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35

抑制剂 & 化合物

2

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T8987	Epiblastin A	Casein Kinase	Metabolism; Stem Cells
	Epiblastin A 是 ATP 竞争性的酪蛋白激酶 1 (CK1) 抑制剂，能够抑制 CK1α (IC50:8.9 µM)、 CK1δ (IC50:0.5 µM)、CK1 ɛ (IC50:4.7 µM)。它能够抑制 CK1 诱导外胚层干细胞重编程为胚胎干细胞。
T16695	Pyrintegrin	Integrin	Cytoskeletal Signaling
	Pyrintegrin 是一种 β1 整合素激动剂，也是 2,4-二取代的嘧啶，可促进胚胎干细胞存活。它可用作足细胞保护剂，能增强细胞-细胞外基质 (ECM) 粘附介导的整联蛋白信号传导，具有强大的成脂作用。
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。
T11571	HLY78 4-Ethyl-5-methyl-5,6-dihydro-[1,3]dioxolo[4,5-j]phenanthridine	Wnt/beta-catenin	Cytoskeletal Signaling; Stem Cells
	HLY78 (4-Ethyl-5-methyl-5,6-dihydro-[1,3]dioxolo[4,5-j]phenanthridine) 是 Wnt/β-catenin 信号通路的激活剂，通过靶向通道中 Axin 的 DIX 域，增强 Axin-LRP6 交联，诱导 Wnt 信号转导。
T7196	HG-10-102-01 [4-[[5-氯-4-(甲基氨基)-2-嘧啶基]氨基]-3-甲氧基苯基]-4-吗啉基甲酮	LRRK2	Autophagy
	HG-10-102-01 是富含亮氨酸重复激酶 2 和突变型G2019S 抑制剂，IC50分别为20.3 nM 和3.2 nM。
T8005	Cardiogenol C hydrochloride 2-[[2-[(4-甲氧基苯基)氨基]-4-嘧啶基]氨基]乙醇盐酸盐,Cardiogenol C HCl,Cardiogenol C	Wnt/beta-catenin	Cytoskeletal Signaling; Stem Cells
	Cardiogenol C hydrochloride (Cardiogenol C) 是一种细胞渗透性嘧啶诱导剂，能够促使 ESCs 分化为心肌细胞。在有限的可塑性范围内，它可以对已经沿袭的祖细胞类型产生心肌生成效应，是一种心肌生成试剂，在动物模型中可以用作细胞移植研究中提高心脏修复的工具。
T3221	Oct3/4-inducer-1 2-(4-(4-methoxybenzyloxy)phenyl)acetonitrile,2-(4-[(4-甲氧基苄基)氧基]苯基)乙腈	Others; OCT	Membrane transporter/Ion channel; Others
	Oct3/4-inducer-1 (2-(4-(4-methoxybenzyloxy)phenyl)acetonitrile) 是Oct3/4诱导剂，能够促进 Oct3/4 的表达和稳定，提高其在多种人体细胞中的转录活性。
T2161	Cardiogenol C	Wnt/beta-catenin	Cytoskeletal Signaling; Stem Cells
	Cardiogenol C 是一种细胞渗透性嘧啶诱导剂，能够诱导 ESCs 分化为心肌细胞(EC50:100 nM)。在有限的可塑性范围内，它可以对已经沿袭的祖细胞类型产生心肌病，是一种心肌发生剂。
T3162	IDE1	Others	Others
	IDE1 是定形内胚层诱导物，有用于器官移植等方面的潜力。
T11469	GSK-3484862	DNA Methyltransferase	Chromatin/Epigenetic
	GSK-3484862 是有效的 DNA 甲基转移酶 Dnmt1的非共价抑制剂。GSK-3484862 通过诱导 DNA 低甲基化起抗癌作用。GSK-3484862 介导小鼠胚胎干细胞的整体去甲基化。
T2019	OAC2	OCT	Membrane transporter/Ion channel
	OAC2 是一种 Oct4 激活剂，通过 Oct4 基因启动子激活表达，通过提高胚胎成纤维细胞诱导多能干细胞的产生速率来提高重编程效率，是 OAC1 的类似物。
T2301	SB 202190 FHPI,SB202190	Apoptosis; p38 MAPK; Autophagy	Apoptosis; Autophagy; MAPK
	SB 202190 (FHPI) 是一种 p38 MAPK 抑制剂，可以抑制 p38α 和 p38β2 (IC50=50/100 nM)，具有选择性和细胞渗透性。SB 202190 具有抗肿瘤活性，还可以诱导人胚胎干细胞向心肌细胞分化。
T60143	MitoBloCK-6	Apoptosis	Apoptosis
	MitoBloCK-6 是一种有效的Erv1/ALR 抑制剂，IC50分别为 900 nM 和 700 nM。MitoBloCK-6 还抑制Erv2，IC50值为1.4 μM。MitoBloCK-6 可通过释放细胞色素 c 诱导 hESCs 细胞凋亡。
T2310	CHIR-99021 Laduviglusib,CT99021,CHIR-99021	GSK-3; Wnt/beta-catenin; Autophagy	Autophagy; Cytoskeletal Signaling; PI3K/Akt/mTOR signaling; Stem Cells
	CHIR-99021 (CT99021) 是一种 Wnt/β-catenin 信号通路激活剂，也是一种 GSK-3α/β抑制剂 (IC50=10/6.7 nM)，具有选择性和口服活性。CHIR-99021 可以诱导细胞自噬，可增强小鼠和人类胚胎干细胞的自我更新。
T28866	Stemazole	Apoptosis	Apoptosis
	Stemazole 是一种新型小分子人类干/祖细胞增殖激活剂，可促进人类胚胎干细胞的存活并保持干性，促进少突胶质细胞前体细胞在体外的存活。Stemazole 能显著提高细胞存活率和克隆形成数，并呈剂量依赖性，降低细胞凋亡率，促进运动功能障碍的恢复和髓鞘的修复。Stemazole 可作为脱髓鞘疾病的治疗剂，促进OPC 体外存活和体内再生。
T3637	Pifithrin-β hydrobromide Cyclic PFT-α,PFT-β,Cyclic Pifithrin-α hydrobromide,Pifithrin-β,PFT β (hydrobromide)	Ferroptosis; p53	Apoptosis
