2. Protein Tyrosine Kinase/RTK PI3K/Akt/mTOR MAPK/ERK Pathway Stem Cell/Wnt Immunology/Inflammation GPCR/G Protein Apoptosis
  3. Btk Akt mTOR p38 MAPK ERK CCR Apoptosis
  4. PLS-123

LPS-123 is a covalently irreversible BTK inhibitor with an IC50 of < 5 nM. LPS-123 simultaneously inhibits the catalytic activity of BTK at Tyr551 and its self-activation at Tyr223. LPS-123 inhibits phosphorylation of the AKT/mTOR and MAPK signaling pathways, activation of PLCγ2, ERK1/2, p38, AKT, and mTOR, and blocks the production of CCL3 and CCL4 chemokines. LPS-123 exhibits significant anti-proliferative activity against various B-cell lymphoma cell lines and effectively induces apoptosis via a caspase-dependent pathway. LPS-123 also demonstrates significant antitumor activity in the OCI-Ly7 xenograft model. LPS-123 can be used for lymphoma research.

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

PLS-123

PLS-123 Chemical Structure

CAS No. : 1431727-04-6

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PLS-123 Related Antibodies

Top Publications Citing Use of Products

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Akt Akt1 Akt2 Akt3

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mTOR mTORC1 mTORC2

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p38 MAPK Akt1 p38α p38β MAPK13 p38δ p38γ

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ERK ERK1 ERK2 ERK5 ERK8

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CCR1 CCR2 CCR3 CCR4 CCR5 CCR6 CCR7 CCR8 CCR9

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Description

LPS-123 is a covalently irreversible BTK inhibitor with an IC50 of < 5 nM. LPS-123 simultaneously inhibits the catalytic activity of BTK at Tyr551 and its self-activation at Tyr223. LPS-123 inhibits phosphorylation of the AKT/mTOR and MAPK signaling pathways, activation of PLCγ2, ERK1/2, p38, AKT, and mTOR, and blocks the production of CCL3 and CCL4 chemokines. LPS-123 exhibits significant anti-proliferative activity against various B-cell lymphoma cell lines and effectively induces apoptosis via a caspase-dependent pathway. LPS-123 also demonstrates significant antitumor activity in the OCI-Ly7 xenograft model. LPS-123 can be used for lymphoma research[1].

Cellular Effect
Cell Line Type Value Description References
Ramos IC50
13 nM
Compound: 38
Inhibition of Btk in human Ramos cells assessed as inhibition of PLC-gamma2 phosphorylation at Tyr1217 after 1 hr by Western blot analysis
Inhibition of Btk in human Ramos cells assessed as inhibition of PLC-gamma2 phosphorylation at Tyr1217 after 1 hr by Western blot analysis
[PMID: 24915291]
Ramos IC50
13 nM
Compound: 38
Inhibition of Btk phosphorylation at Tyr551 in human Ramos cells after 1 hr by Western blot analysis
Inhibition of Btk phosphorylation at Tyr551 in human Ramos cells after 1 hr by Western blot analysis
[PMID: 24915291]
Molecular Weight

617.58

Formula

C31H26F3N7O4
CAS No.
SMILES

O=C(NC1=CN=C(NC2=CC=CC(NC(CNC(C=C)=O)=O)=C2)N=C1)C3=CC(NC(C4=CC=CC(C(F)(F)F)=C4)=O)=CC=C3C
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Room temperature in continental US; may vary elsewhere.
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Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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PLS-123 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.

Keywords:

PLS-1231431727-04-6PLS123PLS 123BtkAktmTORp38 MAPKERKCCRApoptosisBruton tyrosine kinasePKBProtein kinase BMammalian target of RapamycinExtracellular signal regulated kinasesCC chemokine receptorInhibitorinhibitorinhibit

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