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Chemical Structure| 934593-90-5 Chemical Structure| 934593-90-5

Structure of LW6
CAS No.: 934593-90-5

Chemical Structure| 934593-90-5

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LW6 (HIF-1α inhibitor) is a novel HIF-1 inhibitor with an IC50 of 4.4 μM, decreasing HIF-1α protein expression without affecting HIF-1β expression.

Synonyms: HIF-1α inhibitor; LW8; Hypoxia-Inducible Factor-1α Inhibitor

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Product Details of LW6

CAS No. :934593-90-5
Formula : C26H29NO5
M.W : 435.51
SMILES Code : O=C(OC)C1=CC=C(O)C(NC(COC2=CC=C(C34CC5CC(C4)CC(C5)C3)C=C2)=O)=C1
Synonyms :
HIF-1α inhibitor; LW8; Hypoxia-Inducible Factor-1α Inhibitor
MDL No. :MFCD09907563

Safety of LW6

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

Related Pathways of LW6

epigenetics

Isoform Comparison

Biological Activity

Target
  • HIF

    HIF, IC50:4.4 μM

In Vitro:

Cell Line
Concentration Treated Time Description References
HeLa cells 20 µM 3 days LW6 significantly suppressed the growth of HeLa cells, but not significantly at 2–10 µM. PMC10855897
3T3-L1 cells 2–20 µM 3 days LW6 at 2–20 µM significantly promoted glucose uptake in 3T3-L1 cells, with the strongest effect at 10 µM. PMC10855897
661W photoreceptor cells 25 µM 12 hours LW6 inhibited HIF-1α expression, reduced BNIP3 and FUNDC1 protein levels, decreased the LC3-II/LC3-I ratio, and upregulated P62 PMC8591297
MIO-M1 Müller cells 25 µM 12 hours LW6 inhibited HIF-1α expression, reduced BNIP3 and FUNDC1 protein levels, decreased the LC3-II/LC3-I ratio, and upregulated P62 PMC8591297
human umbilical vein endothelial cells (HUVECs) 25 µM 12 hours LW6 inhibited HIF-1α expression, reduced BNIP3 and FUNDC1 protein levels, decreased the LC3-II/LC3-I ratio, and upregulated P62 PMC8591297
Caco-2 cells 5 µM 120 minutes To study the permeability of LW6 in Caco-2 cells, the results showed that the permeability of LW6 in Caco-2 cells was 2.1 × 10^-6 cm/s, indicating that it is likely to be moderately permeable in the intestine. PMC8070284

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
C57BL/6J mice oxygen-induced retinopathy (OIR) model intravitreal injection 30 mg/kg twice daily for 11 days LW6 inhibited HIF-1α expression, reduced BNIP3 and FUNDC1 protein levels, decreased the LC3-II/LC3-I ratio, and upregulated P62 PMC8591297
BALB/c nude mice OSCC lymph node metastasis model Intraperitoneal injection 7.5mg/kg Monday, Wednesday, Friday, for 3 weeks To investigate the inhibitory effect of LW6 on OSCC lymph node metastasis, the combination of LW6 and DAC significantly reduced the weight and volume of lymph nodes. PMC11743850
ICR mice Male ICR mice Intravenous and oral 1 mg/kg/day Once daily for 28 days To study the pharmacokinetics and metabolism of LW6 in mice, the results showed that LW6 was rapidly converted to its active metabolite APA in mice, and the oral bioavailability was low (1.7 ± 1.8%). PMC8070284

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.30mL

0.46mL

0.23mL

11.48mL

2.30mL

1.15mL

22.96mL

4.59mL

2.30mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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