2. PROTAC Stem Cell/Wnt Apoptosis
  3. PROTACs YAP c-Myc Apoptosis
  4. H122

H122 is a PROTAC degrader for TEAD that degrades TEAD1 with a DC50 of 3 nM. H122 exhibits good affinity to TEAD2, TEAD3, and TEAD4 with Ki values of 2.0, 3.6 and 1.6 nM, respectively. H122 relies on binding to TEAD1 and CRBN, functional E3 ligase activity, and a functional proteasome for degradation.H122 induces degradation of TEAD3 and forms a ternary complex with TEAD4 and CRBN/DDB1 to mediate degradation.H122 downregulates expression of Myc target genes. H122 exhibits antitumor efficacy in MSTO-211H mouse xenograft models.H122 can be used for the research of malignant mesothelioma.
(Pink: TEAD ligand (HY-151525); Blue: Cereblon ligand (HY-W087383); Black: linker).

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

H122

H122 Chemical Structure

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Based on 1 publication(s) in Google Scholar

H122 Related Antibodies

Top Publications Citing Use of Products

View All PROTACs Isoform Specific Products:

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von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

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YAP/TAZ YAP/TAZ-TEAD TEAD YAP1

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

H122 is a PROTAC degrader for TEAD that degrades TEAD1 with a DC50 of 3 nM. H122 exhibits good affinity to TEAD2, TEAD3, and TEAD4 with Ki values of 2.0, 3.6 and 1.6 nM, respectively. H122 relies on binding to TEAD1 and CRBN, functional E3 ligase activity, and a functional proteasome for degradation.H122 induces degradation of TEAD3 and forms a ternary complex with TEAD4 and CRBN/DDB1 to mediate degradation.H122 downregulates expression of Myc target genes. H122 exhibits antitumor efficacy in MSTO-211H mouse xenograft models.H122 can be used for the research of malignant mesothelioma[1]. (Pink: TEAD ligand (HY-151525); Blue: Cereblon ligand (HY-W087383); Black: linker).

In Vitro

H122 (Compound 40) binds potently to human TEAD1, TEAD2, TEAD3, and TEAD4 proteins in vitro, with highest affinity for TEAD1 (Ki = 0.3 nM)[1].
H122 promotes the formation of a ternary complex between TEAD4 and the CRBN/DDB1 E3 ligase complex in vitro, a key step for PROTAC-mediated degradation[1].
H122 (4 days) potently inhibits the growth of MSTO-211H and NCI-H226 cancer cell lines in vitro, with higher activity in NCI-H226 cells (IC50 = 0.6 nM)[1].
H122 (10-100 nM; 1-24 h) potently and rapidly degrades TEAD1, TEAD3, and TEAD4 proteins in MSTO-211H and NCI-H226 cancer cells, with TEAD1 degradation DC50 = 3.0 nM in MSTO-211H cells[1].
H122 (0.1-1000 nM; 4 h) suppresses the expression of TEAD target genes in MSTO-211H cells in vitro in a dose-dependent manner, confirming inhibition of TEAD transcriptional activity[1].
H122 (100 nM; 4 h) induces widespread transcriptional reprogramming in MSTO-211H cells, with significant downregulation of Myc target genes and other TEAD-associated oncogenic genes[1].
H122 (1-1000 nM; 24 h (cell cycle), 48 h (apoptosis)) induces G1 cell cycle arrest and apoptosis in MSTO-211H cancer cells, contributing to its antiproliferative activity[1].

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

H122 Related Antibodies

Western Blot Analysis[1]

Cell Line: MSTO-211H and NCI-H226 cells
Concentration: 10 nM (both cell lines); 10, 100 nM (MSTO-211H cells); 100 nM (NCI-H226 cells)
Incubation Time: 1, 2, 4, 6, 8, 12, 24 h (10 nM treatment)
Result: Induced rapid degradation of TEAD1, TEAD3, and TEAD4 in both cell lines.
Achieved degradation half-life (t1/2) values: MSTO-211H (TEAD1): 3.52 h, NCI-H226 (TEAD1): 1.83 h.
Reached TEAD1 degradation DC50 in MSTO-211H cells: 3.0 nM.

Real Time qPCR[1]

Cell Line: MSTO-211H cells
Concentration: 0.1 nM, 1 nM, 10 nM, 100 nM, 1000 nM
Incubation Time: 4 h
Result: Dose-dependently downregulated mRNA levels of TEAD target genes CYR61, CTGF, ANKRD1, and NPPB.

Apoptosis Analysis[1]

Cell Line: MSTO-211H cells
Concentration: 1 nM, 10 nM, 100 nM, 1000 nM
Incubation Time: 48 h
Result: Induced significant apoptosis at 100 nM after 48 h treatment.

