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49

抑制剂 & 化合物

4

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T12367	Parsaclisib INCB050465	PI3K	PI3K/Akt/mTOR signaling
	Parsaclisib (INCB050465) 是有效的、选择性的、具有口服活性的PI3Kδ抑制剂，其 IC50=1 nM。它相对于其他 PI3K I 类同工型的选择性约为 20000 倍。它可用于复发或难治性 B 细胞恶性肿瘤的研究。
T9519	Eliapixant BAY 1817080	P2X Receptor	Membrane transporter/Ion channel; Neuroscience
	Eliapixant (BAY 1817080) 是一种选择性的P2X3受体拮抗剂，IC50值为 8 nM，可用于难治性慢性咳嗽的研究。
T20759	XRP44X XRP-44-X,XRP 44X,XRP-44X,XRP 44 X	Ras	GPCR/G Protein; MAPK
	XRP44X (XRP 44X) 是Ras 诱导的转录激活的抑制剂，IC50为 10 nM，通过 FGF-2 抑制 Ras-Erk-1/2 通路激活。它抑制Elk3。它还对微管有影响。
T28297	Parsaclisib hydrochloride Parsaclisib HCl,INCB-50465,INCB 050465,INCB-050465,INCB050465 HCl,INCB 50465,INCB50465 HCl	PI3K	PI3K/Akt/mTOR signaling
	Parsaclisib hydrochloride (INCB050465 HCl) 是一种选择性的、有效的，具有口服活性的 PI3Kδ抑制剂，IC50=1 nM。它相对于其他 PI3K I 类同工型的选择性约为 20000 倍。它可用于复发或难治性 B 细胞恶性肿瘤的研究。
T76692	Mosunetuzumab BTCT-4465A	Others	Others
	Mosunetuzumab (BTCT-4465A) 是一种基于免疫球蛋白 G1 且靶向 CD20 (B 细胞) 和 CD3 (T 细胞) 的人源化抗体。Mosunetuzumab 重定向 T 细胞以接合和消除恶性 B 细胞，可用于研究复发或难治性 (R/R) B 细胞非霍奇金淋巴瘤 (B-NHL)和难治性滤泡性淋巴瘤。
T76718	Brentuximab	TNF	Apoptosis
	Brentuximab 是靶向 CD30 的嵌合抗体，是 Brentuximab vedotin 的裸抗。Brentuximab 具有抗肿瘤活性，可用于研究复发或难治性霍奇金淋巴瘤。
T21444	Diphenylcyclopropenone DPCP,Diphencyprone,二苯基环丙烯酮	Others	Others
	Diphenylcyclopropenone (DPCP) 是局部免疫调节剂，可用于研究斑秃。
T3078	SGI-1776 SGI-1776 free base,Pim-Kinase Inhibitor IX	Apoptosis; FLT; Pim; Autophagy	Angiogenesis; Apoptosis; Autophagy; Chromatin/Epigenetic; JAK/STAT signaling; Tyrosine Kinase/Adaptors
	SGI-1776 (Pim-Kinase Inhibitor IX) 是一种Pim 抑制剂，抑制 Pim-1、Pim-2 和 Pim-3 的活性，IC50值分别为 7 nM、363 nM 和 69 nM。
T76927	Bersanlimab BI-505	Integrin	Cytoskeletal Signaling
	Bersanlimab (BI-505) 是一种全人源靶向细胞间粘附分子-1 (ICAM-1）的单克隆抗体。Bersanlimab 具有抗癌作用，可用于研究复发/难治性多发性骨髓瘤。
T77750	Rosmantuzumab OMP-131R10	Others	Others
	Rosmantuzumab (OMP-131R10) 是一种人源化抗 R-spondin 3 (RSPO3)单克隆抗体。Rosmantuzumab 具有潜在的抗肿瘤活性，可用于研究晚期复发难治性实体瘤。
T71973	Gilteritinib hemifumarate ASP2215 hemifumarate	FLT; TAM Receptor	Angiogenesis; Tyrosine Kinase/Adaptors
	Gilteritinib hemifumarate (ASP2215 hemifumarate) 是一种高效的 ATP 竞争性 FLT3（IC50 ： 0.29 nM）和 AXL（IC50： 0.73 nM）双重抑制剂，可用于治疗复发或难治性 FLT3 突变的 AML。
T76685	Glofitamab RO7082859,RG 6026,CD20-TCB	Others	Others
	Glofitamab (RO7082859) 是一种新型针对 CD20 结合 T 细胞的二价抗体。Glofitamab 通过与恶性细胞上的 CD20 结合促使 T 细胞增殖活化和肿瘤细胞杀伤。Glofitamab 可用于缓解复发或难治性 B 细胞淋巴瘤。
T77909	Mirzotamab
	Mirzotamab clezutoclax（ABBV-155）是一种IgG1κ型靶向CD276/B7-H3的抗体偶联物（ADC），通过与BCL抑制剂Clezutoclax结合而构成。该化合物用于参与针对复发/难治性实体瘤的紫杉烷相关研究。
