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35

抑制剂 & 化合物

2

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T11469	GSK-3484862	DNA Methyltransferase	Chromatin/Epigenetic
	GSK-3484862 是有效的 DNA 甲基转移酶 Dnmt1的非共价抑制剂。GSK-3484862 通过诱导 DNA 低甲基化起抗癌作用。GSK-3484862 介导小鼠胚胎干细胞的整体去甲基化。
T77614	DpC	Others	Others
	DPC 是一种抗肿瘤化合物，对癌细胞增殖有抑制作用，IC50为 0.007-0.096 μM。DPC 可参与多种抗癌疗法，可用于研究癌症。
T8839	ICCB280	Apoptosis; Others	Apoptosis; Others
	ICCB280 是一种 C/EBPα诱导剂，通过激活 C/EBPα 并影响其下游靶点，具有终末分化、增殖停滞和凋亡的抗白血病特性。
T3625	Bempedoic acid ETC1002,ESP-55016,ETC 1002,ETC-1002	ATP Citrate Lyase; AMPK	Chromatin/Epigenetic; Metabolism; PI3K/Akt/mTOR signaling
	Bempedoic acid (ETC1002) 是一种 ATP-柠檬酸裂解酶抑制剂，可激活AMPK。它是脂质和碳水化合物代谢的调节剂。
T9498	BAY-8400	DNA-PK	DNA Damage/DNA Repair; PI3K/Akt/mTOR signaling
	BAY-8400是一种具有口服活性、有效和选择性 DNA 依赖蛋白激酶 (DNA-PK) 抑制剂(IC50=81 nM)，与靶向α疗法联合使用显示协同疗效。BAY-8400 可用于癌症研究。
T3579	PLX8394	Raf	MAPK
	PLX8394 是一种口服活性的丝氨酸/苏氨酸蛋白激酶 B-Raf (BRAF) 蛋白抑制剂。 PLX8394 可以选择性地结合并抑制野生型和突变形式的 BRAF 的活性，然后抑制表达 BRAF 突变形式的肿瘤细胞的增殖。 PLX8394 似乎对表达多种激酶突变形式的肿瘤有效，并且可能是对其他对 BRAF V600E 突变体特异的 BRAF 抑制剂疗法耐药的肿瘤的有效治疗剂。
T27497	GSK-982 GSK 982,GSK982
	GSK-982, an opioid receptor antagonist, has activity as potential therapies for obesity.
T30236L	Axelopran sulfate
	Axelopran sulfate is used in Oral Therapies for Opioid-induced Bowel Dysfunction in Patients with Chronic Noncancer Pain.
T40166	Bexirestrant
	Bexirestrant is an orally active ER-α degrader commonly employed in the research of antiestrogen and antineoplastic therapies.
T71245	ARRY-502
	ARRY-502 is a CRTH2 antagonist. Regulation of cytokine activity is important in molecularly targeted therapies for asthma.
T71865	DSM43
	DSM43 is a dihydroorotate dehydrogenase (DHODH) inhibitor. Malaria puts at risk nearly half the world's population and causes high mortality in sub-Saharan Africa, while drug resistance threatens current therapies. The pyrimidine biosynthetic enzyme dihydroorotate dehydrogenase (DHODH) is a validated target for malaria treatmen
T70847	BMS-351
	BMS-351 is a potent and selective, nonsteroidal CYP17A1 lyase inhibitor with robust selectivity over steroidogenic CYPs 21A2 and 11B1. BMS-351 emerges as an outstanding preclinical candidate to treat CRPC and is likely to minimize the side effects of current therapies due to its exceptional selectivity. BMS-351 is potentially useful for the Treatment of Prostate Cancer.
T74337	DNA crosslinker 1 dihydrochloride
	DNA crosslinker 1 (dihydrochloride)作为有效DNA小沟结合剂,具有1.1°C的结合亲和力（ΔTm），适用于抗癌研究。
T68346	KRN383
	KRN383 also inhibited the proliferation of the ITD-positive cell lines with IC(50) values of < or =2.9 nM. A single oral administration of 80 mg/kg of KRN383 eradicated ITD-positive xenograft tumors in nude mice and prolonged the survival of SCID mice carrying ITD-positive AML cells. The effectiveness of a single oral dose of KRN383 suggests that it has the potential to be used in a wide variety of clinical regimens, including multicycle and combination therapies.
T79340	GLS1 Inhibitor-7	Glutaminase	Proteases/Proteasome
	GLS1 Inhibitor-7 (compound 4d) 作为一种GLS1 抑制剂，表现出抑制浓度50%所需浓度（IC50）为46.7 μM，潜在用途涉及抗癌、抗衰老和抗肥胖。
T82296	GluN1(359-378)
	GluN1(359-378)为抗N-甲基-D-天冬氨酸受体(NMDAR)抗体，具有穿透血脑屏障的能力。该化合物主要应用于抗NMDAR脑炎治疗的免疫系统研究。
T74879	306-N16B
	306-N16B 是一种脂质纳米颗粒，可实现 Cas9 mRNA 和 sgRNA 的系统性协同递送。306-N16B 可将 mRNA 转运至肺内皮细胞。306-N16B 可用于基因组编辑疗法的研究。
