2. Protein Tyrosine Kinase/RTK Stem Cell/Wnt JAK/STAT Signaling Epigenetics
  3. FLT3 JAK c-Kit
  4. JI6

JI6 is a potent, selective and orally active FLT3 inhibitor, with IC50s of ～40, 8, and 4 nM for FLT3-WT, FLT3-D835Y, and FLT3-D835H, respectively. JI6 also inhibits JAK3 and c-Kit, with IC50s of ～250 and ～500 nM, respectively. JI6 can be used for the research of acute myeloid leukemia.

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JI6

JI6 Chemical Structure

CAS No. : 856436-16-3

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Based on 1 publication(s) in Google Scholar

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Description

JI6 is a potent, selective and orally active FLT3 inhibitor, with IC50s of ～40, 8, and 4 nM for FLT3-WT, FLT3-D835Y, and FLT3-D835H, respectively. JI6 also inhibits JAK3 and c-Kit, with IC50s of ～250 and ～500 nM, respectively. JI6 can be used for the research of acute myeloid leukemia[1].

IC50 & Target[1]

FLT3-D835H

4 nM (IC50)

FLT3-D835Y

8 nM (IC50)

FLT3-WT

40 nM (IC50)

JAK3

~250 nM (IC50)

c-Kit

~500 nM (IC50)

In Vitro

JI6 (3-1000 nM; 1-4 days) selectively inhibits the viability of MV4-11 cells in a dose-dependent manner, with an IC50 of ～25 nM[1].
JI6 (1-2000 nM; 48 h) potently inhibits the viability of HCD-57 cells expressing FLT3-ITD, FLT3-D835Y, and FLT3-D835H with IC50s of ～40 nM, but it displays essentially no effects on the parent HCD-57 or the cells transformed with JAK2V617F[1].
JI6 (100-500 nM; 24 h) induces apoptosis and cell cycle arrest in both FLT3-ITD- and FLT3-D835Y-expressing HCD-57 cells[1].
JI6 (50-500 nM; 3 h) inhibits phosphorylation of FLT3 and its downstream signaling transducers including ERK and Akt in FLT3-ITD- and FLT3-D835Y-transfromed HCD-57 cells[1].

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

JI6 Related Antibodies

Cell Viability Assay[1]

Cell Line: MV4-11, HL60, Karpas 299, and Jurkat cells
Concentration: 3-1000 nM
Incubation Time: 48 hours
Result: Inhibited MV4-11 cells and no effects of JI6 on the three remaining cells at a concentration as high as 1 μM.

Apoptosis Analysis[1]

Cell Line: FLT3-ITD- and FLT3-D835Y-transformed HCD-57 cells
Concentration: 100, 500 nM
Incubation Time: 24 hours
Result: Increased the percentage of apoptotic and necrotic cells and displayed no effects on the apoptosis of the parent HCD-57 cells.

Cell Cycle Analysis[1]

Cell Line: FLT3-ITD- and FLT3-D835Y-transformed HCD-57 cells
Concentration: 100, 500 nM
Incubation Time: 24 hours
Result: Significantly reduced G2 and S phase cells and increased G1 phase cells in both FLT3-ITD and D835Y cells.

Cell Viability Assay[1]

Cell Line: FLT3-ITD- and FLT3-D835Y-transformed HCD-57 cells
Concentration: 50, 100, 500 nM
Incubation Time: 3 hours
Result: Inhibited phosphorylation of FLT3, ERK1, ERK2 and Akt.
In Vivo

JI6 (15 mg/kg; i.p. daily for 3 weeks) inhibits the proliferation of FLT3-D835Y-transformed HCD-57 in immunodeficient mice and prolongs the mice survival[1].
JI6 (25 mg/kg; p.o. daily for 3 weeks) suppresses myeloproliferative phenotypes in FLT3-ITD knock-in mice[1].
JI6 (100 mg/kg; a single i.p.) significantly inhibits phosphorylation of FLT3 and downstream signal transductionin mice expressing FLT3-D835Y[1].

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

Animal Model: NSG mice (10-12 weeks old, male) were implanted with FLT3-D835Y-transformed HCD-57 cells[1]
Dosage: 15 mg/kg
Administration: I.p. daily for 3 weeks
Result: Reduced the spleen size and prolonged the survival of these mice.
Molecular Weight

383.42

Formula

C19H17N3O4S
CAS No.
SMILES

O=C1NC2=CC=C(C3=CN=CC=C3)C=C2/C1=C/C4=CC=CN4.O=S(O)(C)=O
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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JI6 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:

JI6856436-16-3JI 6JI-6FLT3JAKc-KitCluster of differentiation antigen 135CD135Fms like tyrosine kinase 3Janus kinaseSCFRCD117acute myeloid leukemiaAMLInhibitorinhibitorinhibit

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