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101

抑制剂 & 化合物

3

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T7121	Sulfaclozine 磺胺氯吡嗪,Sulfachloropyrazine,Sulfachloropyrazine sodium,N-(5-氯-3-吡嗪基)-4-氨基苯磺酰胺	Antibacterial; Antibiotic; Parasite	Microbiology/Virology
	Sulfachloropyrazine sodium(Sulfachloropyrazine) 是一种磺酰胺衍生物，具有抗菌和抗球虫作用。Sulfachloropyrazine sodium(Sulfachloropyrazine) 用于各种家禽疾病。
T16501	PF-3644022	p38 MAPK; Serine Protease; MAPK	MAPK; Proteases/Proteasome
	PF-3644022 是可口服的，具有 ATP 竞争性的MAPKAPK2 (MK2)选择性抑制剂，IC50为 5.2 nM，Ki 为 3 nM。它有效抑制 TNFα 的产生并具有抗炎作用，还抑制 MK3 和 p38 调节/激活激酶，IC50分别为 53 和 5.0 nM。
T6148	CX-6258 hydrochloride CX-6258 HCl,Pim-Kinase Inhibitor X	Pim	Chromatin/Epigenetic; JAK/STAT signaling
	CX-6258 hydrochloride (Pim-Kinase Inhibitor X) 是一种强效选择性的泛 Pim 激酶抑制剂，对Pim-1、Pim-2 和 Pim-3 作用的IC50值分别为 5、25 和 16 nM。
T15549	Icosabutate	Others	Others
	Icosabutate is a structurally engineered and orally active ω-3 polyunsaturated fatty acid. Icosabutate is well tolerated, and efficacious in lowering non-high-density lipoprotein cholesterol (non-HDL-C) levels in persistent hypertriglyceridemia.
T28073	MLS1547 MLS000051547,MLS 1547,MLS-1547	Dopamine Receptor	GPCR/G Protein; Neuroscience
	MLS1547 (MLS000051547) 是一种高效的 G 蛋白偏向多巴胺 D2 受体激动剂，Ki 为 1.2 μM。 MLS1547 在钙动员试验中刺激 D2R G 蛋白介导的信号传导，EC50 为 0.37 μM。
T12462	PI3Kδ-IN-1	PI3K	PI3K/Akt/mTOR signaling
	PI3Kδ-IN-1 是高效，选择性的 PI3Kδ 抑制剂，IC50 为 1.7 nM。
T3692	GNE-477 GNE 477	PI3K; mTOR	PI3K/Akt/mTOR signaling
	GNE-477 是一种高效的双重PI3K(IC50=4 nM)、mTOR(Ki=21 nM) 抑制剂。
T14217	AMG 579 AMG-579	PDE	Metabolism
	AMG 579 是一种有效的选择性 PDE10A 抑制剂 (IC50 = 0.1 nM)。
T14302	Olorinab APD 371	Cannabinoid Receptor	GPCR/G Protein
	Olorinab (APD 371) (APD 371) 是大麻素受体 2 型 (CB2) 强有效的、选择性的全激动剂，其对 hCB2 的EC50 值为 6.2 nM。
T3544	SHP099 hydrochloride	Phosphatase; Others	Metabolism; Others
	SHP099 hydrochloride 是一种有效的、选择性的、口服生物可利用的、有效的 SHP2 抑制剂。
T2338	JZL195	FAAH; Lipase; Autophagy	Autophagy; Metabolism; Neuroscience
	JZL195 是一种选择性有效的脂肪酸酰胺水解酶和单酰甘油脂肪酶双重抑制剂，IC50s 分别为 2 和 4 nM。
T12165	nAChR agonist 1 DUN71755	AChR	Neuroscience
	nAChR agonist 1 (DUN71755) 是一种脑渗透性和口服有效的正变构 α7 烟碱乙酰胆碱受体 (α7 nAChR) 调节剂。它在 Ca2+中，对内源性表达 α7 nAChR 的人 IMR-32 神经母细胞瘤细胞的EC50为 0.32 μM。它可用于阿尔茨海默病的研究。
T36526	IL-17 modulator 4	Interleukin	Immunology/Inflammation
	IL-17 modulator 4 是 IL-17 modulator 1 的前药，IL-17 modulator 1 是 IL-17 的有效调节剂。
T4690	Betrixaban hydrochloride(330942-05-7(free base)) PRT054021 hydrochloride,盐酸贝曲西班	Factor Xa	Metabolism
	Betrixaban hydrochloride(330942-05-7(free base)) (PRT054021 hydrochloride) 是一种有效的、选择性的、口服有效的 Xa 因子 (fXa) 抑制剂 (IC50: 1.5 nM)。
T12181	NaV1.7 inhibitor-1	Sodium Channel	Membrane transporter/Ion channel
	NaV1.7 inhibitor-1 是有效的、选择性的电压门控钠通道 (Nav) 1.7 抑制剂，对于hNaV1.7的IC50为 0.6 nM，其选择性是 hNaV1.5 的 80 倍。
T2030	Tiplaxtinin PAI-039,Tiplasinin	PAI-1; Apoptosis	Apoptosis; Metabolism
	Tiplaxtinin (Tiplasinin) 是一种具有口服活性的选择性纤溶酶原激活物抑制剂-1 抑制剂，IC50为 2.7 μM。
