDC puncta, indicating autophagy was blocked at the early stage. PMC8628289
HBC-5 cells 10 μM 72 hours Treatment with Spautin-1 did not significantly affect cell viability. PMC8628289

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
SKH-1 mice UVB-induced skin tumor model Topical administration 2 mg/mL Once daily for 3 days Spautin-1 promoted the growth of established tumors and significantly increased new tumor formation when combined with UVB irradiation PMC4835978
Nude mice BPK mammary tumor transplant model intraperitoneal injection 0.01 μg/site Single administration, TST performed 15 minutes later To evaluate the effect of Spautin-1 in combination with Metformin on the growth of BPK mammary tumors, results showed that the combination significantly inhibited tumor growth. PMC6103709
Nude mice Prostate cancer xenograft model Intraperitoneal injection 0.2 nmol/g/min Continuous for 5h or 23h Spautin-1 significantly suppressed the growth of prostate cancer xenografts PMC6460657
Nude mice Myeloma xenograft model Intraperitoneal injection 100 mg/kg Once daily for 16 days Combined administration of Spautin-1 and Palbociclib almost suppressed tumor growth within 30 days PMC10462714

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.69mL

0.74mL

0.37mL

18.43mL

3.69mL

1.84mL

36.87mL

7.37mL

3.69mL

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