Cell Cycle Analysis[1]

Cell Line: MSTO-211H cells
Concentration: 1 nM, 10 nM, 100 nM, 1000 nM
Incubation Time: 24 h
Result: Arrested cell cycle at the G1 phase at 10 nM after 24 h treatment.
Parmacokinetics
Species Dose Route T1/2 Cmax AUC0-t AUC0-∞ MRT Bioavailability C0 Vz CL Vss
Mice[1] 5 mg/kg i.v. 1.94 h / 1215 ng·h/mL 1237 ng·h/mL 0.69 h / 5691 ng/mL 11.5 L/kg 70.6 mL/min/kg 3.79 L/kg
Mice[1] 10 mg/kg i.p. 2.68 h 1157 ng/mL 2960 ng·h/mL 3001 ng·h/mL 2.76 h 121 % / / / /
Mice[1] 5 mg/kg p.o. / 7.86 ng/mL 5.39 ng·h/mL / 0.51 h 0.44 % / / / /
In Vivo

H122 (Compound 40) (10-50 mg/kg; i.p.; daily for 21 days, single injection) significantly degrades TEAD1 in MSTO-211H xenograft tumor tissues and inhibits tumor growth in a dose-dependent manner, with the 20 mg/kg daily i.p. dose yielding a T/C value of 37.7% and no associated body weight loss[1].

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

Animal Model: BALB/c nude (female, 5-6 weeks old, MSTO-211H cell xenograft model)[1]
Dosage: 10 mg/kg; 20 mg/kg; 50 mg/kg
Administration: i.p.; daily for 21 days (10, 20 mg/kg); single injection (50 mg/kg)
Result: Significantly reduced TEAD1 levels in MSTO-211H tumor tissues (TEAD3/4 degradation was less pronounced, TEAD2 was undetectable) with a single 50 mg/kg i.p.
dose.
Resulted in a tumor volume T/C value of 37.7% (markedly reduced tumor growth compared to control) with daily 20 mg/kg i.p.
treatment for 21 days.
Inhibited tumor growth, with less robust efficacy than the 20 mg/kg dose, with daily 10 mg/kg i.p.
treatment for 21 days.
Observed no loss of body weight in treated mice, indicating good tolerance.
Led to persistent reduction of TEAD1 levels in tumor tissues with prolonged 20 mg/kg treatment.
Clinical Trial
Molecular Weight

838.32

Formula

C45H45ClFN5O8
Appearance

Solid

Color

Light yellow to yellow

SMILES

COCCOC1=C([C@@]([C@@]2=C(C=CC3=C2C[C@@](C4=CC=CC=C4)(O3)CNCCC5CCN(CC5)C6=CC=C(C7=C6)C(N(C7=O)C8C(NC(CC8)=O)=O)=O)Cl)=C(C=C1)C(N)=O)F
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (119.29 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.1929 mL 5.9643 mL 11.9286 mL
5 mM 0.2386 mL 1.1929 mL 2.3857 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

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C2

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Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (2.98 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (2.98 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
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% 
+
%
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Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 98.33%

SDS (252 KB)

COA (250 KB) HNMR (149 KB) RP-HPLC (241 KB) LCMS (237 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.1929 mL 5.9643 mL 11.9286 mL 29.8215 mL
5 mM 0.2386 mL 1.1929 mL 2.3857 mL 5.9643 mL
10 mM 0.1193 mL 0.5964 mL 1.1929 mL 2.9822 mL
15 mM 0.0795 mL 0.3976 mL 0.7952 mL 1.9881 mL
20 mM 0.0596 mL 0.2982 mL 0.5964 mL 1.4911 mL
25 mM 0.0477 mL 0.2386 mL 0.4771 mL 1.1929 mL
30 mM 0.0398 mL 0.1988 mL 0.3976 mL 0.9941 mL
40 mM 0.0298 mL 0.1491 mL 0.2982 mL 0.7455 mL
50 mM 0.0239 mL 0.1193 mL 0.2386 mL 0.5964 mL
60 mM 0.0199 mL 0.0994 mL 0.1988 mL 0.4970 mL
80 mM 0.0149 mL 0.0746 mL 0.1491 mL 0.3728 mL
100 mM 0.0119 mL 0.0596 mL 0.1193 mL 0.2982 mL
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H122 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

H122H 122H-122PROTACsYAPc-MycApoptosisYes-associated proteinMycTEAD3NCI-H226proteasomeTEAD familyTEAD4TEAD1MSTO-211Hmalignant mesotheliomaCRBNMyc target genesInhibitorinhibitorinhibit

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