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36

抑制剂 & 化合物

1

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Cat. No.	Product Name	Target	Signaling Pathways
T6847	GSK-J1 GSK J1	Histone Demethylase	Chromatin/Epigenetic
	GSK-J1 是一种高效的 H3K27 组蛋白去甲基化酶抑制剂，在无细胞试验中对 JMJD3 (KDM6B) 和 UTX (KDM6A) 的 IC50 分别为 28 nM 和 53 nM，比其他测试的去甲基化酶选择性高 10 倍以上。
T11475	GSK-J1 lithium salt	Histone Demethylase	Chromatin/Epigenetic
	GSK-J1 lithium salt 是一种有效的 H3K27me3/me2-去甲基化酶 JMJD3/KDM6B 和 UTX/KDM6A 的抑制剂，对 KDM6B 的 IC50值为 60 nM。
T71916	GSK-J1 sodium salt
	GSK-J1 sodium salt is a potent inhibitor of the H3K27 histone demethylases JMJD3 and UTX.
T68836	ADS-J1
	ADS-J1 is an HIV-1 entry inhibitor that potently inhibits seminal amyloid fibrillization and block fibril-mediated enhancement of viral infection. Semen-derived amyloid fibrils, comprising SEVI (semen-derived enhancer of viral infection) fibrils and SEM1 fibrils, may remarkably enhance HIV-1 sexual transmission and are potential targets for the development of an effective microbicide.
T33281	Melflufen Prodrug J-1, Melflufen, Melphalan flufenamide,Melphalan flufenamide,J 1,J1,J-1
	Melphalen fluoroaniline, also known as melphalen, J-1, or prodrug J-1, is a prodrug of melphalen, in which the alkylating agent melphalen is combined with fluoroaniline and has potential antitumor and antiangiogenic activities.
T12908	SIBA 5'-Deoxy-5'-isobutylthioadenosine,5'-Isobutylthioadenosine,5ˊ-异丁硫基-5ˊ-脱氧腺苷	Nucleoside Antimetabolite/Analog; HSV	Cell Cycle/Checkpoint; DNA Damage/DNA Repair; Microbiology/Virology
	SIBA (5'-Deoxy-5'-isobutylthioadenosine) 是 SAH 的合成类似物，可作为 S-腺苷甲硫氨酸介导的甲基转移的抑制剂。它干扰多种酶活性，可逆地阻断单纯疱疹病毒 1 型病毒的繁殖。
T5512	JNJ16259685 .TN.T 16259685	GluR	Neuroscience
	JNJ16259685 (TN.T 16259685) 是选择性mGlu1 受体拮抗剂，可浓度依赖性地抑制 mGlu1 的突触的活化，IC50值为 19 nM。
T9980	AVJ16	IGF-1R	Tyrosine Kinase/Adaptors
	AVJ16作为胰岛素生长因子2 mRNA 结合蛋白家族的成员，可与某些基因的mRNA 结合来调节蛋白质翻译。
T4251	GJ103 sodium salt	ATM/ATR	DNA Damage/DNA Repair; PI3K/Akt/mTOR signaling
	GJ103 sodium salt 是 GJ072 的活性类似物，它是一种通读化合物 (RTC)。它已被证明可以降低水溶液的表面张力，使分子更容易在溶液中移动。它还被证明可以降低水溶液的粘度，使分子更容易在溶液中移动。此外，它还被证明可以降低水溶液的pH 值，这会对生物体的生化和生理过程产生各种影响。
T8320	J14 J-14	Reactive Oxygen Species	Immunology/Inflammation; Metabolism; NF-κB
	J14 是一种可逆的 sulfiredoxin 抑制剂，IC50=8.1 μM。它能够抑制sulfiredoxin 诱导氧化应激，使细胞内ROS 积累，导致细胞毒性和癌细胞死亡。
T3448	GJ103	Others	Others
	GJ103 是通读化合物 GJ072 的活性类似物。一些 GJ072 类似物（例如，GJ103、GJ106、GJ109 和 GJ111）通过 FCATMpSer1981 和 IRIF 测定一致地证明了它们在所有三种 PTC 中的活性。 GJ103 具有与 RTC13 或 RTC14 相似的通读活性，但比 RTC13 和 RTC14 对 A-T 细胞的耐受性更高。
TP1906L1	DPC AJ1951 acetate	Thyroid hormone receptor(THR)	Endocrinology/Hormones
	DPC-AJ1951 acetate 是一种 14 个氨基酸的肽，可作为甲状旁腺激素 (PTH)/PTH 相关肽受体 (PPR) 的有效激动剂。在骨吸收的体外和体内测定中表征了它的活性。
T9104	TJ191	Apoptosis	Apoptosis
	TJ191 是一种选择性抗癌试剂，靶向低 TβRIII 表达的恶性T 细胞白血病/淋巴瘤细胞，可研究癌症。
T75942	DPC-AJ1951 TFA
	DPC-AJ1951 TFA，是一种含有14个氨基酸的肽类化合物，有效充当甲状旁腺激素(PTH)/PTH相关肽受体(PPR)激动剂，在体外及体内骨吸收实验中展现活性。
T79387	YJ182
	YJ182为NDM-1抑制剂（IC50：0.23 μM）。该化合物同样针对IMP-1、VIM-2、GIM-1和MMP-2具有抑制作用，其IC50值分别为0.25 μM、0.61 μM、0.49 μM及6.92 μM。YJ182适用于细菌感染的研究领域。
T37409	DPC-AJ1951 (trifluoroacetate salt) DPC-AJ1951 (trifluoroacetate salt)
	DPC-AJ1951 is a peptide agonist of the parathyroid hormone (PTH)/PTH-related peptide receptor (PPR; EC50 = 0.15 nM in HEK293 cells expressing human PPR). It induces cAMP production in SAOS-2 and UMR106 cells that endogenously express human and rat PPR, respectively (EC50s = 2.2 and 1.1 nM, respectively). DPC-AJ1915 stimulates osteoclast-mediated bone resorption in fetal rat long-bone explant cultures and increases collagen synthesis and cell proliferation in neonatal mouse parietal bone explants...
T27648	J1075 J 1075,J-1075
	J1075 is an histone deacetylase 8 (HDAC8) inhibitor.