T12660L	BAY1238097	Epigenetic Reader Domain	Chromatin/Epigenetic
	BAY1238097 是一种具有有效性和选择性的溴结构域和末端外基序(BET)抑制剂，具有抗癌活性，在AML (急性髓性白血病) 和MM (多发性骨髓瘤) 模型中表现出较强的抗增殖活性。BAY1238097 可用于研究晚期难治性恶性肿瘤。
T9969	EZM0414	Histone Methyltransferase	Chromatin/Epigenetic
	EZM0414 是一种有效、选择性、口服生物利用度高的SETD2抑制剂，在 SETD2 生化分析中，IC50值为18 nM；在细胞分析中，IC50值为34 nM。EZM0414可用于复发或难治性多发性骨髓瘤和弥漫性大 B 细胞淋巴瘤的研究。
T6541	Ibutilide Fumarate Corvert Fumarate,U70226E,富马酸伊布利特	Calcium Channel; Sodium Channel	Membrane transporter/Ion channel; Metabolism
	Ibutilide Fumarate (U70226E) 是一种 III 类抗心律失常药物，可作用于急性心梗阻塞。
T6476	Dofetilide UK 68789,UK-68798,Tikosyn,多非利特	Potassium Channel	Membrane transporter/Ion channel
	Dofetilide (UK 68789) 是一种具有口服活性、有效的且特异性的IKr 阻滞剂，作为 III 类抗心律失常药物。Dofetilide 可用于心血管疾病研究。
T15257	Etripamil MSP-2017,(-)-MSP-2017	Calcium Channel	Membrane transporter/Ion channel; Metabolism
	Etripamil (MSP-2017) 是一种短效L 型钙通道拮抗剂，可用于治疗阵发性室上性心动过速的研究。它通过抑制房室结细胞中钙慢通道的钙离子流入，显示房室结传导并延长房室结不应期
T0866	Propafenone Rythmol,普罗帕酮,Propafenonum	Potassium Channel; MRP; Sodium Channel	Immunology/Inflammation; Membrane transporter/Ion channel
	Propafenone (Propafenonum) 是钠通道阻滞剂，它对 β 受体具有高亲和力 (IC50=32 nM)。它能够阻断瞬时外向钾电流 (Ito) (IC50: 4.9 nM) 和持续延迟整流器K+电流 (Isus) (IC50: 8.6 nM) ，具有抗心律失常的作用。它能够诱导线粒体功能障碍及诱导细胞凋亡，从而抑制食管癌增殖。
T25593	Labetuzumab govitecan IMMU-130,Labetuzumab-SN38,hMN14-SN38,IMMU130,IMMU 130	Others	Others
	Labetuzumab govitecan is an anti-CEACAM5/SN-38 antibody-drug conjugate for therapy of refractory or relapsing metastatic colorectal cancer.
T17215	Valnoctamide Valmethamide	GABA Receptor	Membrane transporter/Ion channel; Neuroscience
	Valnoctamide inhibits benzodiazepine-refractory status epilepticus. Valnoctamide acts directly on GABAA receptors.
T26092	Risotilide
	Risotilide is a voltage-dependent potassium channel inhibitor. It can prolong cardiac action potentials and refractory periods.
T13672	EC0489	Others	Others
	EC0489, Small molecule-drug conjugate (SMDC) ,a conjugate of folic acid and desacetyl vinblastine hydrazide, is a high-affinity ligand for the folate receptor (FR). Refractory or metastatic Tumor.
T13279	Valemetostat tosylate DS-3201 tosylate	Histone Methyltransferase	Chromatin/Epigenetic
	Valemetostat tosylate is a dual inhibitor of EZH1/2 and used in the research of relapsed/refractory peripheral T-cell lymphoma.
T37821	AP 14145 hydrochloride
