製品番号: HY-189570

TMLB-G9

TMLB-G9 is an orally active B3GAT3 inhibitor (human K_d = 0.72 μM). TMLB-G9 blocks glycosaminoglycan biosynthesis and inhibits chondroitin sulfate biosynthesis in hepatocellular carcinoma cells. TMLB-G9 induces apoptosis by upregulating cleaved PARP and cleaved caspase-3. TMLB-G9 induces G0/G1 cell cycle arrest by upregulating Rb and downregulating CDK1, CDK2, Cyclin A2, Cyclin E1, and phosphorylated Rb. TMLB-G9 inhibits migration and invasion by reversing epithelial-mesenchymal transition, manifested as upregulation of E-cadherin and downregulation of N-cadherin, vimentin, MMP-2, MMP-9, and ZEB1. TMLB-G9 inhibits colony formation. TMLB-G9 exhibits broad-spectrum antitumor activity against multiple cancer cell lines. TMLB-G9 can be used for research on hepatocellular carcinoma.

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CAS 番号: 3127781-85-2
分子式: C₃₃H₂₆N₄O₇
分子量:590.58

保管条件:

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

TMLB-G9 構造式

CAS 番号: 3127781-85-2

価格（税別）

Amount: USD 0.00

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Use of MCE Products

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

生物活性
- 製品説明
- IC₅₀ & Target
- Cellular Effect
- 体外実験
- Parmacokinetics
- 体内実験
化学情報
純度とドキュメンテーション
参考文献
Calculators
Help & FAQs
関連分類
Bioz

生物活性

製品説明

IC₅₀ & Target

^[1]

CDK1

CDK2

MMP-9

Caspase 3

MMP-2

PARP アイソフォーム固有の製品をすべて表示 :

Caspase アイソフォーム固有の製品をすべて表示 :

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Cellular Effect

Cell Line	Type	Value	Description	References
Huh-7	IC50	0.36 μM	Antiproliferative activity against Huh7 cells assessed as viability inhibition by cell viability assay. Antiproliferative activity against Huh7 cells assessed as viability inhibition by cell viability assay.	acs.jmedchem.6c02080
Hep3B	IC50	0.31 μM	Antiproliferative activity against Hep3B cells assessed as viability inhibition by cell viability assay. Antiproliferative activity against Hep3B cells assessed as viability inhibition by cell viability assay.	acs.jmedchem.6c02080
PLC-PRF-5	IC50	1.14 μM	Antiproliferative activity against PLC/PRF/5 cells assessed as viability inhibition by cell viability assay. Antiproliferative activity against PLC/PRF/5 cells assessed as viability inhibition by cell viability assay.	acs.jmedchem.6c02080
SNU-387	IC50	3.40 μM	Antiproliferative activity against SNU387 cells assessed as viability inhibition by cell viability assay. Antiproliferative activity against SNU387 cells assessed as viability inhibition by cell viability assay.	acs.jmedchem.6c02080
HCCLM3	IC50	0.35 μM	Antiproliferative activity against HCCLM3 cells assessed as viability inhibition by cell viability assay. Antiproliferative activity against HCCLM3 cells assessed as viability inhibition by cell viability assay.	acs.jmedchem.6c02080
NCI-H460	IC50	1.21 μM	Antiproliferative activity against NCI-H460 cells assessed as viability inhibition by cell viability assay. Antiproliferative activity against NCI-H460 cells assessed as viability inhibition by cell viability assay.	acs.jmedchem.6c02080
PC-3	IC50	0.13 μM	Antiproliferative activity against PC3 cells assessed as viability inhibition by cell viability assay. Antiproliferative activity against PC3 cells assessed as viability inhibition by cell viability assay.	acs.jmedchem.6c02080
AGS	IC50	1.27 μM	Antiproliferative activity against AGS cells assessed as viability inhibition by cell viability assay. Antiproliferative activity against AGS cells assessed as viability inhibition by cell viability assay.	acs.jmedchem.6c02080
HT-29	IC50	1.49 μM	Antiproliferative activity against HT29 cells assessed as viability inhibition by cell viability assay. Antiproliferative activity against HT29 cells assessed as viability inhibition by cell viability assay.	acs.jmedchem.6c02080
SW-620	IC50	0.84 μM	Antiproliferative activity against SW620 cells assessed as viability inhibition by cell viability assay. Antiproliferative activity against SW620 cells assessed as viability inhibition by cell viability assay.	acs.jmedchem.6c02080
MDA-MB-231	IC50	1.29 μM	Antiproliferative activity against MDA-MB-231 cells assessed as viability inhibition by cell viability assay. Antiproliferative activity against MDA-MB-231 cells assessed as viability inhibition by cell viability assay.	acs.jmedchem.6c02080
U-251	IC50	0.89 μM	Antiproliferative activity against U251-MG cells assessed as viability inhibition by cell viability assay. Antiproliferative activity against U251-MG cells assessed as viability inhibition by cell viability assay.	acs.jmedchem.6c02080
H4	IC50	0.85 μM	Antiproliferative activity against H4 cells assessed as viability inhibition by cell viability assay. Antiproliferative activity against H4 cells assessed as viability inhibition by cell viability assay.	acs.jmedchem.6c02080
MEG-01	IC50	3.76 μM	Antiproliferative activity against MEG01 cells assessed as viability inhibition by cell viability assay. Antiproliferative activity against MEG01 cells assessed as viability inhibition by cell viability assay.	acs.jmedchem.6c02080
Jurkat	IC50	0.46 μM	Antiproliferative activity against Jurkat cells assessed as viability inhibition by cell viability assay. Antiproliferative activity against Jurkat cells assessed as viability inhibition by cell viability assay.	acs.jmedchem.6c02080

体外実験

Anti-cancerCell Cycle RegulationApoptosisOthers

Anti-cancer

TMLB-G9 inhibits the proliferation of HCC and pan-cancer cells, with IC₅₀ values as low as 0.13 μM and 0.31 μM in PC3 and Hep3B, respectively^[1].
TMLB-G9 (0.01-1 μM; 16 days) inhibits colony formation in Huh7 and Hep3B cells^[1].
TMLB-G9 (0.5-1 μM; 6-48 h) inhibits the migration and invasion of Huh7 and Hep3B cells and reverses EMT^[1].

