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Chemical Structure| 1392399-03-9 Chemical Structure| 1392399-03-9

Structure of BIX-01294 3HCl
CAS No.: 1392399-03-9

Chemical Structure| 1392399-03-9

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BIX-01294 trihydrochloride is a reversible and highly selective G9a and GLP histone methyltransferase inhibitor, with IC50s of 1.7 μM and 0.9 μM, respectively. It inhibits G9a/GLP by competing for binding with the amino acids N-terminal of the substrate lysine residue. As a (1H-1,4-diazepin-1-yl)-quinazolin-4-yl amine derivative, BIX-01294 trihydrochloride induces necroptosis and autophagy, and exhibits antitumor activity in recurrent tumor cells.

Synonyms: BIX 01294; BIX-01294 trihydrochloride

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Product Details of BIX-01294 3HCl

CAS No. :1392399-03-9
Formula : C28H41Cl3N6O2
M.W : 600.02
SMILES Code : COC1=CC2=NC(N3CCN(C)CCC3)=NC(NC4CCN(CC5=CC=CC=C5)CC4)=C2C=C1OC.[H]Cl.[H]Cl.[H]Cl
Synonyms :
BIX 01294; BIX-01294 trihydrochloride
MDL No. :MFCD16618384
InChI Key :FMURUEPQXKJIPS-UHFFFAOYSA-N
Pubchem ID :46945860

Safety of BIX-01294 3HCl

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Related Pathways of BIX-01294 3HCl

epigenetics

Isoform Comparison

Biological Activity

Target
  • Histone Methyltransferase

    G9a, IC50:2.7 μM

In Vitro:

Cell Line
Concentration Treated Time Description References
Bladder cancer cells (J82) 2–5 μM Inhibited cell proliferation PMC7409321
Bone cancer cells (U2OS) 2–5 μM Inhibited cell proliferation PMC7409321
Brain cancer cells (U251) 2–5 μM Inhibited cell proliferation PMC7409321
Breast cancer cells (MCF10A and MCF7) 2–5 μM Inhibited cell proliferation PMC7409321
Cervical cancer cells (HeLa) 2–5 μM Inhibited cell proliferation PMC7409321
Colon cancer cells (HCT116 and RKO) 2–5 μM Inhibited cell proliferation PMC7409321
Liver cancer cells (Hep2G) 2–5 μM Inhibited cell proliferation PMC7409321
Lung cancer cells (H1299) 2–5 μM Inhibited cell proliferation PMC7409321
Sympathetic nervous system cancer cells (BE(2)-C, SMS-KCNR, SHEP1) 2–5 μM Inhibited cell proliferation PMC7409321
KG1 cells 10 μM 48 hours BIX-01294 activated the PERK/NRF2 pathway in KG1 cells, leading to HO-1 upregulation, suppression of p38 phosphorylation and ROS generation, thereby limiting its induced apoptosis. PMC7158163
U937 cells 10 μM 48 hours BIX-01294 significantly induced phosphorylation of p38 and triggered apoptosis in U937 cells. PMC7158163
DPSCs 1 μM 2 weeks BIX-01294 significantly promotes chondrogenic differentiation of DPSCs, as indicated by increased expression levels of cartilage-signature markers and markedly increased proteoglycans. PMC10460901
Rabbit aortic vascular smooth muscle cells (RAVSMCs) 5 μM 24 hours BIX-01294 treatment resulted in reduced numbers of RAVSMCs, and this effect was independent of cell proliferation and apoptosis. PMC7053323
Human aortic vascular smooth muscle cells (HAVSMCs) 5 μM 24 hours BIX-01294 treatment resulted in reduced numbers of HAVSMCs, and this effect was independent of cell proliferation and apoptosis. PMC7053323
HEY cells 5 μM 24 hours BIX-01294 significantly increased the expression of SLC31A1 in ZNF711-downregulated EOC cells and reduced the IC50 value of CDDP, enhancing CDDP sensitivity. PMC8441092
SKOV3 cells 5 μM 24 hours BIX-01294 significantly increased the expression of SLC31A1 in ZNF711-downregulated EOC cells and reduced the IC50 value of CDDP, enhancing CDDP sensitivity. PMC8441092

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Nude mice Intra-peritoneal tumor model Intra-peritoneal injection 30 mg/kg daily, continuous treatment BIX-01294 significantly inhibited tumor growth in ZNF711-downregulated EOC cells and prolonged the survival time of tumor-bearing mice. PMC8441092

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.67mL

0.33mL

0.17mL

8.33mL

1.67mL

0.83mL

16.67mL

3.33mL

1.67mL

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