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64

抑制剂 & 化合物

5

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T21302	UNC569 UNC 569	TAM Receptor	Tyrosine Kinase/Adaptors
	UNC569 (UNC 569) 是一种ATP 竞争性的、可逆、具有口服活性的Mer 激酶抑制剂，其IC50=2.9 nM，Ki=4.3 nM。它还抑制Axl 和Tyro3，IC50分别为 37 nM 和 48 nM。它可用于研究急性淋巴细胞白血病和非典型畸胎瘤/横纹肌瘤。
T4230	PF-3758309 hydrochloride PF-03758309 hydrochloride	Apoptosis; PAK	Apoptosis; Cytoskeletal Signaling
	PF-3758309 hydrochloride (PF-03758309 hydrochloride) 是一种口服的、可逆的 ATP 竞争性PAK4抑制剂，Kd 为 2.7 nM，Ki 为 18.7 nM。它抑制锚定独立生长、诱导凋亡、细胞骨架重塑和抑制增殖，具有 PAK4 抑制剂的预期细胞功能。
T6626	PF-3758309 PF-309,PF-03758309,PF 3758309	Apoptosis; PAK	Apoptosis; Cytoskeletal Signaling
	PF-3758309 (PF-03758309) 是一种可口服的、可逆的 ATP 竞争性 PAK4抑制剂。它是一种 PAK4 抑制剂，可抑制锚定独立生长、诱导凋亡、细胞骨架重塑和抑制增殖。
T7326	6H05 (TFA) 6H05 TFA,6H05 trifluoroacetate	Ras	GPCR/G Protein; MAPK
	6H05 TFA (6H05 trifluoroacetate) 是一种选择性变构致癌突变体 K-Ras(G12C) 抑制剂。
T37422L	Ras Inhibitory Peptide acetate Ras Inhibitory Peptide acetate(159088-48-9 Free base)	Ras	GPCR/G Protein; MAPK
	Ras Inhibitory Peptide acetate 是一种参与 Ras 依赖性信号通路的肽，Ras 在致癌受体引发的人类癌症中起重要作用。
T6556	K-Ras(G12C) inhibitor 9	Raf	MAPK
	K-Ras(G12C) inhibitor 9 是致癌 K-Ras(G12C) 的变构抑制剂。
T6555	K-Ras(G12C) inhibitor 12	Apoptosis; Raf; Ras	Apoptosis; GPCR/G Protein; MAPK
	K-Ras(G12C) inhibitor 12是一种K-Ras(G12C)抑制剂，作用于H1792细胞，EC50为0.32 μM。
T9589	SI-113	SGK	Metabolism
	SI-113 是一种有效的选择性 SGK1 抑制剂，SGK1 是一种丝氨酸/苏氨酸蛋白激酶，可调节多种致癌信号级联反应。
T2275	YK-4-279 4,7-二氯-1,3-二氢-3-羟基-3-[2-(4-甲氧基苯基)-2-氧代乙基]-2H-吲哚-2-酮	Apoptosis; DNA/RNA Synthesis	Apoptosis; Cell Cycle/Checkpoint; DNA Damage/DNA Repair
	YK 4-279是一种RNA 解旋酶A 与致癌转录因子EWS-FLI1结合抑制剂，能抑制ESFT 细胞增长，诱导凋亡。
T1744	BIX02188	Apoptosis; MEK	Apoptosis; MAPK
	BIX02188 是一种具有选择性和有效性的 MEK5 抑制剂，抑制 MEK5 诱导表达致癌突变体FLT3-ITD的细胞凋亡。
T69980	XMU-MP-2	BTK; Protease	Angiogenesis; Proteases/Proteasome; Tyrosine Kinase/Adaptors
	XMU-MP-2 是一种有效和选择性的蛋白酶抑制剂，具有抗癌活性，在小鼠异种移植模型中抑制致癌 BRK 驱动的肿瘤的生长。
T60031	NRX-1933
	NRX-1933 是一种分子胶，可增强致癌转录因子 β-Catenin 与其同源 E3 连接酶 SCFβ-TrCP 之间的相互作用。
T6284	Onalespib AT13387,Onalespib (AT13387)	HSP	Cytoskeletal Signaling; Metabolism
	Onalespib (AT13387) 是一种合成的、口服生物可利用的热休克蛋白 90 (Hsp90) 小分子抑制剂，Kd 值为 0.71 nM。具有潜在的抗肿瘤活性。它选择性地与 Hsp90 结合，从而抑制其伴侣功能并促进参与肿瘤细胞增殖和存活的致癌信号蛋白的降解。
T8402	Regorafenib Hydrochloride 瑞戈非尼盐酸盐,BAY73-4506 hydrochloride	Raf; VEGFR; c-RET; PDGFR; Autophagy	Angiogenesis; Apoptosis; Autophagy; MAPK; Tyrosine Kinase/Adaptors
	Regorafenib Hydrochloride (BAY73-4506 hydrochloride) 是一种新型口服多激酶抑制剂，可抑制血管生成、基质和致癌受体酪氨酸激酶，具有强大的临床前抗肿瘤活性。它靶向作用于 VEGFR1/2/3、PDGFRβ、Kit、RET 和 Raf-1，IC50值分别为 13/4.2/46、22、7、1.5 和 2.5 nM。
T3646	RSL3 RSL3 1S,1S,3R-RSL3	Ferroptosis; GPX; Glutathione Peroxidase	Apoptosis; Metabolism; oxidation-reduction
	RSL3 (RSL3 1S) 是一种 GPX4 的抑制剂，抑制阻断 GSH 合成的 system xc- (IC50=100 nM)。RSL3 是一种不依赖 VDAC 的铁死亡激活剂，对携带致癌 RAS 的肿瘤细胞具有选择性。
T9072	Tuxobertinib BDTX-189	EGFR; HER; BTK; RIP kinase	Angiogenesis; Apoptosis; JAK/STAT signaling; NF-κB; Tyrosine Kinase/Adaptors
