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抑制剂 & 化合物

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Cat. No.	Product Name	Target	Signaling Pathways
T13176	TNO155 Batoprotafib	Phosphatase	Metabolism
	TNO155 是具有口服活性野生型SHP2的选择性变构抑制剂 (IC50= 0.011 µM)。它有研究 RTK 依赖性恶性肿瘤（尤其是晚期实体瘤）的潜力。
T9756	AZD-9574	PARP	Chromatin/Epigenetic; DNA Damage/DNA Repair
	AZD-9574 是 SSB 位点的 PARP1 特异性抑制剂。 AZD-9574 具有抗癌活性，可用于 HRD+ 乳腺癌和晚期实体恶性肿瘤的研究。
T16781	Rogaratinib BAY1163877	FGFR	Angiogenesis; Tyrosine Kinase/Adaptors
	Rogaratinib (BAY1163877) 选择性抑制成纤维细胞生长因子受体。
T5699	SSE15206	Apoptosis; Microtubule Associated	Apoptosis; Cytoskeletal Signaling
	SSE15206 是一种克服多药耐药性的微管聚合抑制剂，其在 HCT116 细胞中的 GI50值为 197 nM。由于癌细胞中纺锤体形成不完整，导致 G2/M 停滞，有丝分裂异常。
T62902	NDI-034858 TAK-279,NDI-03485	IL Receptor; Tyrosine Kinases	Immunology/Inflammation; Tyrosine Kinase/Adaptors
	NDI-034858 (TAK-279) 是一种酪氨酸激酶2(TYK2)抑制剂( Kd＜200 pM)，靶向 Tyk2的JH2结构域，可治疗IL12和IL23异常表达引起的自身免疫性疾病。
T79492	h-NTPDase8-IN-1	Phosphatase	Metabolism
	h-NTPDase8-IN-1 是一种特异性氨磺酰苯甲酰胺类 h-NTPDases8 抑制剂（IC 50 = 0.28 ± 0.07 μM）。h-NTPDase8-IN-1 可用于研究 h -NTPDase 表达异常带来的疾病。
TQ0236	Tirabrutinib ONO-4059,GS-4059,Velexbru	BTK	Angiogenesis; Tyrosine Kinase/Adaptors
	Tirabrutinib (GS-4059) (ONO-4059) 是一种口服有效的高选择性 Bruton’s Tyrosine Kinase (BTK) 抑制剂 (能透过血脑屏障)，其 IC50 值为 6.8 nM。Tirabrutinib 不可逆共价结合 BTK 并抑制异常 B 细胞受体信号传导。Tirabrutinib 可用于自身免疫性疾病和血液学恶性肿瘤的研究。
T15576	Indibulin 2-(1-(4-氯苄基)-1H-吲哚-3-基)-2-氧代-N-(吡啶-4-基)乙酰胺,ZIO 301,D 24851	Apoptosis; Microtubule Associated	Apoptosis; Cytoskeletal Signaling
	Indibulin (D 24851) 是一种口服有效的微管蛋白合成抑制剂，具有抗有丝分裂和抗肿瘤活性，且神经毒性小。它降低了肌间神经张力，产生异常的纺锤体，激活有丝分裂检查点蛋白 Mad2 和 BubR1，并诱导有丝分裂停滞和细胞凋亡。
T71639	AUH-6-96
	AUH-6-96 is an inhibitor of JAK/STAT signaling, inhibiting both constitutive and interleukin-6-induced STAT3 phosphorylation, selectively affecting cell viability only of cancer cells harboring aberrant JAK/STAT signaling.
T24647	PKR-IN-C51 PKRINC51,PKR IN C51,PKR-inhibitor-C51,PKR inhibitor C51
	PKR-IN-C51 is an inhibitor of protein kinase R. It acts by correcting the aberrant splicing of MBNL1-dependent pre-mRNAs in DM1 cells without affecting the splicing pattern in normal non-DM1 cells.
T70318	AMG-337 monohydrate
	AMG-337 monohydrate is a highly selective small molecule MET inhibitor. Aberrant hepatocyte growth factor (HGF)/MET signaling has been implicated in hepatocarcinogenesis, suggesting that MET may serve as an attractive therapeutic target in hepatocellular carcinoma.
T61435	(S)-Cdc7-IN-18
	(S)-Cdc7-IN-18, a potent CDC7 inhibitor, effectively impedes the overactivation of MCM2, a crucial tumor cell marker, induced by huCdc7 overexpression. Consequently, it inhibits the aberrant proliferation of tumor cells. This compound, exhibits promise for cancer disease research [1].
T79672	DUB-IN-7
	DUB-IN-7(化合物43)作为一种DUBs的抑制剂，主要用于针对JAK2活性失调所导致的疾病，例如白血病的研究。
T70941	CLR01 sodium
	CLR01 is a molecular tweezer. CLR01 reduces aggregated, pathologic, and seeding-competent α-synuclein in experimental multiple system atrophy. CLR01 inhibits aberrant superoxide dismutase 1 (SOD1) self-assembly in vitro and in the G93A-SOD1 mouse model of ALS. CLR01 inhibits Ebola and Zika virus infection. CLR01 Stabilizes a Disordered Protein-Protein Interface. CLR01, Modulates Aggregation of the Mutant p53 DNA Binding Domain and Inhibits Its Toxicity.
T36718	Tie2 Inhibitor 7
	Tie2 Inhibitor 7 blocks Tie2 kinase activity with a Ki value of 1.3 μM.. It has been shown to inhibit angiopoietin 1-induced Tie2 autophosphorylation and downstream signaling with an IC50 value of 0.3 μM. This compound can prevent endothelial cell tube formation and aberrant vessel growth in a rat model of Matrigel-induced choroidal neovascularization.
