1. PI3K/Akt/mTOR
  2. PI3K
  3. LAS191954

LAS191954 is a potent, selective and orally active PI3Kδ inhibitor for inflammatory diseases treatment, with an IC50 of 2.6 nM.

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

LAS191954 Chemical Structure

LAS191954 Chemical Structure

CAS No. : 1403947-26-1

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Description

LAS191954 is a potent, selective and orally active PI3Kδ inhibitor for inflammatory diseases treatment, with an IC50 of 2.6 nM[1].

IC50 & Target[1]

PI3Kδ

2.6 nM (IC50)

Cellular Effect
Cell Line Type Value Description References
HUVEC IC50
295 nM
Compound: 26; LAS191954
Inhibition of PI3Kbeta in HUVEC assessed as reduction in sphingosine-1-phosphate stimulated akt phosphorylation at Ser473 residue preincubated for 15 mins followed by sphingosine-1-phosphate stimulation for 5 mins by HTRF assay
Inhibition of PI3Kbeta in HUVEC assessed as reduction in sphingosine-1-phosphate stimulated akt phosphorylation at Ser473 residue preincubated for 15 mins followed by sphingosine-1-phosphate stimulation for 5 mins by HTRF assay
[PMID: 28105286]
Sf21 IC50
2.6 nM
Compound: 26; LAS191954
Inhibition of full length recombinant human N-terminal His6-tagged PI3K p110delta/human p85alpha expressed in baculovirus infected sf21 cells using PIP2 as substrate preincubated for 30 mins followed by substrate addition by HTRF assay
Inhibition of full length recombinant human N-terminal His6-tagged PI3K p110delta/human p85alpha expressed in baculovirus infected sf21 cells using PIP2 as substrate preincubated for 30 mins followed by substrate addition by HTRF assay
[PMID: 28105286]
THP-1 IC50
7.8 nM
Compound: 26; LAS191954
Inhibition of PI3Kdelta in human THP1 cells assessed as reduction in MCSF-stimulated akt phosphorylation at Thr308 preincubated for 30 mins followed by MCSF stimulation for 3 mins by ELISA
Inhibition of PI3Kdelta in human THP1 cells assessed as reduction in MCSF-stimulated akt phosphorylation at Thr308 preincubated for 30 mins followed by MCSF stimulation for 3 mins by ELISA
[PMID: 28105286]
Molecular Weight

397.39

Formula

C20H15N9O

CAS No.
SMILES

O=C1N(C2=CC=CC=C2)C([C@@H](NC3=C(C#N)C(N)=NC=N3)C)=NN4C1=C(C#N)C=C4

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
References
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LAS191954 Related Classifications

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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.

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Product Name:
LAS191954
Cat. No.:
HY-101114
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