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39

抑制剂 & 化合物

2

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T38732	PERK-IN-4	PERK	Apoptosis
	PERK-IN-4 是一种具有高效性和选择性的 PERK 抑制剂，IC50 值为 0.3 nM。PERK-IN-4 可用于研究癌症和神经系统疾病。
T10299	AMG PERK 44	ERK	MAPK
	AMG PERK 44 is an orally active and selective PERK inhibitor (IC50: 6 nM) and induces autophagy. It has 1000-fold and 160-fold selectivity over GCN2 (IC50: 7300 nM) and B-Raf (IC50 >1000 nM), respectively.
T72053	PERK-IN-6	PERK	Apoptosis
	PERK-IN-6 是一种新型高效的 PERK 抑制剂(IC50 : 2.5 nM)。
T12410	PERK-IN-3	ERK	MAPK
	PERK-IN-3 is a potent inhibitor of PERK(IC50 of 7.4 nM).
T12409	PERK-IN-2	ERK	MAPK
	PERK-IN-2 is a potent inhibitor of PERK(IC50 of 0.2 nM).
T63008	PERK-IN-5
	PERK-IN-5 是一种高度选择性的、高效的、口服具有活力的蛋白激酶 R 样内质网 (ER) 激酶 (PERK) 抑制剂，能够作用于 PERK (IC50: 2 nM) 与 p-eIF2α (IC50: 9 nM)。在 786-O 肾细胞癌异种移植瘤模型中，PERK-IN-5 可以明显抑制肿瘤生长。
T63007	(S)-PERK-IN-5
	(S)-PERK-IN-5 是 PERK-IN-5 的 S 对映体。(S)-PERK-IN-5 是一种 PERK 抑制剂 (IC50: 0.101-0.250 μM)。
T2654	GSK2656157	Apoptosis; PERK; Autophagy	Apoptosis; Autophagy
	GSK2656157 是一种ATP 竞争性的PERK 选择性抑制剂，IC50值为 0.9 nM。
T9196	IACS-13909 BBP-398	Phosphatase	Metabolism
	IACS-13909 (BBP-398) 是具有口服活性的、选择性的 SHP2变构抑制剂，其 IC50=15.7 nM，Kd=32 nM。与其他磷酸酶相比，它对 SHP2的选择性更高。它能够抑制受体酪氨酸激酶 (RTK)/MAPK 途径的信号传导，并具有抗癌作用。
T6854	GSK621	Apoptosis; AMPK; Autophagy	Apoptosis; Autophagy; Chromatin/Epigenetic; PI3K/Akt/mTOR signaling
	GSK621 是一种特异性AMPK 激动剂，对 AML 细胞系的IC50值为13-30 μM。它可诱导自噬和凋亡，还可诱导eiF2α磷酸化。
T2614	GSK2606414	Apoptosis; PERK; Autophagy	Apoptosis; Autophagy
	GSK2606414 是可渗透细胞且有口服活性的蛋白激酶 R 样内质网激酶抑制剂，IC50值为 0.4 nM。
T21976	ONO-8130	Prostaglandin Receptor	GPCR/G Protein; Immunology/Inflammation
	ONO-8130 是前列腺素 EP1 受体选择性拮抗剂，口服有活力，能够阻断 L6 脊髓中ERK 的磷酸化。它可缓解环磷酰胺致膀胱炎小鼠的膀胱疼痛，可用于研究间质性膀胱炎。
T22436	Takeda-6d	VEGFR	Angiogenesis; Tyrosine Kinase/Adaptors
	Takeda-6d 是一种新型、有效的 DFG-out RAF/血管内皮生长因子受体 2 (VEGFR2) 抑制剂，IC50 分别为 7.0 nM 和 2.2 nM。
T6183	ISRIB (trans-isomer) ISRIB,ISRIB trans-isomer,trans-isomer,trans-ISRIB	Apoptosis; PERK; Autophagy	Apoptosis; Autophagy
	ISRIB (trans-isomer) (ISRIB trans-isomer)是一种 PERK 的高效抑制剂，可有效逆转 eIF2α 磷酸化的作用，IC50值为 5 nM。
T2027	ISRIB	PERK	Apoptosis
	ISRIB 是一种有效的选择性 PERK 抑制剂。
T11374	GCN2-IN-6	Others; PERK	Apoptosis; Others
	GCN2-IN-6 经酶法和细胞分析证实，是一种口服有效GCN2抑制剂，IC50分别为1.8 nM 和9.3 nM。GCN2-IN-6 还是 eIF2α 激酶PERK 抑制剂，在酶法测定和细胞测定中的IC50分别为 0.26 nM 和 230 nM。
T14902	CCT020312	PERK	Apoptosis
	CCT020312 是 EIF2AK3 和 PERK 的选择性激活剂。 CCT020312 持久抑制细胞增殖并引发 EIF2A 的磷酸化。
T61859	MK-28	Antiviral; PERK	Apoptosis; Immunology/Inflammation
	MK-28 是一种具有选择性的 PERK 激动剂，可降低亨廷顿病模型的毒性并延长生存期。MK-28 对MK28胃癌细胞有显著的杀伤作用。
