JAK3-IN-6

SKU: orb1301745

Description

JAK3-IN-6 is a potent and irreversible inhibitor of Janus Associated Kinase 3 (JAK3), exhibiting an IC50 of 0.15 nM. This small molecule is a valuable research tool for investigating JAK3-dependent signaling in immunological and hematological research, applicable in both cellular and biochemical assays.

Research Area

Cardiovascular Research, Epigenetics & Chromatin, Signal Transduction, Stem Cell & Developmental Biology

Key Properties

• CAS Number: 1443235-95-7
• MW: 350.37
• Purity: 99.94% (May vary between batches)
• Formula: C₁₉H₁₈N₄O₃
• SMILES: CCOC(=O)c1c[nH]c2ncnc(-c3cccc(NC(=O)C(C)=C)c3)c12
• Target: JAK
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (5.71 mM);DMSO:40 mg/mL (114.17 mM)

Bioactivity

• Target IC50:
  JAK3:0.15 nM
• In Vitro:
  a potent inhibitor of JAK3 (0.15 nM) was 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). In vivo, selective JAK3 inhibition was sufficient to block the development of inflammation in a rat model of Rheumatoid Arthritis, while sparing hematopoiesis.
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• Animal Research:
  Female Lewis rats were purchased and housed . 48 rats were divided into six groups (n=8/group). Group 1 were drug-na ve i.e. no compounds were administered throughout the study. On the afternoon of Day 1 (4pm), ABT or vehicle (1 ml/kg p.o.) was administered to Groups 2-5. Days 2-11 (8 am), each animal in Groups 2-5 were administered ABT 10 mpk qd (1 ml/kg p.o.), immediately followed by either vehicle or compound at 5ml/kg p.o. Group 6 animals received vehicle only (5 ml/kg p.o.). Days 2-11 (4 pm) Groups 2-5 were administered vehicle or compound at 5 ml/kg p.o. Animals were monitored and weighed throughout the study. On Day 10, under isoflurane anesthesia, 3 animals from Groups 2-6 were bled via the jugular vein for PK analysis at 4 and 8 h post-8 am dose. On Day 11, blood samples were collected, as described above, at 0 (16 h post-Day 10 pm dose) and 2 h post-am dose for PK, hematology, and clinical chemistry analysis. All remaining animals were euthanized at 2 hrs post-dosing on Day 11 and blood samples were collected for PK, hematology, and clinical chemistry analysis. Data were analyzed using Graphpad prism software. Statistical analyses were performed using a one-way ANOVA with Dunnett s post-hoc test for group comparisons to ABT + vehicle treatment.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Inhibitor, inhibit, JAK, Janus kinase, JAK3IN6, JAK-3-IN-6, JAK3-IN-6, JAK3 IN 6, JAK3

Compound Identifiers

PubChem CID

89629876