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抑制剂 & 化合物

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Cat. No.	Product Name	Target	Signaling Pathways
T24871	TFMB-(S)-2-HG TFMB(S)2HG,TFMB-S-2-HG,TFMB (S) 2 HG,TFMB S 2 HG	DNA Methyltransferase	Chromatin/Epigenetic
	TFMB-(S)-2-HG (TFMB S 2 HG) is a highly effective inhibitor of TET2, the 5'-methylcytosine hydroxylase. Additionally, it significantly inhibits the EglN prolyl hydroxylases. With its unique properties, TFMB-(S)-2-HG holds great promise for advancing research in the field of acute myeloid leukemia (AML).
T17065	TFMB-(R)-2-HG	Others	Others
	TFMB-(R)-2-HG 是一种具有细胞膜渗透性的 (R)-2-HG，急性髓细胞性白血病的致癌因子。它能够响应雌激素戒断损害 SCF ER-Hoxb8 细胞分化。
T67839	HG106	Others	Others
	HG106具有抗炎作用，可用于治疗由 RAS 基因突变引起的各种恶性肿瘤等疾病的生长。
T16384	Olutasidenib FT-2102	Dehydrogenase; Isocitrate Dehydrogenase (IDH)	Metabolism
	Olutasidenib (FT-2102) 是一种可透过血脑屏障的、具有口服活性的、突变型异柠檬酸脱氢酶(IDH)1的选择性有效抑制剂，对IDH1- R132H 和 IDH1- R132C 的IC50分别为 21.2 nM 和 114 nM，可用于急性髓性白血病或骨髓增生异常综合征的研究。
T19612	(2S)-Octyl-α-hydroxyglutarate (2S)-Octyl-2-HG	Others	Others
	(2S)-Octyl-α-hydroxyglutarate ((2S)-Octyl-2-HG) is a S-isomer 2-Hydroxyglutarate modified form.
T7196	HG-10-102-01 [4-[[5-氯-4-(甲基氨基)-2-嘧啶基]氨基]-3-甲氧基苯基]-4-吗啉基甲酮	LRRK2	Autophagy
	HG-10-102-01 是富含亮氨酸重复激酶 2 和突变型G2019S 抑制剂，IC50分别为20.3 nM 和3.2 nM。
T19611	(2R)-Octyl-α-hydroxyglutarate (2R)-Octyl-2-HG	Pim	Chromatin/Epigenetic; JAK/STAT signaling
	(2R)-Octyl-α-hydroxyglutarate ((2R)-Octyl-2-HG) is a D-isomer 2-Hydroxyglutarate modified form.
T3617	Ivosidenib 艾伏尼布,AG-120	Dehydrogenase; Isocitrate Dehydrogenase (IDH)	Metabolism
	Ivosidenib (AG-120) 是一种口服具有活力的异柠檬酸脱氢酶 1 的突变体酶 (mIDH1 enzyme) 抑制剂，能够使 d-2- hydroxyglutatrate (2-HG) 在体内降低。它具有良好的的安全性和临床活性，具有研究 AML 的潜力。
T15551	IDH889	Dehydrogenase	Metabolism
	IDH889 是可口服有效的，脑渗透性的，变构和突变特异性的异柠檬酸脱氢酶抑制剂，对 IDH1 R132* 突变型具有高效选择性。它高效抑制细胞内 2-HG 水平，IC50为 0.014 μM。
T62698	mIDH1-IN-1
	mIDH1-IN-1 (compound 43) 是一种有效的、选择性的 mIDH1 (异柠檬酸脱氢酶 1 突变体) 抑制剂 (IC50: 961.5 nM)。mIDH1-IN-1 可以有效抑制 HT1080 细胞内 2-HG (2-hydroxyglutarate) 的产生 (EC50: 208.6±8.0 nM)。mIDH1-IN-1 对 IDH1 突变体 U-87 细胞表现出明显的抗增殖效果(IC50: 41.8 nM)。mIDH1-IN-1 是一种抗肿瘤剂，能够用于研究 IDH1 突变实体瘤。
T32009	GSK321 GSK 321,GSK-321
	GSK321 is an effective and selective IDH1 mutation inhibitor, which can effectively inhibit the production of 2-HG in HT-1080 cells, and induce IDH1 mutant cells to differentiate into bone marrow at the level of leukemia blasts and more stem cells.
T38653	HG-7-85-01
	HG-7-85-01 is a type II ATP competitive inhibitor targeting wild-type and gatekeeper mutations forms of Bcr-Abl, PDGFRα, Kit, and Src kinases. It effectively inhibits T315I mutant Bcr-Abl kinase, as well as KDR and RET kinases with IC50 values of 3 nM, 20 nM, and 30 nM, respectively. In contrast, HG-7-85-01 exhibits weak or no inhibition towards other kinases (IC50 >2 μM). Furthermore, this compound inhibits cell proliferation through the induction of apoptosis and by impeding cell-cycle progres...
T18692	SNIPER(ABL)-047	Others	Others
	SNIPER(ABL)-047, conjugating HG-7-85-01 (ABL inhibitor) to MV-1 (IAP ligand) with a linker, induces the reduction of BCR-ABL protein with a DC50 of 2 μM[1].
T70932	L6H9
	L6H9 is a novel inhibitor of myeloid differentiation factor 2 (MD2), suppressing HG-induced expression of ACE and AT1 receptor and Angiotensin II (AngII) production in renal NRK‐52E cells, resulting in the decrease in fibrosis markers such as TGF-β and collagen IV.
T70890	ML309
	ML309 is a potent inhibitor of R132H mutant IDH1 capable of reducing 2-hydroxyglutarate production in U87 MG glioblastoma cells. ML309 is capable of potent and selective inhibition of mutant IDH1 and effectively lowers cell-based production of 2-HG in a U87MG mutant glioblastoma cell line.
T63402	(S,R)-WT IDH1 Inhibitor 2
	(S,R)-WT IDH1 Inhibitor 2 是选择性的、有效的突变型 IDH1抑制剂，能够抑制 R132G (IC50: 2.9 nM)、R132C (IC50: 3.8 nM)、R132H (IC50: 4.6 nM) 和 WT IDH1 (IC50: 46 nM)，选择性比 IDH2 高出 100 倍。(S,R)-WT IDH1 Inhibitor 2 具有诱导细胞内 2-HG 减少，髓细胞分化阻滞失效的作用，并且在白血病母细胞和更不成熟的干细胞水平诱导粒细胞分化，可研究用于急性髓系白血病 (AML) 及其他癌症。
T78758	IHMT-IDH1-053	Isocitrate Dehydrogenase (IDH)	Metabolism
	IHMT-IDH1-053（compound 16）为高选择性不可逆IDH1R132H突变抑制剂，IC50值仅为4.7 nM。对IDH1wt和IDH2wt/突变体活性低。该化合物在IDH1R132H突变293T细胞中显著抑制2-羟基戊二酸（2-HG）生成，IC50为28 nM。IHMT-IDH1-053通过与IDH1R132H蛋白的Cys269残基形成共价键，结合至NADPH结合袋附近的变构袋。此外，它能够抑制携带IDH1R132突变的HT1080细胞系及原代AML细胞增殖。
T38204	GAT229
	GAT229 is a positive allosteric modulator of cannabinoid receptor 1 (CB1) and the S-(-) enantiomer of the CB1 modulator GAT211. It does not activate the receptor on its own but enhances the binding and activity of CB agonists. GAT229 (1 μM) enhances the binding of the CB1 full agonist CP 55,940 to CHO cells expressing human recombinant CB1 (hCB1), as well as the activity of 2-arachidonoyl glycerol , arachidonoyl ethanolamide , and CP 55,940 in arrestin2 recruitment assays and increases ERK1/2 an...

