2. MAPK/ERK Pathway Apoptosis
  3. JNK Apoptosis
  4. YL5084

YL5084, a covalent JNK inhibitor, exhibits selectivity for JNK2 and JNK3 over JNK1 with IC50s of 70 nM, 84 nM and 2173 nM, respectively. YL5084 exhibits JNK2-independent antiproliferative effects and induces apoptosis in a JNK2-independent manner.

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YL5084 Chemical Structure

YL5084 Chemical Structure

CAS No. : 2440199-73-3

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YL5084 Related Antibodies

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Description

YL5084, a covalent JNK inhibitor, exhibits selectivity for JNK2 and JNK3 over JNK1 with IC50s of 70 nM, 84 nM and 2173 nM, respectively. YL5084 exhibits JNK2-independent antiproliferative effects and induces apoptosis in a JNK2-independent manner[1].

IC50 & Target[1]

JNK2

70 nM (IC50)

JNK3

84 nM (IC50)

JNK1

2173 nM (IC50)

In Vitro

YL5084 (0.001-100 μM; 72 h) displays dose-dependent antiproliferative effects with GR50 values of 200-300 nM in MM.1S cells[1].
YL5084 (0.5, 2.5 μM; 24 h) induces apoptosis[1].
YL5084 displays weaker inhibition against PIKFYVE (KD=5000 nM in a KdELECT binding assay) in KINOMEscan[1].
YL5084 has moderate metabolic stability in human and mice microsomes with half-lives of 16 and 11 min, respectively [1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

YL5084 Related Antibodies

Cell Proliferation Assay[1]

Cell Line: Multiple myeloma (MM) cell lines
Concentration: 0.001-100 μM
Incubation Time: 72 h
Result: Displayed dose-dependent antiproliferative effects with GR50 values of 200-300 nM.

Apoptosis Analysis[1]

Cell Line: MM.1S cells
Concentration: 0.5, 2.5 μM
Incubation Time: 24 h
Result: Induced apoptosis as evidenced by an increased level of PARP cleavage, an increased level of cleavage of caspase 3, and an increased level of Annexin V/PI staining.
Molecular Weight

600.71

Formula

C35H36N8O2
CAS No.
SMILES

O=C(C1=CC=C(C=C1)NC(/C=C/CN(C)C)=O)N(C[C@@H]2C)C[C@H]2NC3=NC=CC(C4=C(C=CC=C5)N5N=C4C6=CC=CC=C6)=N3
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Room temperature in continental US; may vary elsewhere.
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Purity & Documentation
References
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YL5084 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:

YL50842440199-73-3YL 5084YL-5084JNKApoptosisc-Jun N-terminal kinaseantiproliferativeMultiple myelomaMM.1SInhibitorinhibitorinhibit

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