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Cat. No.: HY-189122

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Lpi-1

Lpi-1 is an ATP-competitive LATS1/2 inhibitor with IC₅₀ values of 4.4 nM and 1.3 nM, respectively. Lpi-1 blocks LATS-mediated YAP1 phosphorylation. Lpi-1 reversibly inhibits LATS1/2 in cells and in vivo, activating the YAP/TAZ signaling pathway. Lpi-1 can be used for research on acute liver injury and colitis.

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

CAS No.: 2251130-98-8
Formula: C₁₉H₁₃ClFN₃O₂
Molecular Weight:369.78

Storage:

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

Lpi-1 Chemical Structure

CAS No.: 2251130-98-8

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target

^[1]

Lats1

4.4 nM (IC₅₀)

Lats2

1.3 nM (IC₅₀)

Lats1

243.3 nM (Kd)

Lats2

111.6 nM (Kd)

YAP1

TAZ

All YAP Isoforms :

In Vitro

LPi-1 (15 min) is a potent ATP-competitive inhibitor of LATS1 and LATS2 in cell-free ELISA kinase assays, with IC₅₀ values of 4.4 nM and 1.3 nM, respectively^[1].
LPi-1 (30 min) binds directly to LATS1 and LATS2 with K_d values of 243.3 nM and 111.6 nM, respectively^[1].
LPi-1 (100 μM) directly engages LATS1/2 and increases their thermal stability by 8.5°C and 9.5°C^[1].
LPi-1 (0.1-10 μM; 1-8 h) reversibly inhibits LATS1/2, reduces YAP1/TAZ phosphorylation, and promotes nuclear YAP1/TAZ localisation and target gene expression in HepG2 cells; this effect is dose-dependent across multiple cell lines^[1].
LPi-1 (10 days) promotes YAP-dependent proliferation and SOX9⁺/HNF4α⁺ biliary/progenitor transdifferentiation in primary mouse hepatocyte-derived CLiPs^[1].

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

Western Blot Analysis^[1]

Cell Line:

HepG2 cells
Concentration:

0.1 μM; 0.3 μM; 1 μM; 3 μM; 10 μM
Incubation Time:

1 h; 2 h; 4 h; 5 h; 6 h; 8 h
Result:

Reduced the phosphorylation levels of YAP1/TAZ.

Immunofluorescence^[1]

Cell Line:

HepG2 cells
Concentration:

1 μM; 3 μM
Incubation Time:

1 h; 2 h; 4 h; 5 h; 6 h; 8 h
Result:

Promoted the nuclear localization of YAP1/TAZ in HepG2 cells.

Parmacokinetics

Species	Dose	Route	T_1/2	T_max	C_max	AUC_0-t	AUC_0-inf	CL	MRT_0-t	MRT_0-inf
Mice^[1]	5 mg/kg	i.p.	1.27 h	0.0830 h	1160 ng/mL	1190 ng·h/mL	1200 ng·h/mL	69.4 mL/min/kg	0.848 h	0.971 h

In Vivo

LPi-1 (3 mg/kg and 0.3-30 mg/kg; i.p.; single injection; dose-response) inhibits LATS1/2-mediated YAP1/TAZ phosphorylation in mouse liver in vivo in a dose-dependent manner^[1].
Chronic LPi-1 (3 mg/kg; i.p.; once daily; 2 months) increases liver progenitor/proliferation markers and liver/body weight ratio in healthy mice, and these effects reverse after LPi-1 withdrawal^[1].
LPi-1 (3 mg/kg; i.p.; once daily; 4 weeks) increases liver progenitor/proliferation markers and liver/body weight ratio in postnatal mice^[1].
LPi-1 (3 mg/kg; i.p.; at surgery and twice daily; 7 days) promotes liver regeneration after partial hepatectomy by enhancing hepatocyte proliferation and YAP/TAZ activation^[1].
LPi-1 (3 mg/kg; i.p.; twice daily; beginning 1.5 h after APAP) ameliorates APAP-induced acute liver injury and improves survival in mice^[1].
LPi-1 (3 mg/kg; i.p.; twice daily) protects against DSS-induced colitis and preserves colonocyte proliferation in mice^[1].