	Tuxobertinib (BDTX-189) 是一种高效可口服的选择性 EGFR 和 HER2变构突变抑制剂，具有抗癌活性。它对 EGFR、HER2、BLK 和 RIPK2 的 KD 值分别为 0.2、0.76、13 和 1.2 nM。
T21981	Phthalazinone pyrazole	Aurora Kinase	Cell Cycle/Checkpoint; Chromatin/Epigenetic
	Phthalazinone pyrazole 是强效、选择性和口服生物可利用的 Aurora-A 激酶抑制剂，IC50值为 0.031 μM。它抑制人胚胎干细胞向肝细胞样细胞分化过程中的上皮间质转化。它还可阻止有丝分裂并随后通过增殖细胞的凋亡抑制肿瘤生长。
TQ0048	BI-882370	Raf	MAPK
	BI-882370 是高选择性的RAF 激酶抑制剂，其结合位于 BRAF 激酶的 DFG-out 无活性构象处 (ATP 结合位点)。它抑制 SRC 家族激酶，也抑制 BRAFV600E-mutant、WT BRAF 和 CRAF 激酶，IC50值分别为 0.4、0.8 和 0.6 nM。
T20168	Aurothiomalate sodium 金硫丁二钠,Myocrisin,Myocrisine,Miochrysin,Sodium aurothiomalate,Myochrysine,gold sodium thiomalate	Others; PKC	Chromatin/Epigenetic; Cytoskeletal Signaling; Others
	Aurothiomalate sodium (Miochrysin) 是一种选择性的致癌 PKCι信号传导抑制剂，可抑制肿瘤细胞增殖。它是一种硫氧还蛋白还原酶 (TrxR) 抑制剂，也是一种抗风湿剂。
T6017	Linsitinib OSI-906,林西替尼	IGF-1R	Tyrosine Kinase/Adaptors
	Linsitinib (OSI-906) 是选择性的、有效的、具有口服活性的IGF-1和胰岛素受体(IR)的双重抑制剂，IC50分别为 35 和 75 nM。
T8488	GMB-475	Bcr-Abl	Angiogenesis; Cytoskeletal Signaling; Tyrosine Kinase/Adaptors
	GMB-475 是一种基于PROTAC 的BCR-ABL1酪氨酸激酶降解剂，克服了BCR-ABL1依赖的耐药性。 GMB-475 靶向 BCR-ABL1 蛋白并募集 E3 连接酶 Von Hippel Lindau (VHL)。导致泛素化和随后的致癌融合蛋白降解
T63049	CHD1Li 6.11	Others	Others
	CHD1Li 6.11 是一种致癌 CHD1L 的有效抑制剂，能够作用于 cat-CHD1L 重组蛋白 (IC50: 3.3 μM)。CHD1Li 6.11 是一种口服具有活力的抗肿瘤剂，明显减少由分离的准间充质细胞 (M 表型) 产生的 CRC 异种移植物的肿瘤体积，这些细胞具有增强的致瘤特性。
T70476	SML-10-70-1
	SML-10-70-1 is a Novel Active Site Inhibitor of Oncogenic K-Ras G12C.
T34670	SNIPER(ABL)-38
	SNIPER(ABL)-38 is a specific and nongenetic IAP-dependent protein eraser (SNIPER) which acts as a protein degradation inducer of oncogenic BCR-ABL protein.
T10846	CMLD010509 SDS-1-021	Others	Others
	CMLD010509 (SDS-1-021) is a highly selective inhibitor of the oncogenic translation program supporting multiple myeloma (MM)-including key oncoproteins such as MDM2, CCND1, MYC, MAF, and MCL-1.
T33219	MB725 MB 725,MB-725
	MB725 is a strong and selective inducer of viability reduction in several cancer cell lines containing the oncogenic p53-Y220C mutation.
T1931	6H05 K-Ras inhibitor	Raf; Ras	GPCR/G Protein; MAPK
	6H05 (K-Ras inhibitor) 是致癌突变体 K-Ras(G12C) 的选择性变构抑制剂。
T71635	Murayaquinone
	Murayaquinone is a hepatitis C virus proteinase inhibitor and small molecule antagonist of the oncogenic Tcf/β-catenin protein complex.
T29159	WJD008 WJD-008,WJD 008
	WJD008 is a dual inhibitor of phosphatidylinositol 3-kinase (PI3K)/mammalian target of rapamycin. WJD008 prevents PI3K signaling and inhibits the proliferation of transformed cells with oncogenic PI3K mutant. WJD008 has antiproliferative and anticlonogeni
T32419	KRAS4b-PDEδ stabilizer C19
	KRAS4b-PDEδ stabilizer C19 is a stabilizer of the KRAS4b-PDEδ complex which decreases the proliferation of colorectal cancer cells, and increases apoptosis via decreased activation of oncogenic KRAS4b signaling.
T71717	KRAS4b-IN-D14
