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Chemical Structure| 199596-05-9 Chemical Structure| 199596-05-9

Structure of JIB-04
CAS No.: 199596-05-9

Chemical Structure| 199596-05-9

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JIB-04 is a pan-selective inhibitor of Jumonji histone demethylases, with IC50s of 230 nM for JARID1A, 340 nM for JMJD2E, 855 nM for JMJD3, 445 nM for JMJD2A, 435 nM for JMJD2B, 1100 nM for JMJD2C, and 290 nM for JMJD2D.

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Product Details of JIB-04

CAS No. :199596-05-9
Formula : C17H13ClN4
M.W : 308.76
SMILES Code : ClC1=CN=C(N/N=C(C2=CC=CC=C2)/C3=NC=CC=C3)C=C1
InChI Key :YHHFKWKMXWRVTJ-OQKWZONESA-N
Pubchem ID :6519698

Safety of JIB-04

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H320-H335
Precautionary Statements:P261-P280-P301+P312-P302+P352-P305+P351+P338

Related Pathways of JIB-04

epigenetics

Isoform Comparison

Biological Activity

Target
  • KDM4

    JMJD2D, IC50:290 nM

    JMJD2E, IC50:435 nM

  • KDM6

    JMJD3, IC50:855 nM

  • KDM5

    JARID1A, IC50:230 nM

In Vitro:

Cell Line
Concentration Treated Time Description References
Nalm6 cells 0.5 μM 24 hours JIB-04 increased G9a methylation PMC6180122
Nalm6 cells 0.25 μM 72 hours JIB-04 increased the sensitivity of cells to dexamethasone-induced cell death PMC6180122
SCLC cell lines 0.04 µM to 0.49 µM 4 days JIB-04 significantly decreased the viability of SCLC cell lines, particularly in etoposide-resistant lines PMC11405284
PC-3 cells 260 nM 48 hours Evaluate the effect of JIB-04 on PC-3 cells, results showed that JIB-04 decreased EphA2 expression and increased the silencing efficiency of siEphA2. PMC7938557
DU145 cells 260 nM 48 hours Evaluate the effect of JIB-04 on DU145 cells, results showed that JIB-04 decreased EphA2 expression and increased the silencing efficiency of siEphA2. PMC7938557
H358 non-small cell lung cancer cells 500 nM 24 hours JIB-04 E-isomer specifically upregulates anti-growth genes and downregulates pro-growth genes in H358 cells, while no similar changes were observed in normal cells. PMC3724450
HCC4017 non-small cell lung cancer cells 0.5 µM 24 hours JIB-04 E-isomer increased H3K4me3 levels at the c10orf10 promoter in HCC4017 cells. PMC3724450
LN229 cells 0.1735 µM 24, 48, 72, 96 hours JIB-04 inhibited the proliferation of LN229 cells in a dose-dependent manner. PMC10995515
GBM#P3 cells 1.534 µM 24, 48, 72, 96 hours JIB-04 inhibited the proliferation of GBM#P3 cells in a dose-dependent manner. PMC10995515
J-LAT A2 cells 1 µM JIB-04 treatment increases the local H3K36me3 level at LTR nuc-1 PMC6698651
U1/HIV cells 0.25-1 µM JIB-04 treatment increased HIV-1 Gag mRNA level PMC6698651
J-LAT 10.6 cells 0.25–1 µM JIB-04 treatment increased the percentage of GFP-positive cells PMC6698651
J89GFP cells 0.25–1 µM JIB-04 treatment increased the percentage of GFP-positive cells PMC6698651

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Nude mice SCLC tumor xenograft model Oral 75 mg/kg three times a week, for several weeks JIB-04 significantly inhibited the growth of SCLC tumor xenografts, with reduced tumor volume and weight PMC11405284
Nude mice H358 and A549 lung cancer xenograft models Intraperitoneal injection or Oral 110 mg/kg (IP) or 55 mg/kg (oral) 2–3 times weekly for 5 weeks JIB-04 significantly inhibited the growth of H358 and A549 tumors and reduced tumor burden, while showing no significant effects on body weight or overall health of the mice. PMC3724450

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.24mL

0.65mL

0.32mL

16.19mL

3.24mL

1.62mL

32.39mL

6.48mL

3.24mL

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