	KCa2 (small conductance Ca2+-activated potassium) channel negative allosteric modulator (IC50 = 1.1 μM). Increases the EC50 of Ca2+ on KCa2.3 channels by ~3-fold. Prolongs atrial effective refractory period (AERP) in rats. Reduces atrial fibrillation (AF) duration and prolongs atrial refractoriness without affecting ventricular refractory period in an animal AF model. Diness et al (2017) Termination of vernakalant-resistant atrial fibrillation by inhibition of small-conductance Ca2+-activated K+...
T16406	Orvepitant maleate GW823296 maleate	Neurokinin receptor	GPCR/G Protein; Neuroscience
	Orvepitant maleate is an effective, selective, and well-tolerated neurokinin-1 receptor (NK-1) antagonist (pKi: 10.2 for human neurokinin-1 receptor). Orvepitant maleate has the potential for depressive disorder and chronic refractory cough (CRC) treatmen
T70759	CUDC-907 mesylate
	CUDC-907 mesylate is a small molecule inhibitor of histone deacetylase and PI3 kinase developed by Curis. It is investigated in clinical trials for the treatment of relapsed or refractory lymphomas, thyroid cancer, multiple myeloma, breast cancer and other malignancies.
T76922	Begelomab
	Begelomab (SAND-26) 是一种针对 DPP-4/CD26的鼠IgG2b 单克隆抗体。 Begelomab 可用于严重难治性特发性炎症性肌病的研究。
T21427	Mexiletine Mexitil,Mexiletene,KO-1173,KO1173,KO 1173
	Mexiletine is a non-selective voltage-gated sodium channel blocker. It is a medicine in the class of IB anti-arrhythmic. Mexiletine may also be used in patients experiencing refractory pain and is effective to treat muscle stiffness resulting from myotonic dystrophy or non-dystrophic myotonias.
T80863	Visugromab CTL-002	PD-1/PD-L1	Apoptosis; Cell Cycle/Checkpoint; Immunology/Inflammation
	Visugromab，作为针对GDF-15的中和IgG4单抗，展现出针对PD-1/PD-L1复发/难治性转移性实体瘤的显著疗效。
T80613	Linvoseltamab REGN5458
	Linvoseltamab为双特异性抗体，针对BCMA(TNFRSF17)与CD3epsilon。该化合物于复发/难治性多发性骨髓瘤(RRMM)模型中展示了良好的安全性和效力。
T80270	Invopressin OCE-205	Vasopressin Receptor	GPCR/G Protein
	Invopressin (Compound 42)，一种vasopressin V1A 受体部分激动剂（EC50: 1.0 nM），主要应用于肝硬化相关症状如细菌性腹膜炎、HRS2 及难治性腹水的研究。
T82927	Azintuxizumab
	Azintuxizumab是针对B细胞成熟抗原(BCMA)的IgG4型双特异性单克隆抗体，显示出在治疗复发/难治性多发性骨髓瘤(RRMM)中的应用潜力。
T62524	Panobinostat lactate
	Panobinostat lactate 是一种有效的、口服具有活力的、非选择性 HDAC 抑制剂，具有抗肿瘤作用。Panobinostat lactate 诱导细胞凋亡 (apoptosis) 和自噬 (autophagy)。Panobinostat lactate 能够有效干扰 HIV 潜伏期。Panobinostat lactate 能够用于研究难治性或复发性多发性骨髓瘤。
T80981	Tisagenlecleucel CTL019
	Tisagenlecleucel (CTL019) 是一种自体抗CD19嵌合抗原受体 (CAR) T 细胞治疗，专门针对并消除表达CD19的 B 细胞。该疗法主要用于研究治疗难治性侵袭性弥漫性大 B 细胞淋巴瘤。
T81704	Naptumomab
	Naptumomab是一种针对肿瘤细胞的超级抗原(TTS)融合蛋白。它能激活免疫系统，使之识别并消灭肿瘤细胞。该化合物主要应用于肾细胞癌等难治性实体肿瘤的研究领域。
T70896	PF05020182