Anti-cancer

Cell Cycle Regulation

TMLB-G9 (0.5-1 μM) induces G0/G1 cell cycle arrest in Huh7 and Hep3B cells^[1].

Anti-cancer

Apoptosis

TMLB-G9 (0.5-1 μM) induces apoptosis in Huh7 and Hep3B cells^[1].

Others

TMLB-G9 binds to B3GAT3 in Huh7 and Hep3B cells, with T_agg values of 52.69 °C and 57.15 °C, respectively^[1].
TMLB-G9 (48 h) inhibits chondroitin sulfate biosynthesis in Huh7 and Hep3B cells^[1].

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

Cell Migration Assay ^[1]

Cell Line:

Huh7 and Hep3B cells
Concentration:

1 μM (scratch assay); 0.5 and 1 μM (Transwell and EMT Western blot)
Incubation Time:

12 h (scratch assay, Huh7); 6 h (scratch assay, Hep3B); 48 h (Transwell and EMT Western blot)
Result:

Suppressed wound healing in Huh7 cells from approximately 16% to 9% at 1 μM for 12 h and in Hep3B cells from 13.68% to 3.43% at 1 μM for 6 h.
Significantly suppressed migration and invasion.
Upregulated E-cadherin and downregulated N-cadherin, vimentin, MMP-2, MMP-9, and ZEB1.

Parmacokinetics

Species	Dose	Route	F	AUC_0-t	AUC_0-∞	T_1/2	T_max	C_max	MRT_0-t	MRT_0-∞
Rat^[1]	2 mg/kg	i.v.	/	1094.81 ng·h/mL	1097.32 ng·h/mL	1.03 h	0.08 h	2493.82 ng/mL	0.52 h	0.54 h
Rat^[1]	5 mg/kg	i.p.	11.37 %	311.07 ng·h/mL	318.71 ng·h/mL	4.41 h	5.33 h	25.37 ng/mL	7.72 h	7.80 h
Rat^[1]	10 mg/kg	p.o.	< 1 %	/	/	/	/	/	/	/

体内実験

Anti-cancer

TMLB-G9 (5-20 mg/kg; p.o. (oral gavage); daily; for 16 consecutive days) produces dose-dependent tumor growth inhibition in the Huh7 HCC xenograft mouse model^[1].
TMLB-G9 (20 mg/kg; p.o. (oral gavage); daily; for 16 consecutive days) produces tumor growth inhibition in the HCCLM3 HCC xenograft mouse model^[1].

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

Animal Model:

BALB/c nude^[1]
Dosage:

5 mg/kg, 10 mg/kg, and 20 mg/kg
Administration:

p.o. (oral gavage); daily; 16 consecutive days
Result:

Daily oral gavage of compound TMLB-G9 exhibited a dose-dependent tumor growth inhibition, with inhibition rates of 63.72%, 73.95%, and 83.72% at doses of 5, 10 and 20 mg/kg, respectively, which was comparable to that of lenvatinib and superior to that of compound TMLB-C16.

Animal Model:

BALB/c nude^[1]
Dosage:

20 mg/kg
Administration:

p.o. (oral gavage); daily; 16 consecutive days
Result:

The antitumor effect of compound TMLB-G9 was further confirmed in the HCCLM3-derived xenograft model, showing approximately 54.24% tumor growth inhibition at 20 mg/kg.

Related Protocols :

化学情報

CAS 番号 3127781-85-2
分子量 590.58
分子式 C₃₃H₂₆N₄O₇
SMILES

O=C(OC)C1=CC=C(NC=C2C(C(NCCNC(C3=CC(C4=CC(C=CC=C5)=C5O4)=NC(C3=C6)=CC=C6OC)=O)=O)=O)C2=C1
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件

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

純度とドキュメンテーション

取扱説明書 (2659 KB)

参考文献

[1]. Yin H, et al. Structure-Guided Design, Synthesis, and Evaluation of Novel 6-Methoxyquinoline-4-carboxamide Derivatives as First-in-Class Nano-Molar B3GAT3 Inhibitors for the Treatment of Hepatocellular Carcinoma. Journal of Medicinal Chemistry. 2026 Sep 24;69(18):21440-82.

Calculators

モル濃度計算機

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

Mass Mass

濃度濃度

体積体積

分子量分子量

希釈計算機

濃度 _(開始) × 体積 _(開始) = 濃度 _(終了) × 体積 _(終了)

濃度 _(開始) 濃度 _(開始)

体積 _(開始) 体積 _(開始)

濃度 _(終了) 濃度 _(終了)

体積 _(終了) 体積 _(終了)

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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TMLB-G9

PARP アイソフォーム固有の製品をすべて表示

Caspase アイソフォーム固有の製品をすべて表示

CDK アイソフォーム固有の製品をすべて表示

MMP アイソフォーム固有の製品をすべて表示

生物活性