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

Animal Model:

C57BL/6 (wild-type)^[1]
Dosage:

3 mg/kg; 0.3, 1, 3, 10, and 30 mg/kg
Administration:

i.p.; single injection; dose-response
Result:

Inhibition of YAP1/TAZ phosphorylation in liver reached a maximum at 2 h after i.p. injection of LPi-1 (3 mg/kg).
This inhibition in liver tissues was dose-dependent across 0.3, 1, 3, 10, and 30 mg/kg LPi-1.

Animal Model:

C57BL/6 (male, 6-8 weeks old, 20-25 g)^[1]
Dosage:

3 mg/kg (2 months); 3 mg/kg (2 months then withdrawal 20 days)
Administration:

i.p.; once daily; 2 months; 20 days withdrawal
Result:

Wild-type mice receiving LPi-1 daily for 2 months exhibited a modest increase in the percentage of CK19-positive and Ki67-positive cells, as well as in the liver/body weight ratio, which subsequently returned to baseline levels 20 days after discontinuation of LPi-1.

Animal Model:

C57BL/6 (male, 10 days old, 8-10 g)^[1]
Dosage:

3 mg/kg
Administration:

i.p.; once daily; 4 weeks
Result:

LPi-1 resulted in a moderate increase in the percentage of CK19-positive and Ki67-positive cells, as well as in the liver/body weight ratio, compared with vehicle controls.

Animal Model:

C57BL/6 (male, 8-10 weeks old, 25-30 g)^[1]
Dosage:

3 mg/kg
Administration:

i.p.; at surgery and twice daily; 7 days
Result:

Significantly enhanced liver regeneration, as evidenced by a higher percentage of Ki67- and BrdU-positive cells in the liver and a more rapid increase in the liver/body weight ratio compared to controls between postoperative days 1 and 7.
Mice receiving LPi-1 exhibited decreased Yap1 and TAZ phosphorylation and increased expression of Ccn2/Ctgf and Ccn1/Cyr61 between postoperative days 2 and 6.

Animal Model:

C57BL/6 (male, 6-8 weeks old, 20-25 g)^[1]
Dosage:

3 mg/kg
Administration:

i.p.; twice daily; beginning 1.5 h after APAP
Result:

In the lethal APAP model, LPi-1 increased survival from 10% to 70%.
APAP-fed mice receiving LPi-1 exhibited reduced centrilobular necrotic lesions and TUNEL+ cells at 6 h and prevented sustained expansion of necrosis at 12, 24, and 48 h.
LPi-1 lowered serum ALT and AST levels at specific hours following APAP feeding compared to controls.

Animal Model:

C57BL/6 (male, 8-10 weeks old, 25-30 g)^[1]
Dosage:

3 mg/kg
Administration:

i.p.; twice daily
Result:

Mice receiving LPi-1 showed less weight loss, reduced colitis symptoms including diarrhea and rectal bleeding, more intact intestinal structure, and a higher percentage of Ki67-positive proliferating cells in colon crypts compared with vehicle controls.

Related Protocols :

Chemical Information

CAS No. 2251130-98-8
Molecular Weight 369.78
Formula C₁₉H₁₃ClFN₃O₂
SMILES

O=C(C1=COC(C2=CNC3=C2C=CC=N3)=C1)NCC4=C(Cl)C=CC=C4F
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

Handling Instructions (2659 KB)

References

[1]. Xiao C, et al. Pharmacological targeting of large tumor suppressor kinases (LATS) 1 and 2 augments tissue repair and regeneration. British journal of pharmacology. 2025 Nov;182(22):5536-5555.

Calculators

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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.

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100 mg

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