Lck Inhibitor|cas 847950-09-8|DC Chemicals

Cas No.:	847950-09-8
SMILES:	O=C1N(C2=C(C)C=CC=C2C)C3=NC4=CC=CC=C4N3C5=NC(NC6=CC=C(N7CCN(C)CC7)C=C6)=NC=C15
Formula:	C₃₁H₃₀N₈O
M.Wt:	530.6229
Purity:	>98%
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:

Lck Inhibitor is a new class of compounds that are potent inhibitors of Lck with an IC50 value of 7 nM. in vitro: Lck Inhibitor (compound 25) exhibited good potency in the T-cell receptor-induced IL-2 secretion assay (IL- 2) and also inhibited subsequent T-cell proliferation (T-cell prolif.) in the same human T -cells. in vivo: A once daily dose of 25was administered orally at 10, 30, and 60 mg/kg from day 9 today 17. Paw volume was measured daily from day 9 through day 18. The compound showed a dose-dependent inhibition of arthritis, with an ED50 estimated at 24 mg/kg (Figure 6). Based on the measured plasma levels from the three dose groups, the exposure of 25 at the ED50 was estimated to be 2.7 μM·h (Cmax≈ 0.7 μM).

MSDS

COA

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2018-0101

Cat. No.	Product name	Field of application
DC47332	Antiallergic agent-1	Antiallergic agent-1, a Src-family kinase inhibitor, may serve as a new valuable lead compound for future antiallergic drug discovery.
DC46418	CGP77675 hydrate	CGP77675 hydrate is an orally active and potent inhibitor of Src family kinases. CGP77675 hydrate inhibits phosphorylation of peptide substrates and autophosphorylation of purified Src (IC50s of 5-20 and 40 nM, respectively),and also inhibits Src, EGFR, KDR, v-Abl, and Lck with IC50s of 0.02, 0.15, 1.0, 0.31, and 0.29 μM, respectively. Anticancer activity.
DC45824	iHCK-37	iHCK-37 (ASN05260065) is a potent and specific Hck inhibitor with a Ki value of 0.22 μM. iHCK-37 blocks HIV-1 viral replication with an EC50 value of 12.9 μM. iHCK-37 is used for chronic myeloid leukemia (CML) research.
DC45769	EPQpYEEIPIYL	EPQpYEEIPIYL, a phosphopeptide, is a Src homology 2 (SH2) domain ligand. EPQpYEEIPIYL activates Src family members (e.g. Lck, Hck, Fyn) by binding to SH2 domains.
DC45277	Squarunkin A hydrochloride	Squarunkin A hydrochloride is a potent and selective UNC119-cargo interaction inhibitor (IC50 of 10 nM for inhibiting the UNC119A-myristoylated Src N-terminal peptide interaction). Squarunkin A hydrochloride interferes with the activation of Src kinase in cells.
DC44003	Lck-IN-1	Lck-IN-1 is a potent lymphocyte protein tyrosine kinase (Lck) inhibitor extracted from patent WO2007013673A1, example 48.
DC42049	Tyrosine Kinase Peptide 1	Tyrosine Kinase Peptide 1 is a control substrate peptide for c-Src assay.
DC41814	Caffeic acid-pYEEIE TFA	Caffeic acid-pYEEIE TFA, a non-phosphopeptide inhibitor, exhibits potent binding affinity for the GST-Lck-SH2 domain.
DC41813	Caffeic acid-pYEEIE	Caffeic acid-pYEEIE, a non-phosphopeptide inhibitor, exhibits potent binding affinity for the GST-Lck-SH2 domain.
DC41650	Ac-Tyr(PO3H2)-Glu-Glu-Ile-Glu-OH TFA	Ac-Tyr(PO3H2)-Glu-Glu-Ile-Glu-OH TFA (compound 1) is a high-affinity pentapeptide to bind to the src SH2 domain (IC50≈1 μM). Ac-Tyr(PO3H2)-Glu-Glu-Ile-Glu-OH TFA is an inhibitor for src SH3-SH2:phosphoprotein interactions.