2. Stem Cell/Wnt PROTAC
  3. YAP PROTACs
  4. KG-FP-003

KG-FP-003 is a highly potent, selective, and durable TEAD PROTAC degrader (TEAD1 DC50 = 6 ± 4 nM, TEAD2 DC50 = 68 ± 15 nM, TEAD3 DC50 = 12 ± 5 nM, TEAD4 DC50 = 7 ± 5 nM). KG-FP-003 promotes ubiquitination and degradation of TEAD. KG-FP-003 exhibits anticancer activity against mesothelioma and ovarian cancer.
(Pink: TEAD ligand (HY-186118); Blue: Cereblon E3 ligase ligand; Black: linker).

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

KG-FP-003

KG-FP-003 Chemical Structure

CAS No. : 3066008-42-9

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KG-FP-003 Related Antibodies

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YAP/TAZ YAP/TAZ-TEAD TEAD YAP1

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von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

  • Biological Activity

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  • References

  • Customer Review

Description

KG-FP-003 is a highly potent, selective, and durable TEAD PROTAC degrader (TEAD1 DC50 = 6 ± 4 nM, TEAD2 DC50 = 68 ± 15 nM, TEAD3 DC50 = 12 ± 5 nM, TEAD4 DC50 = 7 ± 5 nM). KG-FP-003 promotes ubiquitination and degradation of TEAD. KG-FP-003 exhibits anticancer activity against mesothelioma and ovarian cancer[1]. (Pink: TEAD ligand (HY-186118); Blue: Cereblon E3 ligase ligand; Black: linker).

IC50 & Target[1]

Cereblon

 

TEAD1

6 nM (DC50)

TEAD2

68 nM (DC50)

TEAD3

12 nM (DC50)

TEAD4

7 nM (DC50)

In Vitro

KG-FP-003 binds to recombinant CRBN-DDB1ΔBPB protein with an IC50 of 591 ± 21 nM[1].
KG-FP-003 (3-fold serial dilution starting at 10 μM; 2 h) binds to CRBN in HEK293T cells overexpressing NanoLuc-CRBN, with an IC50 of 962 ± 86 nM in the cellular binding assay[1].
KG-FP-003 (6 h) potently and selectively degrades all four TEAD isoforms in HiBiT-tagged HEK293T cells after 6 h of treatment (TEAD1 DC50 = 6 ± 4 nM, TEAD2 DC50 = 68 ± 15 nM, TEAD3 DC50 = 12 ± 5 nM, TEAD4 DC50 = 7 ± 5 nM)[1].
KG-FP-003 (72 h potently inhibits the proliferation of NCI-H226 mesothelioma cells, with an IC50 of 27 ± 7 nM after 72 h of treatment[1].

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

KG-FP-003 Related Antibodies

Real Time qPCR[1]

Cell Line: MSTO-211H mesothelioma cells
Concentration: 300 nM
Incubation Time: Unclear
Result: Induced dramatic upregulation of the pro-apoptotic gene BMF and downregulation of the TEAD target gene CTGF.

Cell Cycle Analysis[1]

Cell Line: MSTO-211H mesothelioma cells
Concentration: 100-1000 nM
Incubation Time: 24 h
Result: Increased the percentage of cells in G1 phase from 54.3% to 62.1% at 100 nM, and to 65.2% at 1000 nM, indicating G1 phase cell cycle arrest.
Parmacokinetics
Species Dose Route Tmax Cmax T1/2 MRT0-inf AUC0-last AUC0-inf Bioavailability
Mice[1] 2 mg/kg i.v. 0 h 4431 ng/mL 3.57 h 1.4 h 1043 ng·h/mL 1056 ng·h/mL /
Mice[1] 5 mg/kg i.p. 0.42 h 2007 ng/mL 5.42 h 3.13 h 2560 ng·h/mL 2612 ng·h/mL 99 %
In Vivo

KG-FP-003 (3-30 mg/kg; i.p.; once daily; 21 days) exhibits potent dose-dependent antitumor activity in NF2-deficient MSTO-211H mesothelioma xenografts[1].
KG-FP-003 (10-30 mg/kg; i.p.; once daily; 21 days) induces significant tumor regression in ES2 ovarian carcinoma xenografts at doses of 10 mg/kg and 30 mg/kg[1].

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

Animal Model: BALB/c nude (6-week-old)[1]
Dosage: 3 mg/kg; 10 mg/kg; 30 mg/kg
Administration: i.p.; once daily; 21 days
Result: Induced pronounced degradation of TEAD1 protein and significant tumor growth inhibition compared to vehicle controls.
Achieved a tumor growth inhibition (TGI) rate of 118% at 10 mg/kg.
Achieved a TGI rate of 129% at 30 mg/kg.
Maintained stable body weights in all treated mice throughout the 21-day treatment period.
Molecular Weight

1049.64

Formula

C58H67ClF2N6O8
CAS No.
SMILES

CNC(C1=[C@](C(F)=C2C(C[C@@H]([C@@H]2O)C)=C1)[C@]3=C(C(F)=CC4=C3C[C@@](C5=CC=CC=C5)(O4)CNC6CCC(CC6)C(N7CCC(CC7)CC8CCN(CC8)C(COC9=CC=C(C(C)=C9)N%10CCC(NC%10=O)=O)=O)=O)Cl)=O
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
References
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KG-FP-003 Related Classifications

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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:

KG-FP-0033066008-42-9YAPPROTACsYes-associated proteinxenograft modelsHippo signalingCRBNTEAD4malignant pleural mesotheliomaglioblastoma multiformeBALB/c nude miceTEAD2TEAD3ubiquitin-proteasome systemInhibitorinhibitorinhibit

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