T60360	LSD1/2-IN-3
	LSD1/2-IN-3 是赖氨酸特异性去甲基化酶 1 (LSD1) 的选择性抑制剂，Ki 值是 11 nM，而对LSD2的 Ki 值为 7 μM。LSD1在肿瘤干细胞中异常表达，LSD1/2-IN-3 能够抑制LSD1活性和癌细胞增殖。
T62680	(R)-MLT-985
	(R)-MLT-985 (compound 11) 是一种 MALT1 蛋白酶的有效抑制剂 (IC50: 3 nM)。(R)-MLT-985 在 Jurkat 细胞中对 MALT1 依赖性 IL-2 的 IC50 值为 20 nM。(R)-MLT-985 对 ABC-DLBCL 细胞中的生长和异常 CARD11/BCL10/MALT1 复合物信号传导具有抑制作用。
T68267	RO5068760
	RO5068760 , a substituted hydantoin, is a potent, highly selective, non-adenosine triphosphate (ATP)-competitive MEK1/2 inhibitors. RO5068760 shows significant efficacy in a broad spectrum of tumors with aberrant mitogen-activated protein kinase pathway activation. In vitro, RO5068760 demonstrates MEK1 kinase inhibitory activity with an IC50 of 0.025 μM in a cRaf/MEK/ERK cascade assay RO5068760 showed superior efficacy in tumors harboring B-RafV600E mutation.
T70527	DAT-230
	DAT-230 is a promising microtubule inhibitor that has great potential for the treatment of fibrosarcoma in vitro and in vivo. DAT-230 exhibited potent anti-proliferative activity against various cancer cells. DAT-230 -treatment in HT-1080 cells resulted in microtubule de-polymerization and G2/M phase arrest preceding apoptosis. Phosphor-cdc2 (thr14/tyr15) reduction, cyclin B1 accumulation and aberrant spindles denoted the cyclin B1-cdc2 complex active and M phase arrest in HT-1080 cells treated ...
T60359	cis-4-Br-2,5-F2-PCPA
	cis-4-Br-2,5-F2-PCPA (S1024) 抑制 LSD1 和 LSD2，Ki 值分别为 94 nM 和 8.4 μM。癌症干细胞中 LSD1异常表达，cis-4-Br-2,5-F2-PCPA 能够通过增加 CCRF-CEM 细胞中二甲基化组蛋白 H3 的 K4 (H3K4) 水平，抑制 LSD1活性和癌细胞增殖。
T68480	4SC-207
	4SC-207 is a novel microtubule inhibitor , which shows strong anti-proliferative activity in a large panel of tumor cell lines with an average GI50 of 11 nM. In particular, 4SC-207 is active in multi-drug resistant cell lines, such as HCT-15 and ACHN, suggesting that it is a poor substrate for drug efflux pumps. 4SC-207 inhibits microtubule growth in vitro and in vivo and promotes, in a dose dependent manner, a mitotic delay/arrest, followed by apoptosis or aberrant divisions due to chromosome a...
T68459	RO4927350
	RO4927350 is a potent and highly selective non-ATP-competitive MEK1/2 inhibitor. RO4927350 selectively blocks the MAPK pathway signaling both in vitro and in vivo, which results in significant antitumor efficacy in a broad spectrum of tumor models. RO4927350 inhibits not only ERK1/2 but also MEK1/2 phosphorylation. In cancer cells, high basal levels of phospho-MEK1/2 rather than phospho-ERK1/2 seem to correlate with greater sensitivity to RO4927350. Furthermore, RO4927350 prevents a feedback inc...
T74642	DB1113
	DB1113 (Example 24) 是一种靶向蛋白激酶降解的双功能化合物。DB1113 可降解 ABL1，ABL2，BLK，CDK11B，CDK4，CSK，EPHA3，FER，GAK，LIMK1，MAP3K20，MAP4K1，MAP4K2，MAP4K3，MAP4K5，MAPK14，MAPK7，MAPK8，MAPK9，MAPKAPK2，MAPKAPK3，NLK，PDIK1L，PTK2B，RIPK1，RPS6KA1，RPS6KA3，SIK2，SIK3，STK35，TNK2 和 ULK1。DB1113 可用于研究异常激酶活性介导的疾病或紊乱。
T82971	ARI-1
	ARI-1是一种针对受体酪氨酸激酶样孤儿受体ROR1的抑制剂，对于ROR1异常表达所致的非小细胞肺癌(NSCLC)及EGFR-TKI诱导的耐药性治疗具有显著效果。该化合物能够特异性结合至ROR1的胞外卷曲结构域，并以ROR1依赖性方式抑制PI3K/AKT/mTOR信号通路，进而有效地阻断NSCLC细胞的增殖和迁移。此外，ARI-1还展现了显著的体内抗肿瘤活性。
T74644	DB0614
	DB1113 (Example 24) 是一种靶向蛋白激酶降解的双功能化合物。DB1113 可降解ABL1，ABL2，BLK，CDK11B，CDK4，CSK，EPHA3，FER，GAK，LIMK1，MAP3K20，MAP4K1，MAP4K2，MAP4K3，MAP4K5，MAPK14，MAPK7，MAPK8，MAPK9，MAPKAPK2，MAPKAPK3，NLK，PDIK1L，PTK2B，RIPK1，RPS6KA1，RPS6KA3，SIK2，SIK3，STK35，TNK2 和ULK1。DB1113 可用于研究异常激酶活性介导的疾病或紊乱。