T69776	BAY-707 acetate
	BAY-707 is a substrate-competitive, highly potent and selective inhibitor of MTH1. Despite superior cellular target engagement and pharmacokinetic properties, inhibition of MTH1 with BAY-707 resulted in a clear lack of in vitro or in vivo anticancer efficacy either in mono- or in combination therapies.
T78520	CYT296	Others	Others
	CYT296是一种靶向染色质去凝集的化合物，能增强定义因子(OSKM)介导诱导多能干细胞(iPSC)的生成，并通过诱导小鼠胚胎成纤维细胞(MEFs)染色质的开放状态来促进体细胞的重编程，适用于细胞替代治疗和药物筛选的研究领域。
T38910	mGluR2 antagonist 1
	mGluR2 antagonist 1 is a potent and selective class of negative allosteric modulator targeting the metabotropic glutamate receptor 2 (mGluR2) with high oral bioavailability. It displays a remarkable affinity for mGluR2, with an IC50 value of 9 nM. Furthermore, it exhibits excellent permeability across the blood-brain barrier, making it a promising candidate for central nervous system-related studies or therapies.
T79136	DGKζ-IN-1
	DGKζ-IN-1（化合物9）是一种DGKζ的抑制剂，用于研究与免疫细胞激活相关的癌症或对抗PD-1抗体/抗PD-L1抗体耐药的癌症。
T18522	PC Mal-NHS carbonate ester	Others	Others
	PC Mal-NHS carbonate ester is a cleavable linker specifically designed for the synthesis of antibody-drug conjugates (ADCs)[1]. This chemical compound plays a crucial role in facilitating the conjugation of drugs to antibodies, enabling targeted delivery and enhanced efficacy of therapeutic agents. Its unique carbonate ester structure allows for efficient cleavage in the targeted environment, ensuring the controlled release of the drug payload. Its application in ADC synthesis highlights its imp...
T80578	Evunzekibart ATOR-1017
	Evunzekibart (ATOR-1017)是一种以Fc-γ受体为条件的4-1BB激动剂，属于IgG4亚型抗体。该化合物既可以作为单药疗法，也可与抗PD1治疗相结合，以发挥其抗肿瘤效果。
T71206	Tiagabine-d6 hydrochloride
	Tiagabine-d6 is intended for use as an internal standard for the quantification of tiagabine by GC- or LC-MS. Tiagabine is an inhibitor of GABA transporter 1. It inhibits seizures induced by DMCM in mice. Tiagabine reduces allodynia in a rodent model of neuropathic pain when used at a dose of 72.8 µmol/kg, and it acts synergistically with gabapentin to delay pain responses in mice in the hot plate test. Formulations containing tiagabine have been used as adjunctive therapies in the treatment of ...
T70352	PH11
	PH11 is a novel Focal Adhesion Kinase (FAK) inhibitor. PH11 restores TRAIL apoptotic pathway in PANC-1 cells through down-regulation of c-FLIP via inhibition of FAK and the phosphatidylinositol-3 kinase (PI3K)/AKT pathways. Tumor necrosis factor (TNF)-related apoptosis-inducing ligand (TRAIL) emerges as one of the most-promising experimental cancer therapeutic drugs and is currently being tested in clinical trials. However, both intrinsic and acquired resistance of human cancer cells to TRAIL...
T79051	PCSK9-IN-15
	PCSK9-IN-15（化合物5）是一种高效PCSK9抑制剂，亲和力强（KD<200 nM）。该化合物与胆固醇代谢相关，可调控低密度脂蛋白胆固醇（LDL-C）水平，适用于研究降低胆固醇及血脂异常。
T71467	Nemorubicin HCL
	Nemorubicin HCL is the salt form of Nemorubicin, also known as PNU152243A, a doxorubicin derivative that differs significantly from its parent drug in terms of spectrum of antitumor activity, metabolism and toxicity profile. The drug is active on tumors resistant to alkylating agents, topoisomerase II inhibitors and platinum derivatives. It works primarily through topoisomerase I inhibition. Of note, Nemorubicin is active in cells with upregulation of the nucleotide excision repair (NER) pathway...