T73053	BAY 2965501	PERK	Apoptosis
	BAY 2965501 是一种有效且具有的选择性二酰基甘油激酶 zeta (DGKζ) 抑制剂，诱导 pERK 激活。BAY 2965501 可用于研究癌症。
T8423	ML417	Dopamine Receptor; Arrestin	GPCR/G Protein; Neuroscience
	ML417 是选择性的，可透过血脑屏障的 D3 多巴胺受体激动剂，EC50=38 nM。它能够促进 D3R 介导的 β-arrestin 易位、G 蛋白介导的信号传导和 pERK 磷酸化，对其他 GPCR 介导的信号传导影响小。它对毒素诱导的多巴胺能神经元变性具有神经保护活性。
T11738	K-Ras G12C-IN-4	Ras	GPCR/G Protein; MAPK
	K-Ras G12C-IN-4 是一种 KRAS G12C 共价抑制剂。
T39117	PLX7922 PLX7922
	PLX7922, a RAF inhibitor, demonstrates binding affinity with BRAF V600E and exhibits inhibitory effects on pERK in BRAF V600E cell lines, while inducing pERK activation in mutant NRAS cell lines.
T79123	PF-07284892 ARRY-558
	PF-07284892 (ARRY-558)作为一种SHP2抑制剂，具有口服活性，其IC50为21 nM，能有效降低pERK表达。
T73364	MEK-IN-5
	MEK-IN-5 是一种有效的 MEK 抑制剂和 NO 供体。MEK-IN-5 以剂量和时间依赖性方式显著降低 pMEK 和 pERK 的表达水平。MEK-IN-5 诱导 MDA-MB-231 细胞凋亡 (apoptosis)。
T62371	SOS1-IN-12
	SOS1-IN-12 是一种 SOS1 的有效抑制剂，能够作用于 SOS1 (Ki: 0.11 nM)，对 pERK (IC50: 47 nM)。SOS1-IN-12 能够用于抗癌的研究。
T62003	SOS1-IN-13
	SOS1-IN-13 是有效的SOS1抑制剂。SOS1-IN-13抑制 SOS1 和 pERK 的IC50分别为 6.5 nM 和 327 nM。SOS1-IN-13 在抗癌研究中具有一定的价值。
T71722	Angiogenesis inhibitor BT2
	Angiogenesis inhibitor BT2 is a novel inhibitor of angiogenesis and vascular permeability, inhibiting ERK phosphorylation and the expression of FosB/ΔFosB, VCAM-1, and many genes involved in proliferation, migration, angiogenesis, and inflammation, interacting with MEK1, suppressing retinal CD31, pERK, VCAM-1, and VEGF-A165 expression.
T74356	PROTAC SOS1 degrader-2
	PROTACSOS1 degrader-2 是一种有效的 PROTACSOS1降解剂。PROTACSOS1 Degrader-2 以剂量依赖性方式降低 pERK 和 RAS-GTP 的表达水平。PROTACSOS1degrader-2 在体内显著抑制肿瘤生长。
T69106	Avarol
	Avarol induces apoptosis in pancreatic ductal adenocarcinoma cells by activating PERK-eIF2α-CHOP signaling. Avarl also acts as a competitive AChE inhibitor which are non-hepatotoxic and neuroprotective agents for Alzheimer's disease.
T22104	ML-291
	ML291 is a sufonamidebenzamide compound that induces the unfolded protein response (UPR) and overwhelms the adaptive capacity of UPR, resulting in apoptosis in various solid cancer models. It activates the PERK/eIF2a/CHOP apoptotic pathway of UPR and reduces leukemic cell burden [1].
T39874	GSK143 dihydrochloride
	GSK143 dihydrochloride is a highly selective, orally active inhibitor of spleen tyrosine kinase (SYK), exhibiting a pIC 50 value of 7.5. It effectively inhibits phosphorylated Erk (pErk) with a pIC 50 value of 7.1. The compound demonstrates anti-inflammatory properties and hinders the recruitment of immune cells in the intestinal muscularis of mice.
T71891	G-573
