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25

抑制剂 & 化合物

2

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T15411	GPNA hydrochloride	Apoptosis; Others	Apoptosis; Others
	GPNA hydrochloride 是一种 γ-谷氨酰转移酶的知名底物，可逆地诱导 A549 细胞凋亡。它是一种特定的谷氨酰胺转运蛋白ASCT2抑制剂，还抑制依赖 Na+的载体，如 SNAT 家族 (SNAT1/2/4/5) 和不依赖 Na+的亮氨酸转运蛋白 LAT1/2。
T25450L	GGTI 2147 FA GGTI2147 FA,GGTI-2147 FA,GGTI 2147 FA(191102-87-1 Free base)	Others	Others
	GGTI 2147 FA 是一种选择性 GGT 抑制剂，在海马体实验中双库林诱导的树突棘密度增加被消除，可能会降低小鼠的学习和记忆能力。
T25450	GGTI 2147 GGTI2147,Geranylgeranyl transferase inhibitor-2147,GGTI-2147	NF-κB; Rho	Cell Cycle/Checkpoint; NF-κB
	GGTI 2147 降低 Rac1 活性，下调 p65 的表达，改善 OGD/R 诱导的神经元凋亡。
T24088	GGTI-2133 GGTI2133,GGTI 2133	Transferase	Metabolism
	GGTI-2133 是一种有效的仿肽基香叶基转移酶 I 型抑制剂（GGTase I），IC50值为38 nM。GGTI-2133 可抑制小鼠实验性哮喘中炎症细胞向气道的侵袭。
T62980	GGTI-286 hydrochloride
	GGTI-286 hydrochloride 是一种 GGTase I 的高效抑制剂 (IC50: 2 μM)，也能够有效抑制 K-Ras4B (IC50: 1 μM)。GGTI-286 hydrochloride 在 NIH3T3 细胞中，对 Rap1A 香叶香叶基化的抑制作用高于 H-Ras 的法尼化作用 (IC50=2和 >30 μM)。
T62379	GGTI-286
	GGTI-286 是一种高效的、具有细胞通透性 GGTase I 抑制剂 (IC50: 2 μM)。GGTI-286 对 NIH3T3 细胞中的 Rap1A 香叶香叶基化的(IC50: 2 μM)抑制作用强于 H-Ras 的法尼化作用(IC50>30 μM)。GGTI-286 也可以有效抑制 K-Ras4B 刺激(IC50: 1 μM)。
T62844	GGTI-2154 hydrochloride
	GGTI-2154 hydrochloride 是一种有效的、选择性的 geranylgeranyltransferase I (GGTase I) 抑制剂 (IC50: 21 nM)。GGTI-2154 hydrochloride 对 GGTase I 的选择性是 FTase (IC50: 5600 nM) 的 200 倍以上。GGTI-2154 hydrochloride 能够用于研究癌症。
T69205	GGTI-2166
	GGTI-2166 is a geranylgeranyl transferase I inhibitor. GGTI-2166 inhibit the pOC formation induced by RANKL or TNF-alpha in cultures of both mouse marrow-derived macrophage-colony-stimulating factor (M-CSF) dependent monocytes (MD cells) and the mouse monocyte cell line RAW 264.7 (RAW cells). GGTI-2166 inhibited TRAP activity induced by RANKL or TNF-alpha in both cell cultures and prevented the incorporation of [3H]all-trans geranylgeraniol into prenylated proteins in RAW cells.
T11396	GGTI-2418	Transferase	Metabolism
	GGTI-2418 inhibits GGTase I and FTase activities with IC50s of 9.5 nM and 53 μM, respectively. GGTI-2418 also increases p27(Kip1) and induces significant regression of breast tumors. GGTI-2418 is a highly potent, competitive, and selective geranylgeranyltransferase I (GGTase I) inhibitor.
T70157	GGTI-297
	GGTI-297 is a potent, cell-permeable, and selective peptidomimetic inhibitor of GGTase I compared to Farnesyl Transferase (FTase).
T73822	GGTI-286 TFA
	GGTI-286 TFA 是一种高效的细胞通透性 GGTase I 抑制剂，(IC50为 2 μM。在 NIH3T3 细胞中，GGTI-286 TFA 对 Rap1A 香叶香叶基化的抑制作用高于 H-Ras 的法尼化作用 (IC50s=2 和 >30 μM)。GGTI-286 TFA 还能有效抑制 K-Ras4B 刺激，IC50为 1 μM。
T27412	GGTI2417 GGTI-2417
	GGTI2417 is a potent and selective inhibitor of Geranylgeranyltransferase I. GGTI2417 targets RalB to inhibit anchorage-dependent growth and induce apoptosis and RalA to inhibit anchorage-independent growth.
