Lck Inhibitor CAS: 213743-31-8
MF: C23H22N4O
MW: 370.45
A cell-permeable ATP-competitive inhibitor of Lck.

Lck Inhibitor (CAS 213743-31-8)

Lck Inhibitor | CAS 213743-31-8 is rated 5.0 out of 5 by 1.
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Synonym: 7-Cyclopentyl-5-(4-phenoxyphenyl)-7H-pyrrolo[2,3d] pyrimidin-4-ylamine
Application: A cell-permeable ATP-competitive inhibitor of Lck
CAS Number: 213743-31-8
Purity: ≥95%
Molecular Weight: 370.45
Molecular Formula: C23H22N4O
* Refer to Certificate of Analysis for lot specific data (including water content).
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Lck Inhibitor is a cell-permeable pyrrolopyrimidine compound that acts as a potent, selective, and ATP-competitive inhibitor of Lck (IC50 at 5 μM ATP = < 1 nM, 2 nM, 70 nM, 1.57 μM and 1.98 μM for lck64-509 Y394, Lckcd pY394, Src, Kdr and Tie-2, respectively; IC50 at 1 mM ATP = 16 μM, 66 nM, 126 nM, 420 nM and 5.18 μM for Lck64-509 Y394, Blk, Fyn, Lyn and Csk, respectively). Only minimally affects the activities of other kinases (IC50 = 3.2 μM, > 33 μM, > 50 μM and > 50 μM for EGFR, PKC, CDC2/B and ZAP-70, respectively). Also shown to potently block T-cell receptor-stimulated IL-2 production in vitro (IC50 < 1-40 nM in Jurkat T cells).


References

Burchat, A.F., et al. 2000. Bioorg. Med. Chem. Lett. 10, 2171. Arnold. L.D., et al. 2000. Bioorg. Med. Chem. Lett. 10, 2167.

Physical State :
Solid
Solubility :
Soluble in DMSO (17 mg/ml) at 60° C.
Storage :
Store at 4° C
Melting Point :
239.74° C (Predicted)
Boiling Point :
605.08° C at 760 mmHg (Predicted)
Density :
1.31 g/cm3 (Predicted)
Refractive Index :
n20D 1.70 (Predicted)
IC50 :
Lck: IC50 = 5 µM; EGFR: IC50 = 3.2 µM; PKC: IC50 = > 33 µM; CDC2/B: IC50 = > 50 µM; ZAP-70: IC50 = > 50 µM; Lck64-509 Y394: IC50 = 1 nM; Tyrosine-protein kinase LCK: IC50 = 2 nM (human); Tyrosine-protein kinase BLK: IC50 = 66 nM (Mus musculus); Tyrosine-protein kinase SRC: IC50 = 70 nM (human)
pK Values :
pKb: 5.75
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
WGK Germany :
3
PubChem CID :
6603792
MDL Number :
MFCD04974490
SMILES :
C1CCC(C1)N2C=C(C3=C2N=CN=C3N)C4=CC=C(C=C4)OC5=CC=CC=C5

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Certificate of Analysis

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Lck Inhibitor  Product Citations

See how others have used Lck Inhibitor. Click on the entry to view the PubMed entry .

Citations 1 to 3 of 3 total

PMID: # 28250239  Singh, DK. et al. 2017. Reproduction. 153: 655-669.

PMID: # 24135919  Balbin, OA. et al. 2013. Nature communications. 4: 2617.

PMID: # 21487392  Cao, Y. et al. 2011. The EMBO journal. 30: 2083-93.

Citations 1 to 3 of 3 total
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Rated 5 out of 5 by from Moffat et al Moffat et al. (PubMed ID 15032728) used the Lck inhibitor to stimulate cytokine release by inactivating tyrosine kinase activity via the T-cell receptor. -SCBT Publication Review
Date published: 2015-04-07
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