[CAS NO. 2146095-85-2] SHIN1

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PRODUCTS SPECIFICATIONS [2146095-85-2]

Catalog

HY-112066

Brand

MCE

CAS

2146095-85-2

DESCRIPTION [2146095-85-2]

Overview

MDL	-
Molecular Weight	400.47
Molecular Formula	C24H24N4O2
SMILES	OCC1=CC(C2=CC=CC=C2)=CC(C3(C(C(C)=NN4)=C4OC(N)=C3C#N)C(C)C)=C1

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

4 Publications Citing Use of MCE

Summary

SHIN1 (RZ-2994) is a human serine hydroxymethyltransferse 1 and 2 ( SHMT1/2 ) inhibitor with IC ₅₀ s of 5 and 13 nM, respectively, in an in vitro assay.

IC50 & Target

IC50: 5 nM (SHMT1), 13 nM (SHMT1) ^[1]

In Vitro

SHIN1 (RZ-2994) inhibits human SHIN1 SHMT1/2 with IC ₅₀ s of 5 and 13 nM, respectively in an in vitro assay. SHIN1 inhibits the growth of SHMT2 deletion HCT-116 cells with an IC ₅₀ of 10 nM. SHIN1 (RZ-2994) inhibits SHMT1/2 in HCT-116 cells. SHIN1 (RZ-2994) is particularly active against B-cell malignancies. SHIN1 blocks cell growth through a progressive depletion of purines, leading to loss of nucleotide triphosphates ^[1] .

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

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 : 66.67 mg/mL ( 166.48 mM ; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.4971 mL	12.4853 mL	24.9707 mL
5 mM	0.4994 mL	2.4971 mL	4.9941 mL
10 mM	0.2497 mL	1.2485 mL	2.4971 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: ≥ 1.25 mg/mL (3.12 mM); Clear solution
2.

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

Solubility: ≥ 1.25 mg/mL (3.12 mM); Clear solution
3.

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

Solubility: ≥ 1.25 mg/mL (3.12 mM); Clear solution

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

References

[1] Ducker GS, et al. Human SHMT inhibitors reveal defective glycine import as a targetable metabolic vulnerability of diffuse large B-cell lymphoma. Proc Natl Acad Sci U S A. 2017 Oct 24;114(43):11404-11409.