1. Stem Cell/Wnt
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  3. 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.

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

LATS1/2-IN-1

LATS1/2-IN-1 Chemical Structure

CAS No. : 3024011-99-9

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Description

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[1].

IC50 & Target[1]

YAP1

 

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.

In Vivo

LATS1/2-IN-1 (Compound 27) (30 mg/kg, i.p., single dose) significantly reduces the phosphorylation level of YAP1 at serine 397 (p-YAP1 S397) in mouse liver homogenates[1].
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.

Animal Model: Hairless SKH1 mice were used to establish a full-thickness punch biopsy wound model[1]
Dosage: 0.01 mg/mL or 1.0 mg/mL in 0.1 mL PF-127 hydrogel
Administration: topical, every other day for up to 3 weeks
Result: Accelerated wound closure at both tested concentrations.
Shortened time to complete wound healing.
Showed consistent efficacy across concentrations.
Molecular Weight

503.60

Formula

C26H31F2N3O3S

CAS No.
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

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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LATS1/2-IN-1 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.

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LATS1/2-IN-1
Cat. No.:
HY-175649
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