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13

抑制剂 & 化合物

11

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T1992	Mertansine DM1,Maytansinoid DM1	Microtubule Associated	Cytoskeletal Signaling
	Mertansine (DM1) 是一种微管蛋白抑制剂，也是一种抗体可缀合的美登木素生物碱。它通过连接体连接到单克隆抗体上，形成抗体偶联药物。
T22136	PRL-3 Inhibitor I PRL-3 Inhibitor,BR-1	Phosphatase; Others	Metabolism; Others
	PRL-3 Inhibitor I (BR-1) 是 PRL-3 抑制剂，IC50=0.9 μM。它在细胞检测中显示降低侵袭性。
T2586	Cabozantinib 卡博替尼,XL184,BMS-907351	Apoptosis; VEGFR; FLT; c-Met/HGFR; c-RET; TAM Receptor; c-Kit	Angiogenesis; Apoptosis; Tyrosine Kinase/Adaptors
	Cabozantinib (XL184) 是一种多靶点酪氨酸激酶受体抑制剂，可以抑制 VEGFR2、c-Met、Kit、Axl 和 Flt3 (IC50=0.035/1.3/4.6/7/11.3 nM)。Cabozantinib 具有抗肿瘤和抗血管生成活性。
T5164	Cabozantinib hydrochloride XL184,Cabozantinib hydrochloride (849217-68-1(free base)),BMS-907351,盐酸卡博替尼	VEGFR; FLT; c-Met/HGFR; TAM Receptor; c-Kit; ROR	Angiogenesis; Metabolism; Tyrosine Kinase/Adaptors
	Cabozantinib hydrochloride (XL184) 是一种有效的泛酪氨酸激酶抑制剂，可抑制 VEGFR2、c-Met、Kit、Axl 和 Flt4（IC50：0.035、1.3、4.6、7 和 6 nM）。
T77743	TT-012	Others	Others
	TT-012 具有抗肿瘤活性，选择性结合动态 MITF，并破坏后者的二聚体形成和 DNA 结合。TT-012 对 B16F10 黑色素瘤细胞中 MITF 的转录有抑制作用。TT-012 在动物模型中对 MITF黑色素瘤细胞的生长和肿瘤生长转移有抑制作用。TT-012 对肝脏和免疫细胞具有较少的细胞毒性。
T76072	CCZ01048
	CCZ01048 是一种 α-MSH 类似物，与黑素皮质素 1 受体(MC1R)具有很高的结合亲和力，Ki 值为 0.31 nM。CCZ01048 具有快速内化 B16F10 黑色素瘤细胞和高体内稳定性。CCZ01048 是恶性黑色素瘤 PET 显像的一个有前途的制剂。
T79401	Tyrosinase-IN-13	Tyrosinase	Proteases/Proteasome
	Tyrosinase-IN-13 (compound 3c)为Flurbiprofen的衍生物，具有非竞争性酪氨酸酶抑制活性（IC50=68 μM；Ki=36.3 μM），并对肝细胞癌（HepG2）、结直肠癌（HT-29）及黑色素瘤（B16F10）细胞表现出细胞毒性。
T75029	HEMTAC CDK4/6 degrader 1
	HEMTAC CDK4/6 degrader 1 是一种通过连接HSP90的配体和CDK4/6而形成的PROTAC，其Kd值为35.7 µM。在B16F10黑色素瘤细胞中，该化合物能够诱导CDK4/6的降解，从而将细胞周期阻滞在G0/G1期，并引发细胞凋亡。因此，HEMTAC CDK4/6 degrader 1可被应用于癌症研究领域。
T76072L	CCZ01048 TFA
	CCZ01048 TFA 是一种 α-MSH 类似物，与黑素皮质素1受体(MC1R)具有很高的结合亲和力，Ki 值为 0.31 nM。CCZ01048 TFA 具有快速内化 B16F10 黑色素瘤细胞和高体内稳定性。CCZ01048 TFA 是恶性黑色素瘤 PET 显像的一个有前途的制剂。
T82524	Dual photoCORM 1
	Dual photoCORM 1（化合物 5）是一种无金属的光化学活性双CORM，它不仅展现出良好的细胞摄取性能，还能实时监测CO的释放。
T69269	DMGF
	DMGF, also known as 7,7-dimethoxyagastisfavone, is a biflavonoid isolated from Taxus × media cv. Hicksii. DMGF induces apoptotic and autophagic cell death. DMGF could effectively attenuate the motility of B16F10 cells, and the results of real-time PCR revealed that DMGF also suppressed the expressions of matrix metalloproteinase-2 (MMP-2). MGF can inhibit the metastasis of highly invasive melanoma cancer cells through the down-regulation of F-actin polymerization DMGF may be further developed to...
T69447	APBC
	APBC is a novel PD-L1 inhibitor, effectively interrupting the PD-1/PD-L1 interaction by directly binding to PD-L1, presenting the KD and IC50 values at low-micromolar level, displaying superior antitumor efficacy in hPD-L1 knock-in B16F10-bearing mouse model without the induction of observable liver toxicity.
T64640	Melanin probe-2
	Melanoma is a lethal skin cancer. The early detection of melanoma using positron emission tomography (PET) probes is critical for improving the survival of melanoma patients. Melanin probe-2 is a non-radioactive bromo-picolinamide precursor that has been used for the synthesis of18F-picolinamides based PET probe (melanin probe-1). The tumor-targeting efficacy and imaging property of three melanin probes were evaluated in B16F10 tumor-bearing mice.18F-1 and18F-3 had much lower tumor uptake compar...

