LATS1/2-IN-1
LATS1/2-IN-1 is a potent and selective LATS1 and LATS2 inhibitor. LATS1/2-IN-1 exhibits potent inhibitory activity against LATS1 and LATS2 with IC50 values of 4.4 nM and 5.5 nM as determined via r33P functional assay. LATS1/2-IN-1 displays cellular IC50 values of 136 nM for LATS1 and 36.0 nM for LATS2 as determined via NanoBRET assay. LATS1/2-IN-1 reduces phosphorylation of YAP1 in mouse liver. LATS1/2-IN-1 demonstrates wound healing activity in HT-1080 scratch assay and in vivo SKH1 mouse punch biopsy model. LATS1/2-IN-1 can be used for the study of regenerative medicine indications such as wound healing.
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- CAS No.: 3024011-99-9
- Formule: C26H31F2N3O3S
- Masse moléculaire:503.60
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
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Activité biologique
Description
IC50 & Target
[1]|
YAP1 |
Lats1 |
Lats2 |
LATS1 4.4 nM (IC50, r33P functional assay) |
LATS2 5.5 nM (IC50, r33P functional assay) |
LATS1 136 nM (IC50, NanoBRET assay) |
LATS2 36 nM (IC50, NanoBRET assay) |
LATS1 2.5 nM (Kd) |
LATS2 1.7 nM (Kd) |
In Vitro
LATS1/2-IN-1 (Compound 27) exhibits potent inhibitory activity against LATS1 and LATS2 with IC50 values of 4.4 nM and 5.5 nM as determined via r33P functional assay[1].
LATS1/2-IN-1 displays cellular IC50 values of 136 nM for LATS1 and 36.0 nM for LATS2 as determined via NanoBRET assay[1].
LATS1/2-IN-1 binds to LATS1 and LATS2 with low nanomolar Kd values of 2.5 nM and 1.7 nM as determined via TR-FRET assay[1].
LATS1/2-IN-1 (1 μM, 4 h) induces a 24.8-fold increase in CYR61 mRNA expression in HepG2 cells[1].
LATS1/2-IN-1 (4-500 nM, 16 h) accelerates wound closure in HepG2 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Parmacokinetics
In Vivo
LATS1/2-IN-1 (0.01-1.0 mg/mL in 0.1 mL PF-127 hydrogel, topical, every other day for up to 3 weeks) accelerates dermal wound closure in hairless SKH1 mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Hairless SKH1 mice were used to establish a full-thickness punch biopsy wound model[1]
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Dosage:0.01 mg/mL or 1.0 mg/mL in 0.1 mL PF-127 hydrogel
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Administration:topical, every other day for up to 3 weeks
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Result:Accelerated wound closure at both tested concentrations.
Shortened time to complete wound healing.
Showed consistent efficacy across concentrations.
Chemical Information
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CAS No. 3024011-99-9
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Masse moléculaire 503.60
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Formule C26H31F2N3O3S
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SMILES
O=S1(CCC(N2C[C@@H](C)[C@](O)(C3=C(C)C=C(C4=C5C(NC=C5F)=NC=C4)C=C3F)[C@@H](C)C2)CC1)=O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
LATS1/2-IN-1 Related Classifications
HY-175649 Related Classifications
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