JAK3-IN-6


Catalog No. Size PriceQuantity
M17899-C Contact sales@xcessbio.com for quotation $100Unavailable

Description

JAK3-IN-6 is a potent, selective irreversible Janus Associated Kinase 3 (JAK3) inhibitor, with an IC50 of 0.15 nM.

Product information

CAS Number: 1443235-95-7

Molecular Weight: 350.37

Formula: C19H18N4O3

Chemical Name: ethyl 4-[3-(2-methylprop-2-enamido)phenyl]-7H-pyrrolo[2,3-d]pyrimidine-5-carboxylate

Smiles: CC(=C)C(=O)NC1=CC(=CC=C1)C1N=CN=C2NC=C(C=12)C(=O)OCC

InChiKey: NJPHKVOXHRAPGJ-UHFFFAOYSA-N

InChi: InChI=1S/C19H18N4O3/c1-4-26-19(25)14-9-20-17-15(14)16(21-10-22-17)12-6-5-7-13(8-12)23-18(24)11(2)3/h5-10H,2,4H2,1,3H3,(H,23,24)(H,20,21,22)

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO : 260 mg/mL (742.07 mM; Need ultrasonic).

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

JAK3-IN-6 (compound 2), a potent inhibitor of JAK3 (0.15 nM) is 4300-fold selective for JAK3 over JAK1 in enzyme assays, 67-fold (IL-2 vs. IL-6) or 140-fold (IL-2 vs. EPO or GMCSF) selective in cellular reporter assays and >35-fold selective in human PBMC assays (IL-7 vs. IL-6 or GMCSF). Irreversible JAK3-IN-6 with a JAK1 selective inhibitor 3 (JAK1: 0.96 nM, JAK2: 14 nM, JAK3: >1500 nM, TYK2: 10 nM) are cross titrated to determine if there is an additive or synergistic effect of co-inhibiting JAK1 and JAK3 enzymes on IL-7 signaling in CD3+, CD4+ PBMCs. As shown, the predicted levels of pSTAT5 inhibition based on addition of JAK1 and JAK3 inhibition are very close to the measured effects of cross titrating each compound, demonstrating that there is an additive effect but no synergistic effect of inhibiting JAK1 and JAK3 on blocking STAT5 phosphorylation. Furthermore inhibition of either JAK1 or JAK3 alone is sufficient to fully inhibit pSTAT5.

Products are for research use only. Not for human use.

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