T74429	SJ10542	PROTACs	PROTAC
	SJ10542 是一种有效的选择性 JAK2/3导向苯基戊二酰亚胺 (PG)-PROTAC，对 JAK2、JAK3 和 JAK2-fusion ALL 的 DC50分别为 14、11 和 24 nM。SJ10542 利用 PG 配体作为cereblon(CRBN) 招募剂。
T78682	SJ1461	Epigenetic Reader Domain	Chromatin/Epigenetic
	SJ1461为一种BET抑制剂，具有口服活性。该化合物针对BRD2(BD1)、BRD2(BD2)、BRD4(BD1)与BRD4(BD2)展现出抑制作用，对应IC50值依次为1.6 nM、0.1 nM、6.5 nM及0.2 nM。
T27644	J1037 J 1037,J-1037
	J1037 is a novel Histone Deacetylase 8 (HDAC8) inhibitor .
T27665	JNJ1930942 JNJ-1930942,JNJ 1930942
	JNJ1930942 is a novel positive allosteric modulator of the α7 nicotinic acetylcholine receptor.
T32450	L 643717-01J10 L643717-01J10,L-643717-01J10,L643,717-01J10,L 643,717-01J10,L-643,717-01J10
	L 643717-01J10 is a bioactive chemical.
TP1906	DPC-AJ1951 DPC AJ1951
	Potent 14 amino acid peptide agonist of the parathyroid hormone (PTH) receptor (EC50 = 26 nM).
T77943	SJ1008030 TFA	JAK; PROTACs	Angiogenesis; Chromatin/Epigenetic; JAK/STAT signaling; PROTAC; Stem Cells
	SJ1008030 TFA（化合物8）是一种针对JAK2的PROTAC，能够选择性地降解JAK2蛋白。该化合物在抑制MHH-CALL-4细胞系增殖方面表现出显著效能，其IC50值为5.4 nM。SJ1008030 TFA主要应用于白血病相关研究。
T68317	VJ115
	VJ115 is a novel chemical entity that inhibits the enzyme ENOX1, a NADH oxidase. Genetic and small molecule inhibition of ENOX1 inhibits endothelial cell tubule formation and tumor-mediated neo-angiogenesis. Inhibition of ENOX1 radiosensitizes tumor vasculature, a consequence of enhanced apoptosis. VJ115 inhibition of ENOX1 can impact expression of proteins involved in cytoskeletal reorganization and support a hypothesis in which ENOX1 activity links elevated cellular NADH concentrations with cy...
T74580	SJ1008030
	SJ1008030 (compound 8) 是一种JAK2PROTAC 选择性地降解JAK2。SJ1008030 对 MHH–CALL-4 细胞系的EC50值为 5.4 nM，IC50值为 32.09 nM。SJ1008030 可用于白血病的研究。
T27645	J1038 J-1038,J 1038
	J1038 is a novel Histone Deacetylase 8 (HDAC8) Inhibitor .
T77944	SJ1008030 formic	PROTACs	PROTAC
	SJ1008030 formic（化合物8）是一款针对JAK2的PROTAC，能够选择性地降解JAK2。该化合物在抑制MHH-CALL-4细胞系增殖方面表现出5.4 nM的IC50值，适用于白血病的研究。
T80754	YJ196
	YJ196（Compound 59）作为一种新德里金属-β-内酰胺酶-1（NDM-1）抑制剂，拥有潜在的应用价值。
T71192	JJ1
	JJ1 is a potent, direct, and selective inhibitor of thrombin, which inhibits human platelet aggregation induced by thrombin in a concentration-dependent manner.
T80433	δ-Buthitoxin-Hj1a	Sodium Channel	Membrane transporter/Ion channel
	δ-Buthitoxin-Hj1a为蝎毒肽，作为NaV1.1激动剂具有高效性，其半最大有效浓度(EC50)为17 nM。该化合物适用于Dravet综合征(DS)的研究领域。
T69437	NDJ18
	NDJ18 is a potent and selective SIRT2 inhibitor which validated the in silico protocol and opened up the possibility for generalization and broadening of its application. The anticancer effects of the most potent compound NDJ18 were examined on the triple-negative breast cancer cell line. Results indicated that NDJ18 represents a promising structure suitable for further evaluation.
T24005	DJ101 DJ-101,DJ 101
	DJ101is an effective and metabolically stable inhibitor of tubulin. It can circumvent the drug efflux pumps responsible for multidrug resistance of existing tubulin inhibitors.
T4383	GSK-J4 Hydrochloride GSK J4 HCl,GSK J4 HCl (1373423-53-0 free base)	Histone Demethylase	Chromatin/Epigenetic
	GSK-J4 Hydrochloride (GSK J4 HCl) 是 H3K27me3/me2 去甲基化酶 JMJD3/KDM6B 和 UTX/KDM6A 双抑制剂，IC50分别为 8.6 和 6.6 μM。它是 GSK-J1 的乙酯衍生物，体外 IC50 值大于 50 μM。它抑制 LPS 诱导的人原代巨噬细胞产生 TNF-α，IC50值为 9 μM。
T3100	GSK-J4 GSK J4 HCl	Apoptosis; Histone Demethylase	Apoptosis; Chromatin/Epigenetic
	GSK-J4 (GSK J4 HCl) 是 H3K27me3/me2 去甲基化酶JMJD3/KDM6B 和UTX/KDM6A 双抑制剂，IC50分别为 8.6 μM 和 6.6 μM。它是 GSK-J1 的细胞通透性前药，可诱导内质网应激相关的细胞凋亡。它抑制 LPS 诱导的人原代巨噬细胞产生 TNF-α，IC50值为 9 μM。
T11476	GSK-J2	Others	Others
	GSK-J2, an isomer of GSK-J1, haven't any specific activity. GSK-J1 is a potent inhibitor of H3K27me3/me2-demethylases JMJD3/KDM6B and UTX/KDM6A.

