SKI2496

Cat. No.: HY-117982: FAQs
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SKI2496 is an orally active GnRH receptor antagonist (IC₅₀: 0.25 nM for hGnRHR, 13.2 nM for monkey GnRHR, 279.2 nM for rat GnRHR). SKI2496 blocks Ca²⁺ flux with an IC₅₀ value of 0.76 nM. SKI2496 inhibits ERK1/2 phosphorylation with an IC₅₀ value of 2.6 nM. SKI2496 inhbits serum LH concentrations, and can be used for research of sex hormone-dependent disorders.

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

SKI2496 Chemical Structure

CAS No. : 1308378-95-1

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ERK ERK1 ERK2 ERK5 ERK8

Biological Activity
Purity & Documentation
References
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Description

Cellular Effect

Cell Line	Type	Value	Description	References
CHO-K1	IC₅₀	0.44 nM Compound: 18a	Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay	[PMID: 27608177]
HEK293	IC₅₀	13 nM Compound: 18a	Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs b Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs b	[PMID: 27608177]
HEK293	IC₅₀	13.2 nM Compound: 18a	Antagonist activity against monkey GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 10 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs Antagonist activity against monkey GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 10 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs	[PMID: 27608177]
HEK293	IC₅₀	2.9 nM Compound: 18a	Antagonist activity against human GnRH receptor expressed in HEK293 cells assessed as reduction in ERK1/2 phosphorylation pre-incubated for 5 mins before LHRH stimulation for 5 mins by chemiluminescence based assay Antagonist activity against human GnRH receptor expressed in HEK293 cells assessed as reduction in ERK1/2 phosphorylation pre-incubated for 5 mins before LHRH stimulation for 5 mins by chemiluminescence based assay	[PMID: 27608177]
HEK293	IC₅₀	279.2 nM Compound: 18a	Antagonist activity against rat GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 1 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by l Antagonist activity against rat GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 1 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by l	[PMID: 27608177]
HEK293	IC₅₀	3.7 nM Compound: 18a	Displacement of [125I]D-Trp6-LHRH from monkey GnRH receptor expressed in HEK293 cell membranes incubated for 1 hr by competitive binding assay Displacement of [125I]D-Trp6-LHRH from monkey GnRH receptor expressed in HEK293 cell membranes incubated for 1 hr by competitive binding assay	[PMID: 27608177]
HEK293	IC₅₀	520 nM Compound: 18a	Displacement of [125I]D-Trp6-LHRH from rat GnRH receptor expressed in HEK293 cell membranes incubated for 1 hr by competitive binding assay Displacement of [125I]D-Trp6-LHRH from rat GnRH receptor expressed in HEK293 cell membranes incubated for 1 hr by competitive binding assay	[PMID: 27608177]
HEK293	IC₅₀	6.32 nM Compound: 18a	Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 1 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 1 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by	[PMID: 27608177]

Molecular Weight

739.68

Formula

C₃₅H₃₆F₇N₅O₅

CAS No.

1308378-95-1

SMILES

O=C(O)CCCN[C@H](C1=CC=CC=C1)CN(C(N(CC2=C(C(F)(F)F)C=CC=C2F)C(C)=C3N4CCN(CC5=CC=C(C(F)(F)F)O5)CC4)=O)C3=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Kim SM, et al. Discovery of an Orally Bioavailable Gonadotropin-Releasing Hormone Receptor Antagonist. J Med Chem. 2016 Oct 13;59(19):9150-9172. [Content Brief]

SKI2496 Related Classifications

Endocrinology

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The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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The dilution calculator equation

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)	×	Volume _(start)	=	Concentration _(final)	×	Volume _(final)
	×		=		×
C1		V1		C2		V2

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:

SKI24961308378-95-1SKI 2496SKI-2496GnRH ReceptorERKGonadotropin releasing hormone receptorGNRHRExtracellular signal regulated kinasesInhibitorinhibitorinhibit

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