[CAS NO. 2451481-08-4] Sulfopin

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PRODUCTS SPECIFICATIONS [2451481-08-4]

Catalog

HY-139361

Brand

MCE

CAS

2451481-08-4

DESCRIPTION [2451481-08-4]

Overview

MDL	-
Molecular Weight	281.80
Molecular Formula	C11H20ClNO3S
SMILES	O=C(N(CC(C)(C)C)C(CC1)CS1(=O)=O)CCl

For research use only. We do not sell to patients.

1 Publications Citing Use of MCE

[1]Blood Adv. 2022 Aug 2;bloodadvances.2022007875.

Summary

Sulfopin (PIN1-3) is a highly selective covalent inhibitor of Pin1 with an apparent K _i of 17 nM. Sulfopin blocks Myc-driven tumors in vivo. The peptidyl-prolyl isomerase, Pin1, is exploited in cancer to activate oncogenes and inactivate tumor suppressors ^[1] .

In Vitro

MDA-MB-468 cells show the most pronounced sensitivity to Sulfopin (1, 2.5 μM; 4-8 days) ^[1] .
Sulfopin (2 μM, HEK293 cells; 48 hours) downregulates Myc transcription ^[1] .
Sulfopin (1, 2.5 μM; PATU-8988T cells; 4 days) shows a small but significant reduction in the number of synthesis (S)-phase cells and a corresponding increase of growth 1 (G1)-phase cells ^[1] .

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

Cell Proliferation Assay ^[1]

Cell Line:	Kuramochi, MDA-MB-468, NGP, NBL-S, MDA-MB-468 cells
Concentration:	1, 2.5 μM
Incubation Time:	4,6, 8 days
Result:	Showed variation in antiproliferative effects across cancer cell lines Kuramochi, MDA-MB-468, NGP and NBL-S, with the most pronounced sensitivity observed in MDA-MB-468 cells.

In Vivo

Sulfopin (40 mg/kg; p.o.; QD/BID for 7 days) regresses neuroblastoma in mice ^[1] .
Sulfopin (20-40 mg/kg; i.p.; daily for 27 days) inhibits pancreatic cancer progression in mice ^[1] .
Sulfopin (25-100 μM) blocks neuroblastoma in zebrafish ^[1] .

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

Animal Model:	Transgenic Th-MYCN mice ^[1]
Dosage:	40 mg/kg
Administration:	Once a day (QD) or twice a day (BID) for 7 days
Result:	Sulfopin-treated QD mice showed a significant average increase in survival of 10 days, while Sulfopin-treated BID mice showed an even more pronounced average increase of 28 days.

Appearance

Solid

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL ( 354.86 mM ; Need ultrasonic)

H ₂ O : 4.35 mg/mL ( 15.44 mM ; ultrasonic and warming and heat to 60°C)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	3.5486 mL	17.7431 mL	35.4862 mL
5 mM	0.7097 mL	3.5486 mL	7.0972 mL
10 mM	0.3549 mL	1.7743 mL	3.5486 mL

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

Solubility: ≥ 2.5 mg/mL (8.87 mM); Clear solution
2.

Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)

Solubility: ≥ 2.5 mg/mL (8.87 mM); Clear solution
3.

Add each solvent one by one: 10% DMSO >> 90% corn oil

Solubility: ≥ 2.5 mg/mL (8.87 mM); Clear solution

* All of the co-solvents are available by MCE.

References

[1] Dubiella C, et al. Sulfopin is a covalent inhibitor of Pin1 that blocks Myc-driven tumors in vivo. Nat Chem Biol. 2021;17(9):954-963.