化合物

Cat.No: T13176

Synonym: Batoprotafib

Target: Phosphatase

Cat.No: T9756

Target: PARP

Cat.No: T16781

Synonym: BAY1163877

Target: FGFR

Cat.No: T5699

Target: Apoptosis, Microtubule Associated

Cat.No: T62902

Synonym: TAK-279,NDI-03485

Target: IL Receptor, Tyrosine Kinases

h-NTPDase8-IN-1

Cat.No: T79492

Target: Phosphatase

Cat.No: TQ0236

Synonym: ONO-4059,GS-4059,Velexbru

Target: BTK

Cat.No: T15576

Synonym: 2-(1-(4-氯苄基)-1H-吲哚-3-基)-2-氧代-N-(吡啶-4-基)乙酰胺,ZIO 301,D 24851

Target: Apoptosis, Microtubule Associated

Cat.No: T71639

Cat.No: T24647

Synonym: PKRINC51,PKR IN C51,PKR-inhibitor-C51,PKR inhibitor C51

AMG-337 monohydrate

Cat.No: T70318

Cat.No: T61435

Cat.No: T79672

Cat.No: T70941

Tie2 Inhibitor 7

Cat.No: T36718

Cat.No: T60360

Cat.No: T62680

Cat.No: T68267

Cat.No: T70527

cis-4-Br-2,5-F2-PCPA

Cat.No: T60359

Cat.No: T68480

Cat.No: T68459

Cat.No: T74642

Cat.No: T82971

Cat.No: T74644

Cat. No.	Product Name	Target	Signaling Pathways
T3011	2-Amino-4-(2-aminophenyl)-4-oxobutanoic acid Kynurenine,Dl-Kynurenine,Kynurenin,3-Anthraniloylalanine,犬尿氨酸	Others; Endogenous Metabolite	Metabolism; Others
	2-Amino-4-(2-aminophenyl)-4-oxobutanoic acid (3-Anthraniloylalanine) 是一种酮类和氨基酸衍生物，具有多种生物功能，包括血管舒张、免疫调节和神经调节活性。2-Amino-4-(2-aminophenyl)-4-oxobutanoic acid 是烟酸的前体。2-Amino-4-(2-aminophenyl)-4-oxobutanoic acid 的异常产生与神经系统疾病相关的认知缺陷和抑郁症状有关。2-Amino-4-(2-aminophenyl)-4-oxobutanoic acid 在某些类型的癌细胞中过度表达，可能被用作评估癌症风险的生物标志物。

天然产物

2-Amino-4-(2-aminophenyl)-4-oxobutanoic acid

Cat.No: T3011

Synonym: Kynurenine,Dl-Kynurenine,Kynurenin,3-Anthraniloylalanine,犬尿氨酸

Target: Others, Endogenous Metabolite

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