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Cat. No.: HY-144720

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YH-IV-173

YH-IV-173 is a BRG1 (SMARCA4) bromodomain binder with higher affinity for BRG1 than for BRM. YH-IV-173 acts as a sensitizing agent when combined with Temozolomide (HY-17364), modulating glioblastoma (GBM) cell proliferation and tumor growth. YH-IV-173 treatment alone shows weak effects on glioblastoma cell growth and tumor growth.

For research use only. We do not sell to patients.

CAS No.: 2616813-99-9
Formula: C₂₀H₁₉FN₂O
Molecular Weight:322.38

Storage:

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

Data Sheet (278 KB)

YH-IV-173 Chemical Structure

CAS No.: 2616813-99-9

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Use of MCE Products

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

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References
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Biological Activity

Description

IC₅₀ & Target

^[1]

BRG1

All SWI/SNF Complex Isoforms :

In Vitro

ApoptosisAnti-cancerOthers

Apoptosis

Anti-cancer

YH-IV-173 (11d) (48 h) potently sensitizes MT330 human glioblastoma cells to Temozolomide (TMZ) (HY-17364)-induced apoptosis^[1].

Anti-cancer

YH-IV-173 (up to 7 days) potently enhances the antiproliferative effect of Temozolomide in LN229 human glioblastoma cells^[1].

Others

YH-IV-173 (30 μM; 3 hr) binds to the BRG1 bromodomain in MT330 human glioblastoma cells, as demonstrated by increased protein thermostability in CETSA^[1].

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

In Vivo

Anti-cancer

YH-IV-173 (compound 11d) (10 mg/kg; i.p.; once weekly) exhibits very weak antitumor activity in the subcutaneous GBM xenograft model, but enhances the antitumor effect of Temozolomide (TMZ) (HY-17364)^[1].

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

Animal Model:

NOD.Cg-Prkdcscid Il2rgtm1Wjl/SzJ (NSG) (female; five-week-old; ~25 g; subcutaneous flank xenograft model established via flank injection of luciferase-expressing MT330 GBM cells)^[1]
Dosage:

10 mg/kg
Administration:

i.p.; weekly; initiated 1 week after tumor cell injection
Result:

Exhibited only a slight inhibitory effect on subcutaneous GBM tumor growth as a single agent.
Resulted in tumor volume reaching 1000 mm³ by 3 weeks post-administration as a single agent, requiring euthanasia of mice.
When combined with Temozolomide, produced a tumor growth inhibitory effect.

Related Protocols :

Chemical Information

CAS No. 2616813-99-9
Molecular Weight 322.38
Formula C₂₀H₁₉FN₂O
SMILES

O=C(/C=C/N1[C@@H]2C[C@H](C1)N(C3=CC=C(F)C=C3)C2)C4=CC=CC=C4
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

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (278 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]. He Y, et al. Novel structural-related analogs of PFI-3 (SRAPs) that target the BRG1 catalytic subunit of the SWI/SNF complex increase the activity of temozolomide in glioblastoma cells. Bioorganic & medicinal chemistry. 2022 Jan 01;53:116533. [Content Brief]

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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.

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Biological Activity
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- In Vitro
- In Vivo
Chemical Information
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YH-IV-173

All SWI/SNF Complex Isoforms

Biological Activity

Description

IC50 & Target

In Vitro

In Vivo

Chemical Information

Purity & Documentation

References

Calculators

Help & FAQs

YH-IV-173 Related Classifications

HY-144720 Related Classifications

Bioz

Keywords

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