	G-573 is an allosteric inhibitor of MEK that is both potent and selective. The IC(50) value for pERK inhibition in HCT116 tumours by G-573 was estimated to be 0.406 ÂµM. The IC(50) values for tumour growth inhibition in HCT116 and H2122 were estimated to be 3.43 and 2.56 ÂµM, respectively. ED(50) estimates in HCT116 and H2122 mouse xenograft models were estimated to be ~4.6 and 1.9 mg/kg/day, respectively.
T38626	GSK143
	GSK143 is a potent orally active and highly selective inhibitor of spleen tyrosine kinase (SYK) with a pIC 50 of 7.5. Furthermore, GSK143 effectively inhibits phosphorylated Erk (pErk) with a pIC 50 value of 7.1. In addition, GSK143 exhibits promising anti-inflammatory properties by reducing inflammation and impeding the recruitment of immune cells in the intestinal muscularis of mice.
T74844	Antiproliferative agent-23
	Antiproliferative agent-23，一种微管去稳定剂(MDA)，通过扰乱微管蛋白-微管系统来发挥作用。该化合物通过降低Bcl-2蛋白水平、提高Bax和Cyt c蛋白水平以及激活半胱天冬酶级联反应和线粒体依赖途径来诱导细胞凋亡。此外，Antiproliferative agent-23还能在A549/CDDP细胞（顺铂耐药癌细胞系）中通过PERK/ATF4/CHOP信号通路激活ROS介导的内质网应激，展现出抗肿瘤活性。
T73179	HDAC-IN-50
	HDAC-IN-50是一种口服活性的有效FGFR和HDAC双重抑制剂，其IC50值针对FGFR1、FGFR2、FGFR3、FGFR4、HDAC1、HDAC2、HDAC6、HDAC8分别为0.18、1.2、0.46、1.4、1.3、1.6、2.6、13 nM。该化合物能诱导(Apoptosis)及使细胞周期在G0/G1期停滞，降低pFGFR1、pERK、pSTAT3的表达，展现出抗肿瘤活性。
T79072	KRAS G12D modulator-1	Ras	GPCR/G Protein; MAPK
	KRAS G12D modulator-1（compound 6）是高效KRAS G12D调节剂，NEA-G12D、PPI-G12D 和 pERK-AGS的IC50范围为1-10 μM，适用于癌症研究。
T36642	RAS/RAS-RAF-IN-1
	RAS/RAS-RAF-IN-1 is a potent RAS and RAS-RAF inhibitor. RAS/RAS-RAF-IN-1 has a KD of 5.0 μμ-15 μμ for cyclophilin A (CYPA) binding affinity. RAS/RAS-RAF-IN-1 has antitumor activity[1]. RAS/RAS-RAF-IN-1 (compound 89; for 4 hours) has an EC50 of 0.5 μμ-5.0 μμ for BRAF-GTP-KRAS-G12C disruption and has an IC50 of 1.0 μμ-10 μμ for pERK inhibition in H358 cells[1]. [1]. Meizhong Jin, et al. Compounds that participate in cooperative binding and uses thereof. WO2020132597A1.
T39726	SHP389 SHP389
	SHP389 is an allosteric SHP2 inhibitor, with an IC 50 of 36 nM for both SHP2 and p-ERK.
T36887	8(E),10(E),12(Z)-Octadecatrienoic Acid
	8(E),10(E),12(Z)-Octadecatrienoic acid is a conjugated polyunsaturated fatty acid (PUFA) that has been found inC. officinalisseed oil and has anticancer activity.1,2,3It inhibits the growth of Caco-2 cells when used at concentrations ranging from 10 to 50 μM.28(E),10(E),12(Z)-Octadecatrienoic acid (10 μM) induces formation of thiobarbituric acid reactive substances (TBARS) and apoptosis in DLD-1 colorectal adenocarcinoma cells.3It also inhibits prostaglandin biosynthesis in sheep vesicular gland...