	KRAS4b-IN-D14 is a specific inhibitor of oncogenic KRAS4b signaling which stabilizes the KRAS4b-PDEδ complex and remarkably decreases tumor size and triggered apoptosis of tumor cells.
T69264	Aristeromycin diphosphate
	Aristeromycin diphosphate is an inhibitor of S-adenosylhomocysteine hydrolase (AHCY), inducing miR-26a and regulating oncogenic EZH2 expression, showing high inhibitory activity against AHCY, and causing growth inhibition of prostate cancer.
TP1979	NLS-StAx-h
	Wnt inhibitor (IC50 = 1.4 μM). Stapled peptide inhibitor of oncogenic Wnt signaling. Inhibits β-catenin-transcription factor interactions. Inhibits proliferation and migration of colorectal cancer cells. Cell permeable.
T68383	BIIB028
	BIIB028 is a small-molecule inhibitor of heat shock protein (Hsp) 90 with potential antineoplastic activity. Hsp90 inhibitor BIIB028 blocks the binding of oncogenic client proteins to Hsp90, which may result in the proteasomal degradation of these proteins and so the inhibition of tumor cell proliferation. Hsp90 is a molecular chaperone that plays a key role in the conformational maturation of oncogenic signaling proteins, such as Her2/Erbb2, Akt, Raf1, Bcr-Abl, and mutated p53, in addition to o...
T39688	Zeteletinib BOS-172738,DS-5010,Zeteletinib
	Zeteletinib (BOS-172738; DS-5010) is a highly potent and selective orally active inhibitor of the RET kinase. It demonstrates nanomolar potency against RET while exhibiting over 300-fold selectivity against VEGFR2. Zeteletinib exhibits remarkable efficacy against the wild-type RET, RET V804M/L gatekeeper mutants, as well as the frequently occurring oncogenic RET mutation M918T. Its antitumor activity is potent.
T82381	Fmoc-Thr(GalNAc(Ac)3-β-D)-OH
	Fmoc-Thr(GalNAc(Ac)3-β-D)-OH 通过抑制癌细胞生长及增强免疫反应的方式，针对特定癌症途径发挥作用。
T71837	HBX
	HBX is a deubiquitinase inhibitor. It inhibits HAdV type 5 (species C, HAdV-C5) replication and oncogenic transformation through inhibition of the cellular pro-viral factor ubiquitin-specific protease 7 (USP7). HBX also significantly inhibits virus genome replication and progeny release of all adenovirus types tested, with the exception of types 12 and 31, from tested species.
T75140	CPD-1224
	CPD-1224 是口服有效的 ALK 抑制剂，是耦连cereblon 配体的ALK 抑制剂衍生物。CPD-1224 靶向 EML4-ALK 致癌融合蛋白，并降解 ALK 和突变体 L1196M/G1202R。
T39927	Zeteletinib hemiadipate BOS-172738 hemiadipate,DS-5010hemiadipate,Zeteletinib hemiadipate
	Zeteletinib hemiadipate (BOS-172738; DS-5010) is an orally active compound that functions as a selective inhibitor of RET kinase. It exhibits nanomolar potency against RET and a 300-fold selectivity towards VEGFR2. Notably, Zeteletinib hemiadipate demonstrates exceptional effectiveness against various forms of RET, including the wild type, RET V804M/L gatekeeper mutants, and the oncogenic RET mutation M918T. Additionally, Zeteletinib hemiadipate exerts potent antitumor effects.
