TMLB-C16

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TMLB-C16 是一种强效且口服有效的 B3GAT3 抑制剂，其 K_D 值为 3.962 μM。TMLB-C16 可抑制 MHCC-97H (IC₅₀ = 6.53 μM) 和 HCCLM3 (IC₅₀ = 6.22 μM) 细胞的增殖和迁移，并诱导细胞周期阻滞和凋亡 (apoptosis)。TMLB-C16 在 MHCC-97H 和 HCCLM3 异种移植瘤小鼠模型中均能抑制肿瘤生长，且未观察到明显的毒性。TMLB-C16 可用于肝细胞癌的研究。

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TMLB-C16 Chemical Structure

CAS No. : 2923531-50-2

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生物活性
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参考文献

生物活性

TMLB-C16 is a potent and orally active B3GAT3 inhibitor with a K_D of 3.962 μM. TMLB-C16 suppresses proliferation and migration, and induces cell cycle arrest and apoptosis in MHCC-97H (IC₅₀ = 6.53 μM) and HCCLM3 cells (IC₅₀ = 6.22 μM). TMLB-C16 inhibits tumor growth in both MHCC-97H and HCCLM3 xenograft tumor mouse models without causing obvious toxicity. TMLB-C16 can be used for hepatocellular carcinoma research^[1].

细胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
AGS	IC₅₀	5.33 μM Compound: TMLB-C16	Anti-tumor activity against human AGS cells assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay Anti-tumor activity against human AGS cells assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay	[PMID: 38919032]
Calu-3	IC₅₀	41.64 μM Compound: TMLB-C16	Anti-tumor activity against human Calu-3 cells assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay Anti-tumor activity against human Calu-3 cells assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay	[PMID: 38919032]
H4	IC₅₀	6.65 μM Compound: TMLB-C16	Anti-tumor activity against human H4 cells assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay Anti-tumor activity against human H4 cells assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay	[PMID: 38919032]
HCC1937	IC₅₀	47.89 μM Compound: TMLB-C16	Anti-tumor activity against human HCC1937 cells assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay Anti-tumor activity against human HCC1937 cells assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay	[PMID: 38919032]
HCCLM3	IC₅₀	18.35 μM Compound: TMLB-C16	Antitumor activity against human HCCLM3 cells assessed as inhibition of cell proliferation measured after 72 hrs by CCK-8 assay Antitumor activity against human HCCLM3 cells assessed as inhibition of cell proliferation measured after 72 hrs by CCK-8 assay	[PMID: 38919032]
HCCLM3	IC₅₀	6.22 μM Compound: TMLB-C16	Antitumor activity against human HCCLM3 cells assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay Antitumor activity against human HCCLM3 cells assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay	[PMID: 38919032]
HT-29	IC₅₀	4.71 μM Compound: TMLB-C16	Anti-tumor activity against human HT-29 cells assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay Anti-tumor activity against human HT-29 cells assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay	[PMID: 38919032]
Hep 3B2	IC₅₀	12.19 μM Compound: TMLB-C16	Antitumor activity against human Hep3B cells assessed as inhibition of cell proliferation measured after 72 hrs by CCK-8 assay Antitumor activity against human Hep3B cells assessed as inhibition of cell proliferation measured after 72 hrs by CCK-8 assay	[PMID: 38919032]
Huh-7	IC₅₀	12.54 μM Compound: TMLB-C16	Antitumor activity against human Huh-7 cells assessed as inhibition of cell proliferation measured after 72 hrs by CCK-8 assay Antitumor activity against human Huh-7 cells assessed as inhibition of cell proliferation measured after 72 hrs by CCK-8 assay	[PMID: 38919032]
Jurkat	IC₅₀	6.69 μM Compound: TMLB-C16	Anti-tumor activity against human Jurkat cells assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay Anti-tumor activity against human Jurkat cells assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay	[PMID: 38919032]
K562	IC₅₀	8.25 μM Compound: TMLB-C16	Anti-tumor activity against human K562 cells assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay Anti-tumor activity against human K562 cells assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay	[PMID: 38919032]
MDA-MB-231	IC₅₀	12.32 μM Compound: TMLB-C16	Anti-tumor activity against human MDA-M8-231 cells assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay Anti-tumor activity against human MDA-M8-231 cells assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay	[PMID: 38919032]
MEG-01	IC₅₀	11.48 μM Compound: TMLB-C16	Anti-tumor activity against human MEG-01 cells assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay Anti-tumor activity against human MEG-01 cells assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay	[PMID: 38919032]
MHCC97H	IC₅₀	17.02 μM Compound: TMLB-C16	Cytotoxicity against (shRNA)-mediated B3GAT3 KO human MHCC97H cells assessed as cell viability measured after 72 hrs by CCK8 assay Cytotoxicity against (shRNA)-mediated B3GAT3 KO human MHCC97H cells assessed as cell viability measured after 72 hrs by CCK8 assay	[PMID: 38919032]
MHCC97H	IC₅₀	18.87 μM Compound: TMLB-C16	Antitumor activity against human MHCC97H cells assessed as inhibition of cell proliferation measured after 72 hrs by CCK-8 assay Antitumor activity against human MHCC97H cells assessed as inhibition of cell proliferation measured after 72 hrs by CCK-8 assay	[PMID: 38919032]
MHCC97H	IC₅₀	6.53 μM Compound: TMLB-C16	Antitumor activity against human MHCC97H cells assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay Antitumor activity against human MHCC97H cells assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay	[PMID: 38919032]
MHCC97H	IC₅₀	6.92 μM Compound: TMLB-C16	Cytotoxicity against (shRNA)-Ctrl transfected human MHCC97H cells assessed as cell viability measured after 72 hrs by CCK8 assay Cytotoxicity against (shRNA)-Ctrl transfected human MHCC97H cells assessed as cell viability measured after 72 hrs by CCK8 assay	[PMID: 38919032]
MKN-45	IC₅₀	13.87 μM Compound: TMLB-C16	Anti-tumor activity against human MKN-45 cells assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay Anti-tumor activity against human MKN-45 cells assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay	[PMID: 38919032]
NCI-H1650	IC₅₀	21.56 μM Compound: TMLB-C16	Anti-tumor activity against human NCI-H1650 cells assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay Anti-tumor activity against human NCI-H1650 cells assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay	[PMID: 38919032]
NCI-H446	IC₅₀	11.58 μM Compound: TMLB-C16	Anti-tumor activity against human NCI-H446 cells assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay Anti-tumor activity against human NCI-H446 cells assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay	[PMID: 38919032]
PC-3	IC₅₀	13.7 μM Compound: TMLB-C16	Anti-tumor activity against human PC-3 cells assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay Anti-tumor activity against human PC-3 cells assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay	[PMID: 38919032]
PLC-PRF-5	IC₅₀	6.52 μM Compound: TMLB-C16	Antitumor activity against human PLC-PRF-5 cells assessed as inhibition of cell proliferation measured after 72 hrs by CCK-8 assay Antitumor activity against human PLC-PRF-5 cells assessed as inhibition of cell proliferation measured after 72 hrs by CCK-8 assay	[PMID: 38919032]
SK-OV-3	IC₅₀	98.74 μM Compound: TMLB-C16	Anti-tumor activity against human SK-OV-3 cells assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay Anti-tumor activity against human SK-OV-3 cells assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay	[PMID: 38919032]
SNU-387	IC₅₀	11.71 μM Compound: TMLB-C16	Antitumor activity against human SNU-387 cells assessed as inhibition of cell proliferation measured after 72 hrs by CCK-8 assay Antitumor activity against human SNU-387 cells assessed as inhibition of cell proliferation measured after 72 hrs by CCK-8 assay	[PMID: 38919032]
SW-620	IC₅₀	8.66 μM Compound: TMLB-C16	Anti-tumor activity against human SW620 cells assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay Anti-tumor activity against human SW620 cells assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay	[PMID: 38919032]
THLE-2	IC₅₀	> 20 μM Compound: TMLB-C16	Antitumor activity against human THLE-2 cells assessed as inhibition of cell proliferation measured after 72 hrs by CCK-8 assay Antitumor activity against human THLE-2 cells assessed as inhibition of cell proliferation measured after 72 hrs by CCK-8 assay	[PMID: 38919032]
THP-1	IC₅₀	23.91 μM Compound: TMLB-C16	Anti-tumor activity against human THP-1 cells assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay Anti-tumor activity against human THP-1 cells assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay	[PMID: 38919032]
U-251	IC₅₀	6.16 μM Compound: TMLB-C16	Anti-tumor activity against human U-251MG cells assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay Anti-tumor activity against human U-251MG cells assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay	[PMID: 38919032]
U-937	IC₅₀	5.99 μM Compound: TMLB-C16	Anti-tumor activity against human U-937 cells assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay Anti-tumor activity against human U-937 cells assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay	[PMID: 38919032]

体外研究
(In Vitro)