化合物

Cat.No: T24871

Synonym: TFMB(S)2HG,TFMB-S-2-HG,TFMB (S) 2 HG,TFMB S 2 HG

Target: DNA Methyltransferase

Cat.No: T17065

Target: Others

Cat.No: T67839

Target: Others

Cat.No: T16384

Synonym: FT-2102

Target: Dehydrogenase, Isocitrate Dehydrogenase (IDH)

(2S)-Octyl-α-hydroxyglutarate

Cat.No: T19612

Synonym: (2S)-Octyl-2-HG

Target: Others

Cat.No: T7196

Synonym: [4-[[5-氯-4-(甲基氨基)-2-嘧啶基]氨基]-3-甲氧基苯基]-4-吗啉基甲酮

Target: LRRK2

(2R)-Octyl-α-hydroxyglutarate

Cat.No: T19611

Synonym: (2R)-Octyl-2-HG

Target: Pim

Cat.No: T3617

Synonym: 艾伏尼布,AG-120

Target: Dehydrogenase, Isocitrate Dehydrogenase (IDH)

Cat.No: T15551

Target: Dehydrogenase

Cat.No: T62698

Cat.No: T32009

Synonym: GSK 321,GSK-321

Cat.No: T38653

SNIPER(ABL)-047

Cat.No: T18692

Target: Others

Cat.No: T70932

Cat.No: T70890

(S,R)-WT IDH1 Inhibitor 2

Cat.No: T63402

Cat.No: T78758

Target: Isocitrate Dehydrogenase (IDH)

Cat.No: T38204

Cat. No.	Product Name	Target	Signaling Pathways
T81629	OAT1/3-IN-2
	OAT1/3-IN-2（化合物8）是一种针对OAT1和OAT3的双重抑制剂。该化合物能够以10 μM的浓度逆转Cys-Hg对HEK-OAT1细胞的毒害作用，并可能对肾脏具有保护效应。OAT1/3-IN-2适用于研究汞导致的肾脏损伤。

天然产物

Cat.No: T81629

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