	PF05020182 is novel potent and selective Kv7.2/4 potassium channel opener. PF-05020182 (2) significantly inhibits convulsions in the MES assay at doses tested, consistent with in vitro activity measure. The physiochemical properties, in vitro and in vivo activities of PF-05020182 support further development as an adjunctive treatment of refractory epilepsy. Facilitating activation, or delaying inactivation, of the native Kv7 channel reduces neuronal excitability, which may be beneficial in cont...
T34686	Sonoflora 1 SF 1,SF-1,Sonoflora1,Sonoflora-1,SF1
	Sonoflora 1, also known as SF1, a PDT photosensitivizer. Chemically, SF1 is an analog of chlorophyll in that its macrocycle backbone is porphyrin-based and the center of the porphyrin ring consists of a metal ion. Preclinical studies showed that SF1 had v
T39963	AP14145 hydrochloride
	AP14145 hydrochloride is a potent negative allosteric modulator of K Ca 2 (SK) channels, specifically targeting K Ca 2.2 (SK2) and K Ca 2.3 (SK3) channels with an IC 50 of 1.1 μM. Inhibition of AP14145 hydrochloride is highly influenced by S508 and A533 amino acids present in the channel. This compound effectively extends the atrial effective refractory period (AERP) in rats and exhibits antiarrhythmic properties in a Vernakalant-resistant porcine model of atrial fibrillation (AF).
T76872	Neihulizumab
	Neihulizumab (ALTB-168) 是一种免疫检查点激动性抗体，可与人 CD162 (PSGL-1)结合，导致活化的 T 细胞下调。Neihulizumab 可用于类固醇难治性急性移植物抗宿主病 (SR-aGVHD)、银屑病、银屑病关节炎和溃疡性结肠炎的研究。
T76729	Lucatumumab
	Lucatumumab (HCD122) 是一种全人抗 CD40拮抗剂单克隆抗体，可阻断 CD40/ CD40L 介导的信号通路。Lucatumumab 可有效介导抗体依赖性细胞介导的细胞毒性 (ADCC) 和肿瘤细胞清除，可用于顽固性淋巴瘤、慢性淋巴细胞白血病 (CLL) 和多发性骨髓瘤研究。
T77084	Mezagitamab
	Mezagitamab (TAK-079) 是一种 IgG1λ 类型的抗CD38单克隆抗体。其通过促进抗体和补体依赖性的细胞毒性，来耗尽表达CD38的肿瘤细胞，显示出在复发/难治性多发性骨髓瘤 (RRMM) 及原发性血小板减少性紫癜 (ITP) 等疾病中的治疗潜力。
T69931	MFH290
	MFH290 is a novel cysteine (Cys)-directed covalent inhibitor of CDK12/13. MFH290 forms a covalent bond with Cys-1039 of CDK12, exhibits excellent kinome selectivity, inhibits the phosphorylation of serine-2 in the C-terminal domain (CTD) of RNA-polymerase II (Pol II), and reduces the expression of key DNA damage repair genes. Importantly, these effects were demonstrated to be CDK12-dependent as mutation of Cys-1039 rendered the kinase refractory to MFH290 and restored Pol II CTD phosphorylation ...
T81490	PHI-101
	PHI-101是口服FLT3抑制剂，在克服多耐药突变方面表现出高效。该化合物对FLT3的ITD或TKD单突变体表现出显著抑制作用，同时也能抑制包括双重（ITD/D835Y或ITD/F691L）和三重（ITD/D835Y/F691L）耐药突变。PHI-101在治疗复发或难治性急性髓系白血病（AML）的研究中显示出应用潜力。
T69492	Ozarelix