T11397	GGTI298	Others	Others
	GGTI298 is a CAAZ peptidomimetic geranylgeranyltransferase I (GGTase I) inhibitor, strongly inhibiting the processing of geranylgeranylated Rap1A with little effect on processing of farnesylated Ha-Ras, with IC50 values of 3 and > 20 μM in vivo, respectively.
T6844	GGTI298 Trifluoroacetate GGTI 298,GGTI 298 TFA salt	Apoptosis; Transferase; Ras	Apoptosis; GPCR/G Protein; MAPK; Metabolism
	GGTI298 Trifluoroacetate (GGTI 298 TFA salt) 是一种GGTase I 抑制剂，能够抑制Rap1A 且IC50值为3μM，对Ha-Ras 的作用很小IC50值 > 20 μM。
T37446	GGTI-2154
	GGTI-2154 is a potent, selective geranylgeranyltransferase I (GGTase I) inhibitor, boasting an IC50 of 21 nM and demonstrating over 200-fold selectivity against FTase (IC50=5600 nM). Its efficacy and specificity make it a valuable tool for cancer research[1][2].
T22128	OU749	Transferase	Metabolism
	OU749 是一种 γ-谷氨酰转移酶 (GGT) 抑制剂，固有 Ki 值为 17.6 μM。
T5415	γ-GT H-GLA(PNA)-OH,L-谷氨酸 5-(3-甲酸-4硝基苯胺)铵盐	Others	Others
	γ-GT (H-GLA(PNA)-OH) 是一种 γ-谷氨酰转移酶(glutamyl transferase)的底物。
T11282	FGTI-2734	Transferase	Metabolism
	FGTI-2734 是有效的RAS C-末端法尼基转移酶 (FT) 和香叶烯基转移酶-1 (GGT-1) 抑制剂，IC50s 分别为 250 nM 和 520 nM。它可以阻断 KRAS 的膜定位，从而解决 KRAS 耐药性问题，并抑制突变的 KRAS 胰腺肿瘤。
T15379	GGsTop Nahlsgen	Others	Others
	GGsTop is a non-toxic and irreversible inhibitor of γ glutamyl transpeptidase (GGT) (Ki: 170 μM for Human GGT). GGsTop protects hepatic ischemia-reperfusion injury in the rat model. GGsTop shows Kons of 150±10 and 51±3 /(M·s) against E.coli GGT and human GGT, respectively.
T11282L	FGTI-2734 mesylate (1247018-19-4 free base) FGTI-2734 mesylate	Others	Others
	FGTI-2734 mesylate, a RAS C-terminal mimetic compound with dual farnesyl transferase (FT) and geranylgeranyl transferase-1 (GGT) inhibitory activities (IC50s of 250 nM and 520 nM for FT and GGT, respectively), mitigates KRAS resistance by preventing its membrane localization, effectively impeding mutant KRAS patient-derived pancreatic tumors.
T11330	FTI-2148 diTFA	Others	Others
	FTI-2148 diTFA is a RAS C-terminal mimetic dual farnesyl transferase (FT-1) and geranylgeranyl transferase-1 (GGT-1) inhibitor with IC50s of 1.4 nM and 1.7 μM, respectively.
T20638	Silthiofam MON 65500,Silthiopham,Latitude,MON65500,MON-65500
	Silthiofam is very effective against Gaeumannomyces graminis var. tritici (Ggt), recently it has been widely used for the take-all control in China. Ggt could cause Wheat take-all.
T11330L	FTI-2148	Others	Others
	FTI-2148 is an inhibitor of RAS C-terminal mimetic dual farnesyl transferase (FT-1) and geranylgeranyl transferase-1 (GGT-1) (IC50s: 1.4 nM and 1.7 μM, respectively).
T82852	BMI-Glu
	BMI-Glu，一种选择性γ-谷氨酰转肽酶(GGT)荧光探针，具有Km值为69.63 µM的高敏感性，以及优异的水溶性和生物相容性。
T81233	S-(p-Nitrobenzyl)glutathione
	S-(p-Nitrobenzyl)glutathione 是一种竞争性谷胱甘肽酶(GGT)抑制剂，能被大鼠肾微粒体转化成相应的半胱氨酸衍生物。该化合物用于研究谷胱甘肽酶系统中GSH的代谢及其降解过程。

