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Cat. No.: HY-187181

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GNE-2181

GNE-2181 is an orally active, blood-brain barrier-penetrant pan-TEAD transcription factor inhibitor, with IC₅₀ values of 13, 26, 61 and 17 nM against TEAD1, TEAD2, TEAD3 and TEAD4, respectively. GNE-8021 allosterically disrupts the TEAD-YAP/TAZ interaction and inhibits TEAD-mediated oncogenic transcriptional programs via the Hippo signaling pathway. GNE-8021 suppresses YAP-driven tumor cell growth. GNE-2181 inhibits the growth of intracranial tumor models in vivo. GNE-2181 can be used for research on brain metastasis of lung cancer.

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CAS No.: 2933893-78-6
화학식: C₂₀H₁₆F₄N₄O₃
분자량:436.36

보관:

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

GNE-2181 Chemical Structure

CAS No.: 2933893-78-6

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
- Parmacokinetics
- In Vivo
Chemical Information
순도&문서
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

제품 설명

IC₅₀ & Target^[1]

TEAD1

13 nM (IC₅₀)

TEAD2

26 nM (IC₅₀)

TEAD3

61 nM (IC₅₀)

TEAD4

17 nM (IC₅₀)

All YAP Isoforms :

All Hippo (MST) Isoforms :

In Vitro

GNE-8021 (overnight) potently inhibits the binding of YAP to purified TEAD1, TEAD2, TEAD3, and TEAD4 proteins, with IC₅₀ values of 2, 4, 8, and 6 nM, respectively^[1].
GNE-2181 (6 days) potently inhibits the proliferation of Hippo pathway-dependent NCI-H226 and MSTO-211H mesothelioma cells, with EC₅₀ values of 3 nM and 7 nM, respectively, while it exhibits only extremely low activity against Hippo pathway-independent VMRC-LCD cells^[1].
GNE-2181 (7-14 days) potently and dose-dependently inhibits colony formation of Hippo pathway-dependent NCI-H226 mesothelioma cells in soft agar, while exerting no significant effect on Hippo pathway-independent ES-2 cells^[1].
GNE-2181 (48 h) downregulates YAP/TAZ-dependent proliferation-related and MAPK-related gene programs in Hippo pathway-dependent NCI-H226 mesothelioma cells, but exerts no effect on Hippo pathway-independent ES-2 cells^[1].
GNE-2181 (6 days) combined with various MAPK pathway inhibitors yields synergistic benefits across multiple cancer cell lines, and particularly exhibits strong synergy with KRAS^G12C inhibitors in KRAS^G12C-mutant NCI-H2122 cells^[1].
GNE-2181 (1 μM; 48 h) induces G0/G1 cell cycle arrest in Hippo pathway-dependent NCI-H226 and MSTO-211H mesothelioma cells following treatment at 1 μM for 48 h^[1].

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

Cell Cycle Analysis^[1]

Cell Line:

Hippo-dependent NCI-H226 and MSTO-211H mesothelioma cells
Concentration:

1 μM (GNE-2181); 10 μM (EdU)
Incubation Time:

48 h (GNE-2181); 20 min (EdU)
Result:

Induced a G0/G1 cell cycle arrest in both NCI-H226 and MSTO-211H cells, as shown by increased EdU-negative (G1) cells and decreased EdU-positive (S-phase) cells.

Parmacokinetics

Species	Dose	Route	CL_plasma	T_1/2	Bioavailability
Mice^[1]	0.3 mg/kg	i.v.	9.2 mL/h/kg	5.6 h	/
Mice^[1]	1 mg/kg	p.o.	/	5.6 h	88 %

In Vivo

GNE-2181 (10-50 mg/kg; p.o.; daily; 4-21 days) achieves dose-dependent inhibition of YAP/TAZ transcriptional activity and mesothelioma tumor growth in subcutaneous NCI-H226 xenografts, with significant efficacy observed at daily oral doses of 10 mg/kg and above^[1].
GNE-2181 (10-50 mg/kg; p.o.; daily; 21 days) demonstrates brain penetrance and significant efficacy against intracranial lung cancer brain metastases in nude mice, with daily oral doses of 10 mg/kg and 50 mg/kg reducing tumor growth and suppressing YAP/TAZ-dependent proliferation^[1].

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

Animal Model:

C.B-17 SCID mice^[1]
Dosage:

10, 20 and 50 mg/kg
Administration:

p.o.; daily; 4 days or 20 days
Result:

Induced a dose- and exposure-dependent decrease in YAP/TAZ target gene signatures (with maximum inhibition at 50 mg/kg) and proliferation gene signatures, comparable in magnitude to GNE-8025 at 10 mg/kg twice daily.
Showed significant reductions in Ki67 and phospho-histone H3 (pHH3) staining in tumors from mice treated with 20 mg/kg daily, indicating decreased proliferation.
Caused significant tumor growth inhibition starting at 10 mg/kg daily in the 21-day efficacy study, with minimal impact on mouse body weight.

Animal Model:

Nude mice (6-week-old)^[1]
Dosage:

10 mg/kg; 50 mg/kg
Administration:

p.o.; daily; 21 days
Result:

Showed significant reduction in intracranial tumor growth at week 3 post-treatment initiation (adjusted p=0.0049 for 10 mg/kg; adjusted p=0.0047 for 50 mg/kg).
Caused significant decreases in YAP/TAZ target gene expression and reduced Ki67 staining in tumor sections from mice treated with 50 mg/kg daily, indicating suppressed proliferation.
Was well-tolerated, with minimal impact on mouse body weight.

Chemical Information

CAS No. 2933893-78-6
분자량 436.36
화학식 C₂₀H₁₆F₄N₄O₃
SMILES

C=C(C(N1CC(C1)C2=NN(C3=C2C(CO)=CC=N3)C4=CC=C(C=C4)OC(F)(F)F)=O)F
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

Handling Instructions (2659 KB)

References

[1]. Hagenbeek TJ, et al. Covalent pan-TEAD inhibitors block YAP activity and demonstrate brain penetrance in a Hippo-dependent cancer model. Nature communications. 2026 Jun 27. [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

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

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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Amount: USD 0.00

Biological Activity
- 제품 설명
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
순도&문서
References

상품명:
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GNE-2181

All YAP Isoforms

All Hippo (MST) Isoforms