	Ozarelix is a fourth generation GnRH antagonist, induces apoptosis in hormone refractory androgen receptor negative prostate cancer cells modulating expression and activity of death receptors. Mechanistically, LHRH antagonists exert rapid inhibition of luteinizing hormone and follicle stimulating hormone with an accompanying rapid decrease in sex hormones and would therefore be expected to be effective in a variety of hormonally dependent disease states including ovarian cancer, prostate cancer,...
T69978	Brostallicin HCl
	Brostallicin is a synthetic, alpha-bromoacrylic, second-generation minor groove binder (MGB), related to distamycin A, with potential antineoplastic activity. Brostallicin binds to DNA minor groove DNA, after having formed a highly reactive glutathione (GSH)-brostallicin complex in the presence of the enzyme glutathione S-transferase (GST), which is overexpressed in cancer cells; DNA replication and cell division are inhibited, resulting in tumor cell death. Compared to typical MGBs, this agent ...
T71228	Adaprolol maleate
	Adaprolol maleate is a beta-blocker and opthalmic which may be used in the treatment of Glaucoma or other ailments of the eye. Adaprolol has marked electrophysiologic effects. Its major action was on sinus node; it prolonged the basic sinus cycle length and had significant effect on intrinsic automaticity as reflected by the prolonged corrected sinus node recovery time and sinuatrial conduction time. There was, also, direct effect on atrial function and AV nodal function. Adaprolol prolonged the...
T68581	AP23464
	AP23464 is a potent adenosine 5'-triphosphate (ATP)-based inhibitor of Src and Abl kinases, displays antiproliferative activity against a human CML cell line and Bcr-Abl-transduced Ba/F3 cells (IC(50) = 14 nM. AP23464 ablates Bcr-Abl tyrosine phosphorylation, blocks cell cycle progression, and promotes apoptosis of Bcr-Abl-expressing cells. Biochemical assays with purified glutathione S transferase (GST)-Abl kinase domain confirmed that AP23464 directly inhibits Abl activity. Importantly, the lo...
T35874	CC260
	CC260 is a selective PI5P4Kα and PI5P4Kβ inhibitor with Kis of 40 nM and 30 nM, respectively. CC260 does not inhibit or weakly inhibits other protein kinases, such as Plk1 and RSK2. CC260 can be used for cell energy metabolism, diabetes and cancer research[1]. In cultured C2C12 myotubes, CC260 (20 μM) enhances Insulin-induced Akt phosphorylation at both Thr-308 and Ser-473 but suppresses S6K phosphorylation (Thr-389) by mTORC1[1]. CC260 (2.5 μM, 5 μM, 10 μM, 20 μM) significantly increases phosph...