化合物

Cat.No: T38732

Target: PERK

Cat.No: T10299

Target: ERK

Cat.No: T72053

Target: PERK

Cat.No: T12410

Target: ERK

Cat.No: T12409

Target: ERK

Cat.No: T63008

(S)-PERK-IN-5

Cat.No: T63007

Cat.No: T2654

Target: Apoptosis, PERK, Autophagy

Cat.No: T9196

Synonym: BBP-398

Target: Phosphatase

Cat.No: T6854

Target: Apoptosis, AMPK, Autophagy

Cat.No: T2614

Target: Apoptosis, PERK, Autophagy

Cat.No: T21976

Target: Prostaglandin Receptor

Cat.No: T22436

Target: VEGFR

ISRIB (trans-isomer)

Cat.No: T6183

Synonym: ISRIB,ISRIB trans-isomer,trans-isomer,trans-ISRIB

Target: Apoptosis, PERK, Autophagy

Cat.No: T2027

Target: PERK

Cat.No: T11374

Target: Others, PERK

Cat.No: T14902

Target: PERK

Cat.No: T61859

Target: Antiviral, PERK

Cat.No: T73053

Target: PERK

Cat.No: T8423

Target: Dopamine Receptor, Arrestin

K-Ras G12C-IN-4

Cat.No: T11738

Target: Ras

Cat.No: T39117

Synonym: PLX7922

Cat.No: T79123

Synonym: ARRY-558

Cat.No: T73364

Cat.No: T62371

Cat.No: T62003

Angiogenesis inhibitor BT2

Cat.No: T71722

PROTAC SOS1 degrader-2

Cat.No: T74356

Cat.No: T69106

Cat.No: T22104

GSK143 dihydrochloride

Cat.No: T39874

Cat.No: T71891

Cat.No: T38626

Antiproliferative agent-23

Cat.No: T74844

Cat.No: T73179

KRAS G12D modulator-1

Cat.No: T79072

Target: Ras

RAS/RAS-RAF-IN-1

Cat.No: T36642

Cat.No: T39726

Synonym: SHP389

8(E),10(E),12(Z)-Octadecatrienoic Acid

Cat.No: T36887

Cat. No.	Product Name	Target	Signaling Pathways
T5A2461	Bufotalin 蟾蜍他灵,Bufotaline,蟾毒它灵,蟾蜍他灵	Apoptosis; Others; Reactive Oxygen Species	Apoptosis; Immunology/Inflammation; Metabolism; NF-κB; Others
	Bufotalin (Bufotaline) 是一种从蟾酥中分离的类固醇内酯，可诱导癌细胞凋亡，也诱导内质网应激的激活，具有强大的抗肿瘤活性。
T79951	Piperkadsin A	Reactive Oxygen Species	Immunology/Inflammation; Metabolism; NF-κB
	Piperkadsin A作为一种ROS抑制剂，能够有效地抑制PMA诱导的人多形核中性粒细胞中ROS的生成，其IC50值为4.3 μM。

天然产物

Cat.No: T5A2461

Synonym: 蟾蜍他灵,Bufotaline,蟾毒它灵,蟾蜍他灵

Target: Apoptosis, Others, Reactive Oxygen Species

Cat.No: T79951

Target: Reactive Oxygen Species

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