T14087	ABT-239	TRP/TRPV Channel	Membrane transporter/Ion channel
	ABT-239是一种新型、高效、非咪唑类H3R 拮抗剂，也是一种TRPV1拮抗剂。
T16996	TAS6417	Apoptosis; EGFR	Angiogenesis; Apoptosis; JAK/STAT signaling; Tyrosine Kinase/Adaptors
	TAS6417 是一种高效的、具有口服活性的 EGFR 突变型抑制剂，可独特的结合到 EGFR 铰链区的 ATP 结合位点，其 IC50值为 1.1-8.0 nM。
T11980	MD-224	Mdm2; E1/E2/E3 Enzyme; PROTACs	Apoptosis; PROTAC; Ubiquitination
	MD-224是一种基于蛋白水解靶向嵌合体（PROTAC）概念的高效、高效的MDM2降解剂，是一类新型抗癌剂。
T3564	SHP099 SHP099 free base,SHP 099,SHP-099	Phosphatase; PERK	Apoptosis; Metabolism
	SHP099 (SHP099 free base) free base 是一种选择性的，有效的，有口服活性的 SHP2抑制剂，IC50=70 nM。
TP1618L	PACAP-38 (31-38), human, mouse, rat acetate PACAP-38 (31-38), human, mouse, rat acetate(138764-85-9 Free base)	PACAP	GPCR/G Protein
	PACAP-38 (31-38), human, mouse, rat acetate 是 PAC1 受体的激活剂。PACAP-38 (31-38), human, mouse, rat acetate 对交感神经元 NPY 和儿茶酚胺的产生具有强效、有效和持续的刺激作用，可用于神经营养和神经保护研究。
T22360	MDR-652	TRP/TRPV Channel	Membrane transporter/Ion channel
	MDR-652是瞬时受体电位香草酸亚型 1 的选择性激动剂，对 hTRPV1 和 rTRPV1 的Ki 分别为 11.4 和 23.8 nM，EC50分别为 5.05 和 93 nM。MDR-652在缓解疼痛方面有研究的价值。
T10964	DB1976	Apoptosis; Others	Apoptosis; Others
	DB1976 是一种 DB270 的硒烯类似物，是一种高效且可渗透细胞的转录因子 PU.1 的抑制剂。在体外，DB1976 有效抑制 PU.1 结合 (IC50 为 10 nM)，可强烈抑制 PU.1/DNA 复合物 (具有高 DB1976-λB 亲和力，KD 为 12 nM)。DB1976 具有诱导细胞凋亡的作用。
T4615	Balsalazide sodium hydrate 巴柳氮钠水合物,Balsalazide disodium dihydrate,巴柳氮钠,Balsalazide disodium salt dihydrate,Balsalazide disodium	STAT; Interleukin	Immunology/Inflammation; JAK/STAT signaling; Stem Cells
	Balsalazide sodium hydrate (Balsalazide disodium) 可通过调节IL-6/STAT3通路起抑癌作用，可用于治疗炎症性肠病。
T16877	SHP394	Others	Others
	SHP394 is an orally efficacious inhibitor of protein tyrosine phosphatase SHP2 (IC50: 23 nM).
T40281	KRAS G12D inhibitor 6
	KRAS G12D inhibitor 6 is an efficacious compound that effectively inhibits KRAS G12D.
T27378	FR-193879 FR193879
	FR-193879 is an efficacious cephem derivative, it has extremely potent therapeutic efficacy against H. pylori.
T16020	MB05032	Others	Others
	MB05032 targeted the AMP binding site of fructose 1,6-bisphosphatase (FBPase), which is a special and efficacious inhibitor of GNG.
T36883	BM-1074
	BM-1074 is a potent and highly efficacious inhibitor of Bcl-2/Bcl-xL with Ki value of < 1nM [1].
TP1618	PACAP-38 (31-38), human, mouse, rat
	PACAP-38 (31-38), human, mouse, rat demonstrates potent, efficacious, and sustained stimulatory effects on sympathetic neuronal NPY and catecholamine production.
T69886	FE-200041
	FE-200041 is a peripheral efficacious kappa opioid agonist.
T15193	EBI-1051	MEK	MAPK
	EBI-1051 is a highly potent and orally efficacious inhibitor of MEK (IC50: 3.9 nM).
T40107	IL-17 modulator 4 sulfate
	IL-17 modulator 4 sulfate is a prodrug of IL-17 modulator 1 . IL-17 modulator 1 is an orally active, highly efficacious IL-17 modulator.
T15365	G-744	BTK	Angiogenesis; Tyrosine Kinase/Adaptors
	G-744 is a selective and orally active inhibitor of Btk (IC50: 2 nM). G-744 is well-tolerated, metabolically stable. It also has an efficacious to treat arthritis.