化合物

GPNA hydrochloride

Cat.No: T15411

Target: Apoptosis, Others

Cat.No: T25450L

Synonym: GGTI2147 FA,GGTI-2147 FA,GGTI 2147 FA(191102-87-1 Free base)

Target: Others

Cat.No: T25450

Synonym: GGTI2147,Geranylgeranyl transferase inhibitor-2147,GGTI-2147

Target: NF-κB, Rho

Cat.No: T24088

Synonym: GGTI2133,GGTI 2133

Target: Transferase

GGTI-286 hydrochloride

Cat.No: T62980

Cat.No: T62379

GGTI-2154 hydrochloride

Cat.No: T62844

Cat.No: T69205

Cat.No: T11396

Target: Transferase

Cat.No: T70157

Cat.No: T73822

Cat.No: T27412

Synonym: GGTI-2417

Cat.No: T11397

Target: Others

GGTI298 Trifluoroacetate

Cat.No: T6844

Synonym: GGTI 298,GGTI 298 TFA salt

Target: Apoptosis, Transferase, Ras

Cat.No: T37446

Cat.No: T22128

Target: Transferase

Cat.No: T5415

Synonym: H-GLA(PNA)-OH,L-谷氨酸 5-(3-甲酸-4硝基苯胺)铵盐

Target: Others

Cat.No: T11282

Target: Transferase

Cat.No: T15379

Synonym: Nahlsgen

Target: Others

FGTI-2734 mesylate (1247018-19-4 free base)

Cat.No: T11282L

Synonym: FGTI-2734 mesylate

Target: Others

Cat.No: T11330

Target: Others

Cat.No: T20638

Synonym: MON 65500,Silthiopham,Latitude,MON65500,MON-65500

Cat.No: T11330L

Target: Others

Cat.No: T82852

S-(p-Nitrobenzyl)glutathione

Cat.No: T81233

Cat. No.	Product Name	Target	Signaling Pathways
T14114	Acivicin 阿西维辛,AT-125,U-42126	Others	Others
	Acivicin (AT-125) is a γ-glutamyl transpeptidase (GGT) inhibitor derived from the Streptomyces sviceus natural product. It possesses anti-cancer and anti-parasitic properties and can effectively cross the blood-brain barrier[1][2].
T77207	Acivicin hydrochloride
	Acivicin hydrochloride (AT-125 hydrochloride)，一种猪链霉菌的天然产物，兼具透过血脑屏障的能力，是γ-谷氨酰转肽酶 (GGT) 的抑制剂，具有抗癌和抗寄生虫的特性。

天然产物

Cat.No: T14114

Synonym: 阿西维辛,AT-125,U-42126

Target: Others

Acivicin hydrochloride

Cat.No: T77207

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