化合物

Cat.No: T1992

Synonym: DM1,Maytansinoid DM1

Target: Microtubule Associated

PRL-3 Inhibitor I

Cat.No: T22136

Synonym: PRL-3 Inhibitor,BR-1

Target: Phosphatase, Others

Cat.No: T2586

Synonym: 卡博替尼,XL184,BMS-907351

Target: Apoptosis, VEGFR, FLT, c-Met/HGFR, c-RET, TAM Receptor, c-Kit

Cabozantinib hydrochloride

Cat.No: T5164

Synonym: XL184,Cabozantinib hydrochloride (849217-68-1(free base)),BMS-907351,盐酸卡博替尼

Target: VEGFR, FLT, c-Met/HGFR, TAM Receptor, c-Kit, ROR

Cat.No: T77743

Target: Others

Cat.No: T76072

Tyrosinase-IN-13

Cat.No: T79401

Target: Tyrosinase

HEMTAC CDK4/6 degrader 1

Cat.No: T75029

Cat.No: T76072L

Dual photoCORM 1

Cat.No: T82524

Cat.No: T69269

Cat.No: T69447

Melanin probe-2

Cat.No: T64640

Cat. No.	Product Name	Target	Signaling Pathways
TN6901	Methyl myristate 肉豆蔻酸甲酯,methyl tetradecanoate	Others	Others
	Methyl myristate (methyl tetradecanoate) 是一种肉豆蔻酸经酯化反应得到的饱和脂肪酸甲酯。对 B16F10 黑色素瘤具有显著的诱导作用。
TMA0958	Forsythoside F 连翘酯苷F,Arenarioside,三糖苯丙素苷	Xanthine Oxidase	Metabolism
	Forsythoside F (Arenarioside) 是一种黄嘌呤氧化酶 (xanthine oxidase) 抑制剂，具有抗高尿酸活性。
TN5086	Syringetin	Others	Others
	Syringetin 是一种存在于葡萄和葡萄酒中的类黄酮衍生物，可促进 B16F10 细胞的黑色素生成，抑制人肺腺癌中成骨细胞介导的破骨细胞生成。
TN6972	Methyl pentadecanoate	Others	Others
	Methyl pentadecanoate 是一种天然产物。它是由肉豆蔻酸酯化得到的饱和脂肪酸甲酯。肉豆蔻酸甲酯(Methyl myristate) 在 B16F10 黑色素瘤中显示出高黑色素诱导。
T0938	Thiabendazole 2-(4-Thiazolyl)benzimidazole,噻菌灵	Microtubule Associated; Mitochondrial Metabolism; Parasite	Cytoskeletal Signaling; Metabolism; Microbiology/Virology
	Thiabendazole (2-(4-Thiazolyl)benzimidazole) 是具有驱虫特性的苯并咪唑衍生物。
TN3605	Casegravol	Others	Others
	Casegravol shows antiproliferative activity against human gastric adenocarcinoma (MK-1), human uterus carcinoma (HeLa), and murine melanoma (B16F10) cells.
T75554	6-O-Isobutyrylbritannilactone
	6-O-Isobutyrylbritannilactone 是一种天然的黑素生成抑制剂。6-O-Isobutyrylbritannilactone 是一种倍半萜，可从英菊花中分离得到。6-O-Isobutyrylbritannilactone 抑制 IBMX 诱导 B16F10 细胞产生黑色素。6-O-Isobutyrylbritannilactone 也调控 ERK、PI3K/AKT 和 CREB，在斑马鱼胚胎模型中显示出抗黑色素原活性。
TN5300	Citrostadienol
	Citrostadienol shows cytotoxic activity against B16F10 melanoma cells.
T28522	Reticulol
	Reticulol is an isocoumarin derivative produced by certain species of Streptomyces. Reticulol inhibits cAMP phosphodiesterase (IC50 = 41 µM). Recticulol (M.W. 222.2) exhibits a potent in vitro cytotoxicity against the human lung tumor cell line A427 and the mouse melanoma cell line B16F10.
TN3644	Chlorophorin	Tyrosinase; Antifection	Microbiology/Virology; Proteases/Proteasome
	Chlorophorin shows high anti-protozoal activity with an MIC of 0.25 microg/ml. Chlorophorin can strongly inhibit mushroom tyrosinase activity with IC50 values of 2.5 ± 0.408 uM; it inhibits α-melanocyte-stimulating hormone-induced melanin production in B16F10 melanoma cells.
TN5477	GB-2a
	GB 2a shows antioxidant and anti-inflammatory effects, it can prevent the carrageenan-induced paw oedema. GB 2a biflavonoid can promote inhibition on tyrosinase activity and reduced melanin biosynthesis in B16F10 cells, which suggests great potential for

天然产物

Methyl myristate

Cat.No: TN6901

Synonym: 肉豆蔻酸甲酯,methyl tetradecanoate

Target: Others

Cat.No: TMA0958

Synonym: 连翘酯苷F,Arenarioside,三糖苯丙素苷

Target: Xanthine Oxidase

Cat.No: TN5086

Target: Others

Methyl pentadecanoate

Cat.No: TN6972

Target: Others

Cat.No: T0938

Synonym: 2-(4-Thiazolyl)benzimidazole,噻菌灵

Target: Microtubule Associated, Mitochondrial Metabolism, Parasite

Cat.No: TN3605

Target: Others

6-O-Isobutyrylbritannilactone

Cat.No: T75554

Cat.No: TN5300

Cat.No: T28522

Cat.No: TN3644

Target: Tyrosinase, Antifection

Cat.No: TN5477

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