T71578	Endoxifen mesylate
	Endoxifen, also known as N-desmethyl-4-hydroxytamoxifen, is a chemical that is under development for estrogen receptor-positive breast cancer. It is also being evaluated as an antipsychotic for treatment of mania and other psychotic disorders. Endoxifen is a nonsteroidal selective estrogen receptor modulator (SERM) of the triphenylethylene group. It is an active metabolite of tamoxifen and has been found to be effective in patients that have failed previous hormonal therapies (tamoxifen, aromat...
T78528	ERX-41	Others	Others
	ERX-41是一种口服活性的立体特异性小分子，靶向溶酶体酸性脂肪酶A (LIPA)。该化合物通过诱导内质网(ER)应激从而导致细胞死亡，这一作用表明ERX-41功能独立于LIPA，但依赖于其在内质网的定位。ERX-41主要用于实体瘤靶向研究。
T30807	CG0009 CG-0009,CG 0009
	CG0009 is a potent and highly selective glycogen synthase kinase 3 (GSK3) inhibitor that inhibitions proliferation, induces apoptosis, and activates the p53-Bax pathway in breast cancer cells through cyclin D1 depletion. CG0009 inhibit breast cancer cell
T72259	3-Chlorogentisyl alcohol
	3-Chlorogentisyl alcohol 是一种有效的 E. coliβ-葡萄糖醛酸酶β-glucuronidase 抑制剂，IC50值为 0.74 µM，Ki 值为 0.58 µM。3-Chlorogentisyl alcohol 显示出抗增殖活性。3-Chlorogentisyl alcohol 具有抗癌和抗炎治疗研究的潜力。
T31828	AZD4694 Flutafuranol,AZD 4694,NAV-4694,AZD-4694,NAV 4694,NAV4694
	Flutafuranol, also known as AZD 4694 and NAV4694, is a bio-active chemical. AZD4694 shows high affinity for beta-amyloid fibrils in vitro (K(d) = 2.3 +/- 0.3 nM). The fluorine-18 labeled AZD4694 may have potential for PET-visualization of cerebral beta-am
T69831	RPR-200765A Mesylayte
	RPR-200765A is a potent and selective inhibitor of p38 MAP kinase (IC50 = 50 nM). It inhibits LPS-stimulated TNFalpha release both in vitro, from human monocytes (EC50 = 110 nM), and in vivo in Balb/c mice (ED50 = 6 mg/kg). At oral doses between 10 and 30 mg/kg/day it reduces the incidence and progression in the rat streptococcal cell wall (SCW) arthritis model when administered in either prophylactic or therapeutic dosing regimens. The compound, which is a mesylate salt and exists as a stable m...
T37736	N-cis-hexadec-9Z-enoyl-L-Homoserine lactone N-(2-oxotetrahydrofuran-3S-yl) Palmitoleyl Amide,N-cis-hexadec-9Z-enoyl-L-Homoserine lactone
	Quorum sensing is a regulatory process used by bacteria for controlling gene expression in response to increasing cell density.[1] This regulatory process manifests itself with a variety of phenotypes including biofilm formation and virulence factor production.[2] Coordinated gene expression is achieved by the production, release, and detection of small diffusible signal molecules called autoinducers. The N-acylated homoserine lactones (AHLs) comprise one such class of autoinducers, each of whic...
T37741	N-hexadecanoyl-L-Homoserine lactone C16-HSL,N-palmitoyl-L-Homoserine,N-hexadecanoyl-L-Homoserine lactone
	Quorum sensing is a regulatory system used by bacteria for controlling gene expression in response to increasing cell density.[1] This regulatory process manifests itself with a variety of phenotypes including biofilm formation and virulence factor production.[2] Coordinated gene expression is achieved by the production, release, and detection of small diffusible signal molecules called autoinducers. The N-acylated homoserine lactones (AHLs) comprise one such class of autoinducers, each of which...