化合物

Cat.No: T6847

Synonym: GSK J1

Target: Histone Demethylase

GSK-J1 lithium salt

Cat.No: T11475

Target: Histone Demethylase

GSK-J1 sodium salt

Cat.No: T71916

Cat.No: T68836

Cat.No: T33281

Synonym: Prodrug J-1, Melflufen, Melphalan flufenamide,Melphalan flufenamide,J 1,J1,J-1

Cat.No: T12908

Synonym: 5'-Deoxy-5'-isobutylthioadenosine,5'-Isobutylthioadenosine,5ˊ-异丁硫基-5ˊ-脱氧腺苷

Target: Nucleoside Antimetabolite/Analog, HSV

Cat.No: T5512

Synonym: .TN.T 16259685

Target: GluR

Cat.No: T9980

Target: IGF-1R

GJ103 sodium salt

Cat.No: T4251

Target: ATM/ATR

Cat.No: T8320

Synonym: J-14

Target: Reactive Oxygen Species

Cat.No: T3448

Target: Others

DPC AJ1951 acetate

Cat.No: TP1906L1

Target: Thyroid hormone receptor(THR)

Cat.No: T9104

Target: Apoptosis

Cat.No: T75942

Cat.No: T79387

DPC-AJ1951 (trifluoroacetate salt)

Cat.No: T37409

Synonym: DPC-AJ1951 (trifluoroacetate salt)

Cat.No: T27648

Synonym: J 1075,J-1075

Cat.No: T74429

Target: PROTACs

Cat.No: T78682

Target: Epigenetic Reader Domain

Cat.No: T27644

Synonym: J 1037,J-1037

Cat.No: T27665

Synonym: JNJ-1930942,JNJ 1930942

Cat.No: T32450

Synonym: L643717-01J10,L-643717-01J10,L643,717-01J10,L 643,717-01J10,L-643,717-01J10

Cat.No: TP1906

Synonym: DPC AJ1951

Cat.No: T77943

Target: JAK, PROTACs

Cat.No: T68317

Cat.No: T74580

Cat.No: T27645

Synonym: J-1038,J 1038

SJ1008030 formic

Cat.No: T77944

Target: PROTACs

Cat.No: T80754

Cat.No: T71192

δ-Buthitoxin-Hj1a

Cat.No: T80433

Target: Sodium Channel

Cat.No: T69437

Cat.No: T24005

Synonym: DJ-101,DJ 101

GSK-J4 Hydrochloride

Cat.No: T4383

Synonym: GSK J4 HCl,GSK J4 HCl (1373423-53-0 free base)

Target: Histone Demethylase

Cat.No: T3100

Synonym: GSK J4 HCl

Target: Apoptosis, Histone Demethylase

Cat.No: T11476

Target: Others

Cat. No.	Product Name	Target	Signaling Pathways
T25562	Justicidin D Neojusticin A,Neojusticin,Lignan J1
	Justicidin D is a lignan that has antiviral activities.

天然产物

Cat.No: T25562

Synonym: Neojusticin A,Neojusticin,Lignan J1

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