T26542	AC-7954
	AC-7954 is a potent and efficacious agonist of urotensin II receptor.
T17175	Troxacitabine BCH-4556,SGX-145,SGX145,SPD-758,BCH4556,beta-L-OddC	Others	Others
	Troxacitabine, a DNA polymerase inhibitor, is potentially used for the treatment of acute myeloid leukemia (AML). In comparison with gemcitabine, troxacitabine was equally active against MiaPaCa and was more efficacious against Panc-01.
T11275	Fesoterodine L-mandelate	Others	Others
	Fesoterodine L-mandelate is a efficacious antimuscarinic agent for the overactive bladder (OAB).
T10527	Betrixaban-d6 Betrixaban D6	Others	Others
	Betrixaban D6 is a deuterium-labeled Betrixaban. Betrixaban is a selective and orally efficacious FXa inhibitor.
T40106	IL-17 modulator 1
	IL-17 modulator 1 is an orally active small molecule. It is highly efficacious in modulating IL-17 and can effectively prevent, treat, or ameliorate various diseases such as psoriasis, ankylosing spondylitis, and psoriatic arthritis.
T15346	FR-190809	Others	Others
	FR-190809 is a nonadrenotoxic and orally efficacious inhibitor of acyl-CoA:cholesterol O-acyltransferase (ACAT) (IC50: 45 nM).
TP1619	PACAP-38 (16-38), human, mouse, rat
	PACAP-38 (16-38), human, mouse, rat demonstrates potent, efficacious, and sustained stimulatory effects on sympathetic neuronal NPY and catecholamine production.
T71353	CCT239065
	CCT239065 is a novel, selective, and efficacious nanomolar pyridopyrazinone V600EBRAF and LCK inhibitor.
T40321	TNF-α-IN-6
	TNF-α-IN-6 is an orally efficacious allosteric inhibitor of TNFα ( K D = 6.8 nM).
T81236	RyRs activator 5
	RyRs activator 5 (Compd A-1) 为针对Spodoptera frugiperda鸟苷酸受体的有效激动剂。
T39996	PROTAC CDK9 degrader-4 PROTAC CDK9 degrader-4
	PROTAC CDK9 degrader-4 is a potent and efficacious chemical compound designed specifically to degrade CDK9, a protein involved in transcription regulation. This compound effectively targets and reduces the levels of CDK9, thereby modulating transcriptional activity.
T77933	SJ995973	PROTACs	PROTAC
	SJ995973是一种高效的BET蛋白质降解剂(PROTAC)。
T16953	Sulfaclozine sodium Sulfachloropyrazine sodium	Antibacterial	Microbiology/Virology
	Sulfaclozine sodium is an efficacious sulphonamide derivative with antibacterial and anticoccidial effects. Sulfaclozine sodium is commonly used for the treatment of various poultry diseases.
T13833	PROTAC BRD4 Degrader-1	Epigenetic Reader Domain	Chromatin/Epigenetic
	PROTAC BRD4 Degrader-1 is an efficacious degrader of BRD4(BRD4 BD1,IC50 of 41.8 nM).
T71307	JNJ-40413269
	JNJ-40413269 is a competitive inhibitor of fatty acid amide hydrolase (FAAH), which demonstrates robust central target engagement, and shows efficacious in a rat model of neuropathic pain.
T39937	M-808
	M-808 is a potent and efficacious covalent inhibitor, targeting the interaction between Menin and MLL. It demonstrates a high binding affinity with an IC50 value of 2.6 nM.

