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Cat. No.: HY-147195

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QH536

QH536 is a degrader of HMG-CoA reductase (HMGCR) with an EC₅₀ of 0.22 μM. QH536 induces ubiquitination and degradation of HMGCR via the ubiquitin-proteasome pathway, inhibits cholesterol biosynthesis, reduces cholesterol levels, suppresses hepatic stellate cell proliferation, and decreases the expression of fibrotic and inflammatory genes/proteins without inducing intracellular cholesterol accumulation. QH536 can be used in the research of cardiovascular diseases and non-alcoholic steatohepatitis (NASH).

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CAS No.: 2754254-07-2
화학식: C₃₃H₄₉N₃O₃
분자량:535.76

보관:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (286 KB)

QH536 Chemical Structure

CAS No.: 2754254-07-2

Amount: USD 0.00

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- 제품 설명
- IC₅₀ & Target
- In Vitro
Chemical Information
순도&문서
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

제품 설명

IC₅₀ & Target

^[1]

HMGCR

0.22 μM (EC₅₀)

In Vitro

QH536 (compound 29) (16 h) potently promotes HMGCR degradation in CHO-7/HMGCR^TM1-8-GFP cells with an EC₅₀ of 0.22 μM^[1].
QH536 (10 μM; 16 h) does not induce cholesterol accumulation in SV589 human fibroblast cells^[1].
QH536 (0.1-10 μM; 16 h) reverses Lovastatin (HY-N0504)-induced HMGCR accumulation and degrades endogenous HMGCR in CHO-K1 cells with an EC₅₀ of 0.13 μM^[1].
QH536 (1-10 μM; 4-8 h) degrades HMGCR in CHO-K1 cells via the ubiquitin-proteasome pathway, requiring functional ubiquitination sites on HMGCR^[1].
QH536 (0.3-10 μM; 7 days) inhibits cholesterol biosynthesis in CHO-7 cells, leading to growth inhibition that is reversed by exogenous cholesterol^[1].
QH536 (0.1-2 μM; 24 h) dose-dependently reduces TGFβ1-induced fibrotic gene (α-SMA, COL1A1, TIMP1, TGFβ1) and protein (α-SMA) expression in LX-2 hepatic stellate cells, with no effect on quiescent cells^[1].
QH536 (0.1-2 μM; 24 h) dose-dependently lowers TGFβ1-induced cholesterol levels and suppresses TGFβ1-induced proliferation in LX-2 hepatic stellate cells, with no effect on quiescent cells^[1].
QH536 (0.1-2 μM; 24 h) dose-dependently lowers LPS-induced cholesterol levels and suppresses LPS-induced inflammatory gene (TNF-α, IL-6, IL-1β) expression in RAW264.7 murine macrophage cells, with no effect on quiescent cells^[1].

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

Western Blot Analysis^[1]

Cell Line:

CHO-K1 cells
Concentration:

0.1-10 μM (with lovastatin); concentration gradient (sterol-depleted medium)
Incubation Time:

16 h
Result:

Eliminated lovastatin-induced HMGCR accumulation, reducing from 15.2-fold increase to 0.4-fold relative to vehicle in a dose-dependent manner.
Degraded endogenous HMGCR with an EC₅₀ of 0.13 μM.

Western Blot Analysis^[1]

Cell Line:

CHO-K1 cells
Concentration:

1-10 μM (8 h with/without MG-132); 1-10 μM (4 h with mevalonate and MG-132); 1-10 μM (transfected cells)
Incubation Time:

8 h (with/without MG-132); 4 h (with mevalonate and MG-132)
Result:

Had its induced HMGCR degradation completely blocked by the proteasome inhibitor MG-132.
Triggered HMGCR ubiquitination in a dose-dependent manner.
Had its degradation effect completely blocked when HMGCR ubiquitination sites (lysine 89 and 248) were mutated to arginine.

Cell Proliferation Assay^[1]

Cell Line:

LX-2 hepatic stellate cells
Concentration:

0.1 μM; 0.2 μM; 0.5 μM; 1 μM; 2 μM
Incubation Time:

24 h
Result:

Significantly inhibited TGFβ1-induced cholesterol levels and cell proliferation in a dose-dependent manner.
Had no effect on quiescent LX-2 cells (without TGFβ1 stimulation).

Chemical Information

CAS No. 2754254-07-2
분자량 535.76
화학식 C₃₃H₄₉N₃O₃
SMILES

C[C@@](C1=CC2)(CC(C=NN3C(C)=O)=C3C(C)1C)[C@](CC4)([H])[C@]2([H])[C@@](CC[C@]5([H])[C@H](C)CCC(N6CCOCC6)=O)([H])[C@]45C
선적

Room temperature in continental US; may vary elsewhere.
보관

Please store the product under the recommended conditions in the Certificate of Analysis.

순도&문서

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (286 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Li XZ, et al. Synthesis of heterocyclic ring-fused analogs of HMG499 as novel degraders of HMG-CoA reductase that lower cholesterol. European journal of medicinal chemistry. 2022 Jun 05;236:114323. [Content Brief]

Calculators

몰농도 계산기

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

농도 희석 계산기

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Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Bioz

Keywords

MOQ

Minimum order quantity

100 mg

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