Cat. No.: HY-164793

TGFBR1-IN-2

Customer Review

Based on 1 Customer Validation

TGFBR1-IN-2 (Compound AQA) is a TGFBR1 inhibitor and an antibacterial agent. TGFBR1-IN-2 is a substrate for cytochrome P450s. TGFBR1-IN-2 contains the pyridyl-6-methyl moiety necessary for Mycobacterium tuberculosis inhibition and has potent inhibitory activity against non-replicating and persistent Mycobacterium tuberculosis.

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

CAS No.: 733806-89-8
Formula: C₁₉H₁₅N₅
Molecular Weight:313.36

Storage:

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

Data Sheet (277 KB)

TGFBR1-IN-2 Chemical Structure

CAS No.: 733806-89-8

Size

Price

Stock

Quantity

Amount: USD 0.00

* Please select Quantity before adding items.

Top Publications Citing

Use of MCE Products

Fluorescent Dye

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

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

Biological Activity

Description

IC₅₀ & Target^[1]

TGFBR1

0.01 μM (Kd)

All TGF-β Receptor Isoforms :

All Cytochrome P450 Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
HepG2	IC₅₀	0.095 μM Compound: 3d	Inhibition of TGF-beta-induced ALK5 in human HepG2 cells by luciferase assay Inhibition of TGF-beta-induced ALK5 in human HepG2 cells by luciferase assay	[PMID: 19285388]
Sf9	IC₅₀	0.025 μM Compound: 3d	Inhibition of human ALK5 kinase expressed in Sf9 cells Inhibition of human ALK5 kinase expressed in Sf9 cells	[PMID: 19285388]

In Vitro

TGFBR1-IN-2 inhibits nonreplicating Mycobacterium tuberculosis, with MIC_90NR of 1 μM, MIC₉₀ of 20 μM, MIC₅₀ of 16 μM^[1].
TGFBR1-IN-2 (2-20 μM, 35 days) inhibits drug-tolerant microorganisms (Mycobacterium tuberculosis-GFP culture with Rifampicin (HY-B0272) and Isoniazid (HY-B0329))^[1].

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

Cell Viability Assay^[1]

Cell Line:

an Mtb-GFP culture with Rifampicin and Isoniazid
Concentration:

2, 20 μM
Incubation Time:

35 days
Result:

Showed full activity against Mtb-GFP (at 2 μM and 20 μM).

In Vivo

TGFBR1-IN-2 (10 mg/kg. p.o.) demonstrates a short half-life and low plasma concentration in CD1 mice, with T_1/2 of 1.8 h, C_max of 280 ng/ mL and AUC_last of 640 h*ng/mL^[1].

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

Chemical Information

CAS No. 733806-89-8
Appearance Solid
Molecular Weight 313.36
Formula C₁₉H₁₅N₅
SMILES

CC1=NC(C2=NC(NC3=CC=NC=C3)=C4C=CC=CC4=N2)=CC=C1
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 (319.12 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

3.1912 mL

15.9561 mL

31.9122 mL

5 mM

0.6382 mL

3.1912 mL

6.3824 mL

10 mM

0.3191 mL

1.5956 mL

3.1912 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)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (277 KB)
SDS (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)
- 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]. Nandakumar, et al. Dual Inhibition of Mycobacterium tuberculosis and the Host TGFBR1 by an Anilinoquinazoline. Journal of medicinal chemistry. 2023, 66(21):14724-14734. [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	3.1912 mL	15.9561 mL	31.9122 mL	79.7804 mL
	5 mM	0.6382 mL	3.1912 mL	6.3824 mL	15.9561 mL
	10 mM	0.3191 mL	1.5956 mL	3.1912 mL	7.9780 mL
	15 mM	0.2127 mL	1.0637 mL	2.1275 mL	5.3187 mL
	20 mM	0.1596 mL	0.7978 mL	1.5956 mL	3.9890 mL
	25 mM	0.1276 mL	0.6382 mL	1.2765 mL	3.1912 mL
	30 mM	0.1064 mL	0.5319 mL	1.0637 mL	2.6593 mL
	40 mM	0.0798 mL	0.3989 mL	0.7978 mL	1.9945 mL
	50 mM	0.0638 mL	0.3191 mL	0.6382 mL	1.5956 mL
	60 mM	0.0532 mL	0.2659 mL	0.5319 mL	1.3297 mL
	80 mM	0.0399 mL	0.1995 mL	0.3989 mL	0.9973 mL
	100 mM	0.0319 mL	0.1596 mL	0.3191 mL	0.7978 mL

Keywords

Product Name:
Cat. No.:
Quantity:
MCE Japan Authorized Agent:

Product Name:
CAS No.:
Species:
Purity:
Quantity:

TGFBR1-IN-2

Anti-Infection Compound Library

Kinase Inhibitor Library

Metabolism/Protease Compound Library

TGF-beta/Smad Compound Library

Anti-Aging Compound Library

Antioxidant Compound Library

Reprogramming Compound Library

Oxygen Sensing Compound Library

Antibacterial Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Obesity Compound Library

Angiogenesis-Related Compound Library

Mitochondria-Targeted Compound Library

Anti-Colorectal Cancer Compound Library

Anti-Prostate Cancer Compound Library

Anti-Pulmonary Fibrosis Compound Library

Osteogenesis Compound Library

Cancer Stem Cells Compound Library

Anti-tuberculosis Compound Library

Metabolic Enzyme Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Cytokine Inhibitors Library

Multi-Target Compound Library

Radioprotector Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Anti-Fibrosis Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

All TGF-β Receptor Isoforms

All Cytochrome P450 Isoforms

Biological Activity

Chemical Information

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

TGFBR1-IN-2 Related Classifications

Cat. No.: HY-164793