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Cat. No.	Product Name	Target	Signaling Pathways
T0987	Gimeracil 吉美嘧啶,吉莫斯特,Gimestat	Autophagy	Autophagy
	Gimeracil (Gimestat) 是一种竞争性可逆的 DPYD(二氢嘧啶脱氢酶，DPD) 有效抑制剂，是口服氟嘧啶衍生物 S-1 的成分，能够抑制 DNA DSB 的修复。
T79799	pan-KRAS-IN-4	Ras	GPCR/G Protein; MAPK
	Pan-KRAS-IN-4 (compound 5) 为一种高效KRAS抑制剂，其IC50值分别为0.37 nM (Kras G12C) 和0.19 nM (Kras G12V)。
T6877	LJH685	Apoptosis; S6 Kinase	Apoptosis; MAPK; PI3K/Akt/mTOR signaling
	LJH685 是一种选择性，ATP-竞争性的RSK 抑制剂, 抑制 RSK1/2/3 生物活性，IC50为 6、5、4 nM。
T6878	LJI308	S6 Kinase	MAPK; PI3K/Akt/mTOR signaling
	LJI308 是泛RSK 抑制剂，对 RSK1、RSK2 和 RSK3 的IC50分别为 6、4 和 13 nM。它抑制辐照、EGF 处理和表达 KRAS 突变的细胞中 RSK (T359/S363) 和 YB-1 (S102) 的磷酸化。
T6719	Varlitinib ASLAN001,ARRY-334543	HER	Angiogenesis; JAK/STAT signaling; Tyrosine Kinase/Adaptors
	Varlitinib (ASLAN001) 是有效，可逆的泛 EGFR 小分子抑制剂，对 HER1，HER2 和 HER4 的 IC50 值分别为7，2，4 nM。
T6836	FIIN-2	FGFR	Angiogenesis; Tyrosine Kinase/Adaptors
	FIIN2 是一种 FGFR 的不可逆抑制剂，能够抑制 FGFR1 (IC50:3.1 nM)，FGFR2 (IC50:4.3 nM)，FGFR3 (IC50:27 nM) 和 FGFR4 (IC50:45 nM)。
T7017	WNK463	Serine/threonin kinase	Cell Cycle/Checkpoint; Metabolism
	WNK463 是口服有活性的 WNK 激酶抑制剂，能够抑制 WNK1 (IC50:5 nM)、WNK2 (IC50:1 nM)、WNK3 (IC50:6 nM)及 WNK4 (IC50:9 nM)。
T77661	h-NTPDase-IN-4	Phosphatase	Metabolism
	h-NTPDase-IN-4 是 NTPDase 的泛抑制剂，对 h-NTPDase1, 1h-NTPDase2, h-NTPDase3, h-NTPDase8具有抑制作用，IC50 分别为 3.58 μM , 10.21 μM , 0.13 μM , 13.57 μM 。
T19649	PF-06273340 PF 6273340,PF 06273340,PF6273340,PF-6273340	Trk receptor	Tyrosine Kinase/Adaptors
	PF-06273340 是一种口服具有活力的、具有选择性的外周限制性Trk 泛抑制剂。
T6380	AMG 900 AMG900,AMG-900,莪术醇.姜黄醇	p38 MAPK; Tyrosine Kinases; Aurora Kinase	Cell Cycle/Checkpoint; Chromatin/Epigenetic; MAPK; Tyrosine Kinase/Adaptors
	AMG 900 是一种有效且高度选择性的泛极光激酶抑制剂，对Aurora A、B 和C 的IC50分别为 5 nM、4 nM 和 1 nM。
T14214	AMG 511	PI3K	PI3K/Akt/mTOR signaling
	AMG 511 是一种高效的、口服有效的 I 类 pan-PI3K 抑制剂，对 PI3Kα, β, δ 和 γ 作用的 Ki 值分别为 4 nM, 6 nM, 2 nM 和 1 nM。它它显著抑制了 PI3K 信号，减少 p-Akt (Ser473)。它在小鼠胶质母细胞瘤移植瘤模型中具有抗肿瘤作用。
T13058	T025	CDK	Cell Cycle/Checkpoint
	T025 是一种泛 CLK 抑制剂，对 CLK1-4 的 Kd 分别为 4.8、0.096、6.5、0.61 和 0.074 nM。 T025 在血液学和实体癌细胞系中表现出抗增殖活性，IC50 为 30-300 nM。 T025 可用于 MYC 驱动疾病的研究。
T2235	Dactolisib 2-甲基-2-[4-[3-甲基-2-氧代-8-(喹啉-3-基)-2,3-二氢咪唑并[4,5-c]喹啉-1-基]苯基]丙腈,BEZ235,NVP-BEZ235	ATM/ATR; PI3K; mTOR; Autophagy	Autophagy; DNA Damage/DNA Repair; PI3K/Akt/mTOR signaling
	Dactolisib (BEZ235) 是一种可口服的 pan-class IPI3K 和 mTOR 抑制剂，抑制 mTORC1和 mTORC2，作用于 p110α/γ/δ/β和 mTOR，IC50分别为 4 nM/5 nM/7 nM/75 nM 和 20.7 nM。
T3334	Velpatasvir GS-5816,维帕他韦	HCV Protease; SARS-CoV	Microbiology/Virology; Proteases/Proteasome
	Velpatasvir (GS-5816) 是一种的 HCV NS5A 抑制剂。它也是 SARS-CoV 3CLpro 的抑制剂，IC50为 2.16 μM。
T6055	Quisinostat 奎诺司他,JNJ-26481585	Apoptosis; HDAC; Autophagy	Apoptosis; Autophagy; Chromatin/Epigenetic; DNA Damage/DNA Repair
	Quisinostat (JNJ-26481585) 是一种高效的，具有口服活性的 pan-HDAC 抑制剂，对 HDAC1、HDAC2、HDAC4、HDAC10、HDAC11 作用的 IC50值范围为 0.11-0.64 nM。它在成神经细胞瘤中能诱导自噬，具有广泛的抗肿瘤活性。
T6865	Quisinostat dihydrochloride Quisinostat 2HCl,Quisinostat (JNJ-26481585) 2HCl,JNJ26854165(Quisinostat) 2HCl,JNJ-26481585 2HCl	Apoptosis; HDAC; Autophagy	Apoptosis; Autophagy; Chromatin/Epigenetic; DNA Damage/DNA Repair
	Quisinostat dihydrochloride (JNJ26854165(Quisinostat) 2HCl) 是一种有口服活性，高效的 pan-HDAC 抑制剂，具有广泛的抗肿瘤活性。它对 HDAC1、HDAC2、HDAC4、HDAC10和HDAC11 的IC50值分别为 0.11 nM、0.33 nM、0.64 nM、0.46 nM 和 0.37 nM。
T17169	Trk-IN-4 PF-6683324 isomer	Trk receptor	Tyrosine Kinase/Adaptors
	Trk-IN-4 is an effective pan-Trk inhibitor in cell-based assays (IC50s: 1.9 nM, 2.6 nM, and 1.1 nM for TrkA, TrkB, and TrkC, respectively).