TMLB-C16 (72 小时) 在 13 种 B3GAT3 高表达的癌细胞系 (例如 NCI-H460、NCI-H1650 和 Calu3 细胞) 中表现出广谱的抗肿瘤活性，且该活性依赖于 B3GAT3，IC₅₀ 值低于 20 μM^[1]。
TMLB-C16 (0-10 μM，14 天) 以剂量依赖的方式抑制 MHCC-97H 和 HCCLM3 细胞的克隆形成^[1]。
TMLB-C16 (0-10 μM，24 小时) 抑制 MHCC-97H 和 HCCLM3 细胞的迁移和分裂^[1]。
TMLB-C16 (0-10 μM，48 小时) 以剂量依赖的方式诱导 MHCC-97H 和 HCCLM3 细胞发生 G0/G1 期细胞周期阻滞和凋亡，同时伴随着 p21、p53 和视网膜母细胞瘤相关蛋白 (Rb) 水平升高，CDK6、cyclin E1 和磷酸化 Rb (p-Rb) 水平降低^[1]。

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

Cell Proliferation Assay^[1]

Cell Line:	MHCC-97H and HCCLM3 cells
Concentration:	0, 5, and 10 μM
Incubation Time:	14 days
Result:	Prevented colony formation in a dose-dependent manner.

Cell Migration Assay ^[1]

Cell Line:	MHCC-97H and HCCLM3 cells
Concentration:	0, 5, and 10 μM
Incubation Time:	24 h
Result:	Suppressed the wound healing of MHCC-97H and HCCLM3 cells from about 22.22% to 0.86% and 15.71% to 1.90%, respectively.

Cell Cycle Analysis^[1]

Cell Line:	MHCC-97H and HCCLM3 cells
Concentration:	0, 5, and 10 μM
Incubation Time:	24 h
Result:	Remarkably repressed the percentage of S-phase in MHCC-97H and HCCLM3 cells at the concentration of 10 and 5 μM, respectively, by accumulating cells in the G0/G1-phase.

Western Blot Analysis^[1]

Cell Line:	MHCC-97H and HCCLM3 cells
Concentration:	0, 5, and 10 μM
Incubation Time:	48 h
Result:	Induced expression of the epithelial surface marker E-cadherin as well as loss of the mesenchymal markers such as N-cadherin, vimentin, matrix metalloproteinase-2 (MMP-2), MMP-9, and zinc finger E-box-binding homeobox 1 (ZEB1). Significantly enhanced expression of p21, p53, and Rb, and decreased CDK6, cyclin E1, and p-Rb in a dose-dependent manner. Remarkably enhanced the expression levels of active c-PARP and c-caspase-3 in MHCC-97H and HCCLM3 cells.

Apoptosis Analysis^[1]

Cell Line:	MHCC-97H and HCCLM3 cells
Concentration:	0, 5, and 10 μM
Incubation Time:	48 h
Result:	Induced apoptosis at both tested concentrations. Increased the early and late apoptotic rates in MHCC-97H at 5 μM by 8.09% and 6.21%, respectively. Increased the early and late apoptotic rates in MHCC-97H at 10 μM by 29.93% and 15.77%, respectively.

体内研究
(In Vivo)

TMLB-C16 (5、10 和 20 mg/kg，灌胃，从第 7 天到第 31 天) 可抑制 MHCC-97H 和 HCCLM3 异种移植肿瘤小鼠模型中的肿瘤生长^[1]。

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

Animal Model:	Male BALB/c nude mice (6-8 weeks) subcutaneously injected with MHCC-97H and HCCLM3 cells^[1]
Dosage:	5, 10 and 20 mg/kg
Administration:	i.g., daily from day 7 to day 31
Result:	Exhibited a dose-dependent tumor inhibition effect in MHCC-97H xenograft model with 70% and 73.49% tumor growth inhibition at doses of 10 and 20 mg/kg, respectively. Exhibited a tumor growth inhibition rate of approximately 59% at the dose of 10 mg/kg in HCCLM3 xenograft model.

分子量

453.88

Formula

C₂₃H₂₀ClN₃O₅

CAS 号

2923531-50-2

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

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

纯度 & 产品资料

产品使用指南 (1538 KB)

参考文献

[1]. Yin H, et al. Discovery of Novel 2-Oxoacetamide Derivatives as B3GAT3 Inhibitors for the Treatment of Hepatocellular Carcinoma. J Med Chem. 2024 Jul 11;67(13):10743-10773. [Content Brief]

TMLB-C16 相关分类

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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.

Keywords:

TMLB-C162923531-50-2ApoptosisCDKCaspasePARPCyclin dependent kinasepoly ADP ribose polymeraseB3GAT3MHCC-97HHCCLM3 cellsxenograft tumor mouse modelhepatocellular carcinomaInhibitorinhibitorinhibit

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MedChemExpress (MCE) 只为有资质的科研机构、医药企业基于科学研究或药证申报的用途提供医药研发服务，不为任何个人或者非科研性质的、非用于药证申报使用等其他用途提供服务。

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TMLB-C16

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