T74278	HSP70-IN-3
	HSP70-IN-3 是一种有效的热休克蛋白 (HSP70) 抑制剂 (ASZ001 和 C3H10T1/2 的 IC50分别为1.1和1.9 μM)。HSP70-IN-3 具有抗 Hedgehog 信号转导通路活性和抗增殖活性，并降低致癌转录因子 GLI1 的表达。
T64059	G12Si-5
	G12Si-5 是一种共价的 K-RasG12S 突变体抑制剂，其 Ki 值为 26 μM。G12Si-5 能够结合 S-IIP 结构域，抑制致癌信号。G12Si-5 能够减少 KRAS G12S 突变细胞中的 ERK 磷酸化水平。
T70424	EBI-907
	EBI-907 is a highly potent and orally efficacious B-RafV600E inhibitor. EBI-907 displays a low single-digit nanomolar activity (IC50 = 4.9 nM), which is >10-fold more potent than Vemurafenib (IC50 = 59 nM). EBI-907 also exhibits high potency in selectively inhibiting the proliferation of BRAF (V600E)-dependent cell lines (A375 and Colo205) and cellular Erk phosporylation, with superior activity to Vemurafenib. EBI-907, displaying potent activity against a number of important oncogenic kinases i...
T63970	EZH2-IN-11
	EZH2-IN-11 是 E2HZ 的有效抑制剂。其中 EZH2 的致癌活性已被各种不同癌症类型中的大量研究中证实。EZH2-IN-11 对癌症疾病表现出研究潜力。
T69055	PD153035 nitrate
	PD153035 is a ATP-competitive EGFR inhibitor with an IC50 and Ki of 25 and 6 pM. PD153035 effectively blocks the enhancement of mitogenesis, induction of early gene expression, and oncogenic transformation that occur in response to EGF receptor stimulation. With human fibroblasts and epidermoid carcinoma cells, PD153035 at nanomolar concentrations rapidly inhibits EGFR autophosphorylation. With breast and ovarian cancer cells, PD153035 not only blocks cell growth via inhibition of EGFR, but also...
T68760	Luminespib mesylate
	Luminespib, also known as AUY-922, NVP-AUY922, VER52296, is a derivative of 4,5-diarylisoxazole and a third-generation heat shock protein 90 (Hsp90) inhibitor with potential antineoplastic activity. Hsp90 inhibitor AUY922 has been shown to bind with high affinity to and inhibit Hsp90, resulting in the proteasomal degradation of oncogenic client proteins; the inhibition of cell proliferation; and the elevation of heat shock protein 72 (Hsp72) in a wide range of human tumor cell lines.
T78694	SHP2-IN-13
	SHP2-IN-13是一种针对SHP2“tunnel site” 的变构抑制剂，具备高选择性及口服活性，IC50值为83.0 nM。该化合物可作为研究潜力药物，用于治疗携带RTK致癌驱动因素的癌症以及SHP2相关疾病。
T9661	MB710
	MB710 是一种氨基苯并噻唑衍生物，是致癌 p53 突变体 Y220C 的稳定剂。MB710 与 Y220C 口袋紧密结合并稳定p53-Y220C，Kd 值为 4 μM。 MB710 在 p53-Y220C 细胞系中显示抗癌活性。
T63436	Aurora A inhibitor 1
	Aurora A inhibitor 1 是有效的、选择性的 Aurora A 抑制剂。 Aurora A 与多种组织学起源的癌症有关，而且在过度表达时可能表现出致癌活性。Aurora A inhibitor 1 表现出潜力进行 Aurora A 介导的癌症疾病的研究。
T78651	Glecirasib JAB-21822,KRAS G12C inhibitor 36	Ras	GPCR/G Protein; MAPK
	Glecirasib (KRAS G12C inhibitor 36) 作为潜在的KRAS G12C抑制剂，在Ras蛋白家族中发挥作用，对细胞内信号传递具重要影响，并在生长发育中扮演关键角色。本化合物显示出研究KRAS G12C介导的癌症潜力。
T26456	A 83586C A83586C,A-83586C
	A-83586C is a depsipeptide antibiotic from Streptomyces karnatakensis with potent against Gram-positive activity in vitro. A-83586C acts as a highly potent inhibitor of beta-catenin/TCF4 signaling within cancer cells, while simultaneously downregulating o