T37085	Luxeptinib
	Luxeptinib (CG-806) is a novel pan-FLT3/pan-BTK inhibitor that is administered orally. It exhibits potent and reversible inhibition of these enzymes, acting through a non-covalent mechanism. Luxeptinib effectively induces cell cycle arrest, apoptosis, or autophagy in acute myeloid leukemia cells [1][2][3][4].
T74495	NS5A-IN-4
	NS5A-IN-4 (Compound 1.12) 是一种具有口服活性的泛基因型丙型肝炎病毒 (HCV)NS5A 抑制剂，对gT1b、gT1a、gT2a、gT3a,gT4a 和gT5a 的IC50分别为 1.2、2296、4.6、362、10.3 和 693 pM。
T63770	PI3K/mTOR Inhibitor-4
	PI3K/mTOR Inhibitor-4 是一种口服具有活力的泛 I 类 PI3K/mTOR 抑制剂。PI3K/mTOR Inhibitor-4 具有酶抑制作用，能够作用于 PI3Kα (IC50: 0.63 nM)、PI3Kγ (IC50: 22 nM)、PI3Kδ (IC50: 9.2 nM) 和 mTOR (IC50: 13.85 nM)。PI3K/mTOR Inhibitor-4 能够用于研究癌症。
T68039	cep-5214
	CEP-5214是一种有效的、低纳摩尔的人 VEGF-R 酪氨酸激酶泛抑制剂，对 VEGF-R1/FLT-1、VEGF-R2/KDR 和VEGF-R3/FLT-4的IC50分别为16、8和4 nM，细胞活性与分离的酶活性相当。
T38847	Vevorisertib Vevorisertib,ARQ 751
	Vevorisertib (ARQ 751) is a highly effective oral compound that selectively inhibits pan-AKT serine/threonine kinases such as AKT1 (with an IC50 value of 0.55 nM), AKT2 (with an IC50 value of 0.81 nM), and AKT3 (with an IC50 value of 1.31 nM). This compound, either as a standalone treatment option or in combination with other anti-cancer agents, is ideally suited for conducting research on solid tumors characterized by PIK3CA/AKT/PTEN mutations[4].
T69200	CGP74514A
	CGP74514A is a CDK1 inhibitor with potential anticancer activity. In U937 cells, CGP74514A - induced apoptosis (5 microM) became apparent within 4 hr and approached 100% by 24 hr. The pan- caspase inhibitor Boc-fmk and the caspase-8 inhibitor lETD-fmk opposed CGP74514A -induced caspase-9 activation and PARP degradation, but not cytochrome c or Smac/DIABLO release. CGP74514A -mediated apoptosis was substantially blocked by ectopic expression of full-length Bel- 2, a loop-deleted mutant Bcl-2, and...
T35771	Destruxin B2
	Destruxin B2 is a cyclic hexadepsipeptide mycotoxin that has been found in M. anisopliae and has antiviral, insecticidal, and phytotoxic activities.1,2,3 It inhibits secretion of hepatitis B virus surface antigen (HBsAg) by Hep3B cells expressing hepatitis B virus (HBV) DNA (IC50 = 1.3 μM).1 Destruxin B2 is toxic to Sf9 insect cells in an electric cell-substrate impedance sensing (ECIS) test with a 50% inhibitory concentration (ECIS50) value of 92 μM.4 It is also phytotoxic to B. napus leaves.3 ...
T38381	CAY17c
	CAY17c is an inhibitor of bromodomain-containing protein 4 (BRD4; IC50= 0.71 μM), as well as class I histone deacetylases (HDACs; IC50s = 0.046, 0.058, 0.075, and 0.167 μM for HDAC1, -2, -3, and -8, respectively) and class IIb HDACs (IC50s = 0.073 and 0.923 μM for HDAC6 and HDAC10, respectively).1It is selective for these enzymes over BRD2, -3, and -T (IC50s = >20 μM for all), as well as over HDAC4, -5, -7, -9, and -11 (IC50s = >10 μM for all). CAY17c inhibits the proliferation of HCT116, SW620,...
T36996	MSA-2 dimer
	MSA-2 dimer is a selective, orally active non-nucleotide STING agonist (Kd=145 μM) with long-term antitumor and immunogenic activity. MSA-2 dimer is bound to STING as a non-covalent dimer exhibiting higher permeability than cyclic dinucleotide[1]. MSA-2 dimer (60 mg/kg; p.o.; 50 days) inhibits tumor growth and prolongs overall survival[1]. MSA-2 dimer (40 mg/kg; s.c.; 25 days) induces complete tumor regression[1].MSA-2 dimer (60 mg/kg; p.o.; 4 hours) increases proinflammatory cytokine (IFN-β) le...