化合物

Cat.No: T7121

Synonym: 磺胺氯吡嗪,Sulfachloropyrazine,Sulfachloropyrazine sodium,N-(5-氯-3-吡嗪基)-4-氨基苯磺酰胺

Target: Antibacterial, Antibiotic, Parasite

Cat.No: T16501

Target: p38 MAPK, Serine Protease, MAPK

CX-6258 hydrochloride

Cat.No: T6148

Synonym: CX-6258 HCl,Pim-Kinase Inhibitor X

Target: Pim

Cat.No: T15549

Target: Others

Cat.No: T28073

Synonym: MLS000051547,MLS 1547,MLS-1547

Target: Dopamine Receptor

Cat.No: T12462

Target: PI3K

Cat.No: T3692

Synonym: GNE 477

Target: PI3K, mTOR

Cat.No: T14217

Synonym: AMG-579

Target: PDE

Cat.No: T14302

Synonym: APD 371

Target: Cannabinoid Receptor

SHP099 hydrochloride

Cat.No: T3544

Target: Phosphatase, Others

Cat.No: T2338

Target: FAAH, Lipase, Autophagy

nAChR agonist 1

Cat.No: T12165

Synonym: DUN71755

Target: AChR

IL-17 modulator 4

Cat.No: T36526

Target: Interleukin

Betrixaban hydrochloride(330942-05-7(free base))

Cat.No: T4690

Synonym: PRT054021 hydrochloride,盐酸贝曲西班

Target: Factor Xa

NaV1.7 inhibitor-1

Cat.No: T12181

Target: Sodium Channel

Cat.No: T2030

Synonym: PAI-039,Tiplasinin

Target: PAI-1, Apoptosis

Cat.No: T14087

Target: TRP/TRPV Channel

Cat.No: T16996

Target: Apoptosis, EGFR

Cat.No: T11980

Target: Mdm2, E1/E2/E3 Enzyme, PROTACs

Cat.No: T3564

Synonym: SHP099 free base,SHP 099,SHP-099

Target: Phosphatase, PERK

PACAP-38 (31-38), human, mouse, rat acetate

Cat.No: TP1618L

Synonym: PACAP-38 (31-38), human, mouse, rat acetate(138764-85-9 Free base)

Target: PACAP

Cat.No: T22360

Target: TRP/TRPV Channel

Cat.No: T10964

Target: Apoptosis, Others

Balsalazide sodium hydrate

Cat.No: T4615

Synonym: 巴柳氮钠水合物,Balsalazide disodium dihydrate,巴柳氮钠,Balsalazide disodium salt dihydrate,Balsalazide disodium

Target: STAT, Interleukin

Cat.No: T16877

Target: Others

KRAS G12D inhibitor 6

Cat.No: T40281

Cat.No: T27378

Synonym: FR193879

Cat.No: T16020

Target: Others

Cat.No: T36883

PACAP-38 (31-38), human, mouse, rat

Cat.No: TP1618

Cat.No: T69886

Cat.No: T15193

Target: MEK

IL-17 modulator 4 sulfate

Cat.No: T40107

Cat.No: T15365

Target: BTK

Cat.No: T26542

Cat.No: T17175

Synonym: BCH-4556,SGX-145,SGX145,SPD-758,BCH4556,beta-L-OddC

Target: Others

Fesoterodine L-mandelate

Cat.No: T11275

Target: Others

Cat.No: T10527

Synonym: Betrixaban D6

Target: Others

IL-17 modulator 1

Cat.No: T40106

Cat.No: T15346

Target: Others

PACAP-38 (16-38), human, mouse, rat

Cat.No: TP1619

Cat.No: T71353

Cat.No: T40321

RyRs activator 5

Cat.No: T81236

PROTAC CDK9 degrader-4

Cat.No: T39996

Synonym: PROTAC CDK9 degrader-4

Cat.No: T77933

Target: PROTACs

Sulfaclozine sodium

Cat.No: T16953

Synonym: Sulfachloropyrazine sodium

Target: Antibacterial

PROTAC BRD4 Degrader-1

Cat.No: T13833

Target: Epigenetic Reader Domain

Cat.No: T71307

Cat.No: T39937

Cat. No.	Product Name	Target	Signaling Pathways
T3741	(-)-borneol L-Borneol,冰片	GABA Receptor	Membrane transporter/Ion channel; Neuroscience
	(-)-borneol (L-Borneol) 对 GABA 受体具有高效的正向调节作用，EC50 为 237 μM。
TN3724	Cryptomoscatone D2	p53	Apoptosis
	Cryptomoscatone D2 is a highly efficacious inhibitor of the G(2) checkpoint, and G(2) checkpoint inhibitors can force cells arrested in G(2) phase by DNA damage to enter mitosis.
TN3721	Cryptofolione	Antifection	Microbiology/Virology
	Z-Cryptofolione and Cryptomoscatone D2 as highly efficacious inhibitors of the G(2) checkpoint, G(2) checkpoint inhibitors can force cells arrested in G(2) phase by DNA damage to enter mitosis. Cryptofolione shows moderate cytotoxicity in both macrophages and T. cruzi amastigotes, it also displays a mild inhibitory effect on the promastigote form of Leishmania spp.

天然产物

Cat.No: T3741

Synonym: L-Borneol,冰片

Target: GABA Receptor

Cryptomoscatone D2

Cat.No: TN3724

Target: p53

Cat.No: TN3721

Target: Antifection

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