化合物

Cat.No: T21302

Synonym: UNC 569

Target: TAM Receptor

PF-3758309 hydrochloride

Cat.No: T4230

Synonym: PF-03758309 hydrochloride

Target: Apoptosis, PAK

Cat.No: T6626

Synonym: PF-309,PF-03758309,PF 3758309

Target: Apoptosis, PAK

Cat.No: T7326

Synonym: 6H05 TFA,6H05 trifluoroacetate

Target: Ras

Ras Inhibitory Peptide acetate

Cat.No: T37422L

Synonym: Ras Inhibitory Peptide acetate(159088-48-9 Free base)

Target: Ras

K-Ras(G12C) inhibitor 9

Cat.No: T6556

Target: Raf

K-Ras(G12C) inhibitor 12

Cat.No: T6555

Target: Apoptosis, Raf, Ras

Cat.No: T9589

Target: SGK

Cat.No: T2275

Synonym: 4,7-二氯-1,3-二氢-3-羟基-3-[2-(4-甲氧基苯基)-2-氧代乙基]-2H-吲哚-2-酮

Target: Apoptosis, DNA/RNA Synthesis

Cat.No: T1744

Target: Apoptosis, MEK

Cat.No: T69980

Target: BTK, Protease

Cat.No: T60031

Cat.No: T6284

Synonym: AT13387,Onalespib (AT13387)

Target: HSP

Regorafenib Hydrochloride

Cat.No: T8402

Synonym: 瑞戈非尼盐酸盐,BAY73-4506 hydrochloride

Target: Raf, VEGFR, c-RET, PDGFR, Autophagy

Cat.No: T3646

Synonym: RSL3 1S,1S,3R-RSL3

Target: Ferroptosis, GPX, Glutathione Peroxidase

Cat.No: T9072

Synonym: BDTX-189

Target: EGFR, HER, BTK, RIP kinase

Phthalazinone pyrazole

Cat.No: T21981

Target: Aurora Kinase

Cat.No: TQ0048

Target: Raf

Aurothiomalate sodium

Cat.No: T20168

Synonym: 金硫丁二钠,Myocrisin,Myocrisine,Miochrysin,Sodium aurothiomalate,Myochrysine,gold sodium thiomalate