化合物

Cat.No: T0987

Synonym: 吉美嘧啶,吉莫斯特,Gimestat

Target: Autophagy

pan-KRAS-IN-4

Cat.No: T79799

Target: Ras

Cat.No: T6877

Target: Apoptosis, S6 Kinase

Cat.No: T6878

Target: S6 Kinase

Cat.No: T6719

Synonym: ASLAN001,ARRY-334543

Target: HER

Cat.No: T6836

Target: FGFR

Cat.No: T7017

Target: Serine/threonin kinase

Cat.No: T77661

Target: Phosphatase

Cat.No: T19649

Synonym: PF 6273340,PF 06273340,PF6273340,PF-6273340

Target: Trk receptor

Cat.No: T6380

Synonym: AMG900,AMG-900,莪术醇.姜黄醇

Target: p38 MAPK, Tyrosine Kinases, Aurora Kinase

Cat.No: T14214

Target: PI3K

Cat.No: T13058

Target: CDK

Cat.No: T2235

Synonym: 2-甲基-2-[4-[3-甲基-2-氧代-8-(喹啉-3-基)-2,3-二氢咪唑并[4,5-c]喹啉-1-基]苯基]丙腈,BEZ235,NVP-BEZ235

Target: ATM/ATR, PI3K, mTOR, Autophagy

Cat.No: T3334

Synonym: GS-5816,维帕他韦

Target: HCV Protease, SARS-CoV

Cat.No: T6055

Synonym: 奎诺司他,JNJ-26481585

Target: Apoptosis, HDAC, Autophagy

Quisinostat dihydrochloride

Cat.No: T6865

Synonym: Quisinostat 2HCl,Quisinostat (JNJ-26481585) 2HCl,JNJ26854165(Quisinostat) 2HCl,JNJ-26481585 2HCl

Target: Apoptosis, HDAC, Autophagy

Cat.No: T17169

Synonym: PF-6683324 isomer

Target: Trk receptor

Cat.No: T37085

Cat.No: T74495

PI3K/mTOR Inhibitor-4

Cat.No: T63770

Cat.No: T68039

Cat.No: T38847

Synonym: Vevorisertib,ARQ 751

Cat.No: T69200

Cat.No: T35771

Cat.No: T38381

Cat.No: T36996

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