Cat. No.: HY-160623

Rentosertib

(Synonyms: INS018_055; TNIK&MAP4K4-IN-2)

Customer Review

Based on 1 Customer Validation

Rentosertib (INS018 055) (compound 112) is the orally active TNIK and MAP4K4 inhibitor with IC₅₀ values of 12-120, 12-120 nM, respectively.

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

Purity: 99.96%
CAS No.: 2828567-39-9
Formula: C₂₇H₃₀FN₇O
Molecular Weight:487.57

Storage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

Rentosertib Chemical Structure

CAS No.: 2828567-39-9

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Fluorescent Dye

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

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Solvent & Solubility
- In Vitro
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

Rentosertib (INS018 055) (compound 112) is the orally active TNIK and MAP4K4 inhibitor with IC₅₀ values of 12-120, 12-120 nM, respectively^[1].

IC₅₀ & Target^[1]

MAP4K4

12-120 nM (IC₅₀)

TNIK

12-120 nM (IC₅₀)

All MAP4K Isoforms :

All TGF-beta/Smad Isoforms :

Smad1
Smad3

All Interleukin Related Isoforms :

In Vitro

Rentosertib (INS018 055) (0-3 μM, 72 h) reduces TGF-β-induced α-SMA protein expressio with an IC₅₀ of 27.14 nM in MRC-5 cell^[2].
Rentosertib (INS018 055) (0-3 μM, 72 h) decreases the expression of N-cadherin, p-SMAD2/SMAD3, increases the expression of E-cadherin, and inhibits TGF-β-induced epithelial-to-mesenchymal transition (EMT) and fibroblast-to-myofibroblast transition (FMT) in A549 cell^[2].

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

Western Blot Analysis^[2]

Cell Line:

A549
Concentration:

0-3 μM
Incubation Time:

72 h
Result:

Decreased the expression of N-cadherin and p-SMAD2/SMAD3, and increased the expression of E-cadherin.

In Vivo

Rentosertib (INS018 055) (3-30 mg/kg, po, twice a day for 2 weeks) improves lung function, and ameliorates pulmonary fibrosis in Bleomycin (HY-17565)-administrated mouse models^[2].
Rentosertib (INS018 055) (3-30 mg/kg, po, single dose) reduces the number of lymphocytes in bronchoalveolar lavage fluid (BALF), inhibits the expressions of pro-inflammatory cytokines, and exhibits anti-inflammatory effect in LPS (HY-D1056)-induced mouse acute lung injury model^[2].

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

Animal Model:

Bleomycin (HY-17565)-induced mouse pulmonary fibrosis models^[2]
Dosage:

3-30 mg/kg
Administration:

po, twice a day for 2 weeks
Result:

Improved lung function, reduced the area of pulmonary fibrosis, and reduced the expression of α-SMA and collagen I.

Animal Model:

LPS (HY-D1056)-induced mouse acute lung injury model^[2]
Dosage:

3-30 mg/kg
Administration:

po, single dose
Result:

Reduced the number of lymphocytes in bronchoalveolar lavage fluid (BALF), reduced the levels of IL-1β, IL-6, IL-7 and TNF-α, and increased the level of IL-4.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 2828567-39-9
Appearance Solid
Molecular Weight 487.57
Formula C₂₇H₃₀FN₇O
Color White to light yellow
SMILES

O=C(C1=CN=C(C2=C(C3=CC=C(C=C3)F)N=CN2C(C)C)N1)NC4=CC=C(N5CCN(CC5)C)C=C4
Synonyms

INS018_055; TNIK&MAP4K4-IN-2
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 (205.10 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.0510 mL

10.2549 mL

20.5099 mL

5 mM

0.4102 mL

2.0510 mL

4.1020 mL

10 mM

0.2051 mL

1.0255 mL

2.0510 mL

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

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

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Dilution Calculator

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Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (275 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Aleksandrs Zavoronkovs, et al. Analogs for the treatment of disease. WO2022179528A1.

[2]. Ren F, et al. A small-molecule TNIK inhibitor targets fibrosis in preclinical and clinical models. Nat Biotechnol. 2025 Jan;43(1):63-75. [Content Brief]

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.

Complete Stock Solution Preparation Table

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	2.0510 mL	10.2549 mL	20.5099 mL	51.2747 mL
	5 mM	0.4102 mL	2.0510 mL	4.1020 mL	10.2549 mL
	10 mM	0.2051 mL	1.0255 mL	2.0510 mL	5.1275 mL
	15 mM	0.1367 mL	0.6837 mL	1.3673 mL	3.4183 mL
	20 mM	0.1025 mL	0.5127 mL	1.0255 mL	2.5637 mL
	25 mM	0.0820 mL	0.4102 mL	0.8204 mL	2.0510 mL
	30 mM	0.0684 mL	0.3418 mL	0.6837 mL	1.7092 mL
	40 mM	0.0513 mL	0.2564 mL	0.5127 mL	1.2819 mL
	50 mM	0.0410 mL	0.2051 mL	0.4102 mL	1.0255 mL
	60 mM	0.0342 mL	0.1709 mL	0.3418 mL	0.8546 mL
	80 mM	0.0256 mL	0.1282 mL	0.2564 mL	0.6409 mL
	100 mM	0.0205 mL	0.1025 mL	0.2051 mL	0.5127 mL

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Rentosertib

Immunology/Inflammation Compound Library

Kinase Inhibitor Library

MAPK Compound Library

Stem Cell Signaling Compound Library

TGF-beta/Smad Compound Library

Wnt/Hedgehog/Notch Compound Library

Clinical Compound Library

Anti-Aging Compound Library

Drug Repurposing Compound Library

Oxygen Sensing Compound Library

Cytoskeleton Compound Library

Orally Active Compound Library

Anti-Obesity Compound Library

Angiogenesis-Related Compound Library

Transcription Factor-Targeted Library

Anti-Colorectal Cancer Compound Library

Anti-Prostate Cancer Compound Library

Anti-Pulmonary Fibrosis Compound Library

Osteogenesis Compound Library

Cancer Stem Cells Compound Library

Serine/Threonine Kinase Inhibitor Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Bioactive Compound Library

Anti-Fibrosis Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

All MAP4K Isoforms

All TGF-beta/Smad Isoforms

All Interleukin Related Isoforms

Biological Activity

Chemical Information

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Rentosertib Related Classifications

HY-160623 Related Classifications