Target: Others, PKC

Cat.No: T6017

Synonym: OSI-906,林西替尼

Target: IGF-1R

Cat.No: T8488

Target: Bcr-Abl

Cat.No: T63049

Target: Others

Cat.No: T70476

Cat.No: T34670

Cat.No: T10846

Synonym: SDS-1-021

Target: Others

Cat.No: T33219

Synonym: MB 725,MB-725

Cat.No: T1931

Synonym: K-Ras inhibitor

Target: Raf, Ras

Cat.No: T71635

Cat.No: T29159

Synonym: WJD-008,WJD 008

KRAS4b-PDEδ stabilizer C19

Cat.No: T32419

Cat.No: T71717

Aristeromycin diphosphate

Cat.No: T69264

Cat.No: TP1979

Cat.No: T68383

Cat.No: T39688

Synonym: BOS-172738,DS-5010,Zeteletinib

Fmoc-Thr(GalNAc(Ac)3-β-D)-OH

Cat.No: T82381

Cat.No: T71837

Cat.No: T75140

Zeteletinib hemiadipate

Cat.No: T39927

Synonym: BOS-172738 hemiadipate,DS-5010hemiadipate,Zeteletinib hemiadipate

Cat.No: T74278

Cat.No: T64059

Cat.No: T70424

Cat.No: T63970

PD153035 nitrate

Cat.No: T69055

Luminespib mesylate

Cat.No: T68760

Cat.No: T78694

Cat.No: T9661

Aurora A inhibitor 1

Cat.No: T63436

Cat.No: T78651

Synonym: JAB-21822,KRAS G12C inhibitor 36

Target: Ras

Cat.No: T26456

Synonym: A83586C,A-83586C

Cat. No.	Product Name	Target	Signaling Pathways
T6S1683	Demethoxycurcumin Curcumin II,去甲氧基姜黄素,Desmethoxycurcumin,脱甲氧姜黄,Monodemethoxycurcumin	Apoptosis; Antioxidant; Antibacterial; Autophagy	Apoptosis; Autophagy; Microbiology/Virology; oxidation-reduction
	Demethoxycurcumin (Desmethoxycurcumin) 是姜黄素的主要活性成分，有抗炎和抗癌作用。
T3763	Fumaric acid Lichenic acid,Fumarate,2-Butenedioic acid,Trans-Butenedioic acid,反丁烯二酸,Donitic acid,Allomaleic acid,富马酸	Endogenous Metabolite	Metabolism
	Fumaric acid (2-Butenedioic acid) 与烟酸酶缺乏症相关，是癌症相关的内源性代谢物。
T40667	L-Azatyrosine
	L-Azatyrosine, an antitumor antibiotic derived from Streptomyces chibaensis, exhibits the ability to restore the normal phenotypic behavior of transformed cells that carry oncogenic Ras genes.
TN4028	Euchrestaflavanone B	PARP; Antifection	Chromatin/Epigenetic; DNA Damage/DNA Repair; Microbiology/Virology
	Euchrestaflavanone B shows antibacterial activity against Gram positive bacteria, Staphylococcus aureus, Bacillus subtilis and Bacillus cereus. Euchrestaflavanone B may function by inhibiting oncogenic disease, at least in part, through the inhibition of
T82326	Genkwadaphnin
	Genkwadaphnin是一种瑞香烷二萜，能够靶向内输蛋白importin-β1，减少CRPC核心驱动因子在细胞核内的积累，并关闭其下游致癌信号通路。此外，Genkwadaphnin在小鼠体内显现出能显著抑制去势抵抗性前列腺癌(CRPC)发展的抗癌活性。

天然产物

Demethoxycurcumin

Cat.No: T6S1683

Synonym: Curcumin II,去甲氧基姜黄素,Desmethoxycurcumin,脱甲氧姜黄,Monodemethoxycurcumin

Target: Apoptosis, Antioxidant, Antibacterial, Autophagy

Cat.No: T3763

Synonym: Lichenic acid,Fumarate,2-Butenedioic acid,Trans-Butenedioic acid,反丁烯二酸,Donitic acid,Allomaleic acid,富马酸

Target: Endogenous Metabolite

Cat.No: T40667

Euchrestaflavanone B

Cat.No: TN4028

Target: PARP, Antifection

Cat.No: T82326

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