化合物

Cat.No: T12367

Synonym: INCB050465

Target: PI3K

Cat.No: T9519

Synonym: BAY 1817080

Target: P2X Receptor

Cat.No: T20759

Synonym: XRP-44-X,XRP 44X,XRP-44X,XRP 44 X

Target: Ras

Parsaclisib hydrochloride

Cat.No: T28297

Synonym: Parsaclisib HCl,INCB-50465,INCB 050465,INCB-050465,INCB050465 HCl,INCB 50465,INCB50465 HCl

Target: PI3K

Cat.No: T76692

Synonym: BTCT-4465A

Target: Others

Cat.No: T76718

Target: TNF

Diphenylcyclopropenone

Cat.No: T21444

Synonym: DPCP,Diphencyprone,二苯基环丙烯酮

Target: Others

Cat.No: T3078

Synonym: SGI-1776 free base,Pim-Kinase Inhibitor IX

Target: Apoptosis, FLT, Pim, Autophagy

Cat.No: T76927

Synonym: BI-505

Target: Integrin

Cat.No: T77750

Synonym: OMP-131R10

Target: Others

Gilteritinib hemifumarate

Cat.No: T71973

Synonym: ASP2215 hemifumarate

Target: FLT, TAM Receptor

Cat.No: T76685

Synonym: RO7082859,RG 6026,CD20-TCB

Target: Others

Cat.No: T77909

Cat.No: T12660L

Target: Epigenetic Reader Domain

Cat.No: T9969

Target: Histone Methyltransferase

Ibutilide Fumarate

Cat.No: T6541

Synonym: Corvert Fumarate,U70226E,富马酸伊布利特

Target: Calcium Channel, Sodium Channel

Cat.No: T6476

Synonym: UK 68789,UK-68798,Tikosyn,多非利特

Target: Potassium Channel

Cat.No: T15257

Synonym: MSP-2017,(-)-MSP-2017

Target: Calcium Channel

Cat.No: T0866

Synonym: Rythmol,普罗帕酮,Propafenonum

Target: Potassium Channel, MRP, Sodium Channel

Labetuzumab govitecan

Cat.No: T25593

Synonym: IMMU-130,Labetuzumab-SN38,hMN14-SN38,IMMU130,IMMU 130

Target: Others

Cat.No: T17215

Synonym: Valmethamide

Target: GABA Receptor

Cat.No: T26092

Cat.No: T13672

Target: Others

Valemetostat tosylate

Cat.No: T13279

Synonym: DS-3201 tosylate

Target: Histone Methyltransferase

AP 14145 hydrochloride

Cat.No: T37821

Orvepitant maleate

Cat.No: T16406

Synonym: GW823296 maleate

Target: Neurokinin receptor

CUDC-907 mesylate

Cat.No: T70759

Cat.No: T76922

Cat.No: T21427

Synonym: Mexitil,Mexiletene,KO-1173,KO1173,KO 1173

Cat.No: T80863

Synonym: CTL-002

Target: PD-1/PD-L1

Cat.No: T80613

Synonym: REGN5458

Cat.No: T80270

Synonym: OCE-205

Target: Vasopressin Receptor

Cat.No: T82927

Panobinostat lactate

Cat.No: T62524

Tisagenlecleucel

Cat.No: T80981

Synonym: CTL019

Cat.No: T81704

Cat.No: T70896

Cat.No: T34686

Synonym: SF 1,SF-1,Sonoflora1,Sonoflora-1,SF1

AP14145 hydrochloride

Cat.No: T39963

Cat.No: T76872

Cat.No: T76729

Cat.No: T77084

Cat.No: T69931

Cat.No: T81490

Cat.No: T69492

Brostallicin HCl

Cat.No: T69978

Adaprolol maleate

Cat.No: T71228

Cat.No: T68581

Cat.No: T35874

Cat. No.	Product Name	Target	Signaling Pathways
T4869	D-Allose 阿洛糖,β-D-Allopyranose,D-(+)-ALLOSE	Others; Endogenous Metabolite	Metabolism; Others
	D-Allose (β-D-Allopyranose) 是内源性代谢产物的一种。
T6S0735	Flavokawain B 黄卡瓦胡椒素B,Flavokavain B,Flavokawin B,2'-Hydroxy-4',6'-Dimethoxychalcone	Apoptosis; Others	Apoptosis; Others
	Flavokawain B (Flavokavain B) 是从卡瓦醉椒的根提取物中，分离出的查尔酮。它是一种凋亡诱导剂，可抑制各种癌细胞株生长。它以极低的无毒浓度抑制人脑内皮细胞的迁移和血管形成，具有抗血管生成活性。
T13764	Lycopodine	Lipoxygenase; Caspase	Apoptosis; Metabolism; Proteases/Proteasome
	Lycopodine, a bioactive compound derived from Lycopodium clavatum spores, effectively inhibits the proliferation of HeLa cells through the induction of apoptosis. This process is mediated by caspase-3 activation. In refractory prostate cancer cells, Lycopodine triggers apoptosis by modulating 5-lipoxygenase and depolarizing the mitochondrial membrane potential, without altering p53 activity.
TN3404	Altholactone	BCL; p38 MAPK; ROS; Akt; Caspase; Antifection; p53	Apoptosis; Cytoskeletal Signaling; Immunology/Inflammation; MAPK; Microbiology/Virology; PI3K/Akt/mTOR signaling; Proteases/Proteasome
	Altholactone may be a potential antimicrobial agent, particularly in ciprofloxacin-refractory S. aureus and E. faecalis infections. It can inhibit the growth of various types of cancer cells through inducing apoptosis via oxidative stress, including bladd

天然产物

Cat.No: T4869

Synonym: 阿洛糖,β-D-Allopyranose,D-(+)-ALLOSE

Target: Others, Endogenous Metabolite

Cat.No: T6S0735

Synonym: 黄卡瓦胡椒素B,Flavokavain B,Flavokawin B,2'-Hydroxy-4',6'-Dimethoxychalcone

Target: Apoptosis, Others

Cat.No: T13764

Target: Lipoxygenase, Caspase

Cat.No: TN3404

Target: BCL, p38 MAPK, ROS, Akt, Caspase, Antifection, p53

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