化合物

Cat.No: T11469

Target: DNA Methyltransferase

Cat.No: T77614

Target: Others

Cat.No: T8839

Target: Apoptosis, Others

Cat.No: T3625

Synonym: ETC1002,ESP-55016,ETC 1002,ETC-1002

Target: ATP Citrate Lyase, AMPK

Cat.No: T9498

Target: DNA-PK

Cat.No: T3579

Target: Raf

Cat.No: T27497

Synonym: GSK 982,GSK982

Axelopran sulfate

Cat.No: T30236L

Cat.No: T40166

Cat.No: T71245

Cat.No: T71865

Cat.No: T70847

DNA crosslinker 1 dihydrochloride

Cat.No: T74337

Cat.No: T68346

GLS1 Inhibitor-7

Cat.No: T79340

Target: Glutaminase

Cat.No: T82296

Cat.No: T74879

BAY-707 acetate

Cat.No: T69776

Cat.No: T78520

Target: Others

mGluR2 antagonist 1

Cat.No: T38910

Cat.No: T79136

PC Mal-NHS carbonate ester

Cat.No: T18522

Target: Others

Cat.No: T80578

Synonym: ATOR-1017

Tiagabine-d6 hydrochloride

Cat.No: T71206

Cat.No: T70352

Cat.No: T79051

Nemorubicin HCL

Cat.No: T71467

Endoxifen mesylate

Cat.No: T71578

Cat.No: T78528

Target: Others

Cat.No: T30807

Synonym: CG-0009,CG 0009

3-Chlorogentisyl alcohol

Cat.No: T72259

Cat.No: T31828

Synonym: Flutafuranol,AZD 4694,NAV-4694,AZD-4694,NAV 4694,NAV4694

RPR-200765A Mesylayte

Cat.No: T69831

N-cis-hexadec-9Z-enoyl-L-Homoserine lactone

Cat.No: T37736

Synonym: N-(2-oxotetrahydrofuran-3S-yl) Palmitoleyl Amide,N-cis-hexadec-9Z-enoyl-L-Homoserine lactone

N-hexadecanoyl-L-Homoserine lactone

Cat.No: T37741

Synonym: C16-HSL,N-palmitoyl-L-Homoserine,N-hexadecanoyl-L-Homoserine lactone

Cat. No.	Product Name	Target	Signaling Pathways
T82046	Irisquinone
	Irisquinone，一种具有抗癌活性的天然产物，同时作为癌症放射增敏剂。该化合物通过降低GSH水平并抑制DNA单链断裂修复，展现其药理作用。
T37291	Lyso-Globotriaosylceramide (d18:1) Lyso-Globotriaosylceramide (d18:1)
	Lyso-globotriaosylceramide is a form of globotriaosylceramide that is lacking the fatty acyl group. It binds to Shiga toxin 1 (Stx1) in the presence of cholesterol and phosphatidylcholine but does not bind Stx2. It also reduces viability and aggregation of human neutrophils induced by phorbol 12-myristate 13-acetate when used at concentrations of 50 and 1 μM, respectively. Lyso-globotriaosylceramide accumulates in the brain, heart, kidney, liver, lung, and spleen in a mouse model of Fabry diseas...

天然产物

Cat.No: T82046

Lyso-Globotriaosylceramide (d18:1)

Cat.No: T37291

Synonym: Lyso-Globotriaosylceramide (d18:1)

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