	Pifithrin-β hydrobromide (Cyclic PFT-α) 是一种 p53 的抑制剂，可逆地阻断 p53 依赖性转录激活和细胞凋亡。IC50值为23 μM。
T77697	BML-278 BML278,BML 278	Sirtuin; Histone Methyltransferase	Chromatin/Epigenetic; DNA Damage/DNA Repair
	BML-278 是一种 SIRT1 激活剂，EC150 值为 1 μM。BML-278 增加父本和母本原核中的 H3K9 甲基化并抑制 H3K9 乙酰化，可用于改善早期胚胎发育。BML-278 促使原代人间充质细胞的细胞周期停止在 G1/S 期，可用于延缓衰老。BML-278 减少 U937 细胞中的微管蛋白乙酰化，增加小鼠 C2C12 成肌细胞的线粒体密度。
T2310L	CHIR-99021 HCl CT99021 HCl,Laduviglusib HCl	GSK-3	PI3K/Akt/mTOR signaling; Stem Cells
	CHIR-99021 HCl (Laduviglusib HCl) 是GSK-3α/β的高效选择性抑制剂，IC50值分别为10 nM和6.7 nM。它对GSK-3表现出显著的选择性，对CDC2、ERK2和其他蛋白激酶的选择性超过500倍。此外，CHIR-99021 HCl 是Wnt/β-catenin信号通路的强大激活剂。此外，它在小鼠和人类胚胎干细胞中都表现出增强自我更新的能力。此外，拉杜维格西单盐酸盐诱导自噬[1][2][3]。
T70520	TWS-119
	TWS-119 is an inhibitor of glycogen synthase kinase-3β (GSK-3β) that induces neuronal differentiation in pluripotent murine embryonal carcinoma cells and embryonic stem cells (ESCs).
T35549	Elsinochrome A
	Elsinochrome A is a perylenequinone fungal metabolite that has been found inHypomycesand has anticancer activity.1Photoactivation of elsinochrome A induces the production of singlet oxygen and apoptosis in R366.4 rhesus monkey embryonic stem cells and HCe-8693 colorectal carcinoma cells when used at concentrations ranging from 1 to 100 μM. 1.Ma, L., Tai, H., Li, C., et al.Photodynamic inhibitory effects of three perylenequinones on human colorectal carcinoma cell line and primate embryonic stem ...
T35561	MS351
	MS351 is an antagonist of chromobox 7 (CBX7) that acts by binding the CBX7 chromodomain. It enhances the binding of long noncoding RNA to the CBX7 chromodomain when used at 25 μM. MS351 induces transcriptional derepression of CBX7 target genes, including p16 (INK4a), in mouse embryonic stem cells and human prostate cancer PC3 cells.
T69743	MEDS433
	MEDS433 is a dihydroorotate dehydrogenase inhibitor (IC50 1.2 nM). MEDS433 inhibited the in vitro replication of hCoV-OC43 and hCoV-229E, as well as of SARS-CoV-2, at low nanomolar range. Notably, the anti-SARS-CoV-2 activity of MEDS433 against SARS-CoV-2 was also observed in kidney organoids generated from human embryonic stem cells.
T61395	Mt KARI-IN-4
	Mt KARI-IN-4 (compound 5c) is a highly effective inhibitor of Mycobacterium tuberculosis ketol-acid reductoisomerase (Mtb KARI), demonstrating a Ki value of 5.48 μM. Additionally, Mt KARI-IN-4 displays inhibitory properties against Mtb H37Rv, with a minimum inhibitory concentration (MIC) of 0.78 μM. Importantly, this compound exhibits low levels of cytotoxicity, as evident from its half-maximal inhibitory concentration (IC 50 ) value of over 72 μg/mL against human embryonic kidney cells (HEK) [1...
T35553	Ganglioside GQ1b Mixture (sodium salt)
	Ganglioside GQ1b is a tetrasialoganglioside that contains two sialic acid residues linked to an inner galactose unit. It stimulates phosphorylation of several ecto-type protein kinase substrates on the surface of GOTO human neuroblastoma cells when used at a concentration of 5 nM. Ganglioside GQ1b promotes differentiation of murine embryonic stem cells (mESCs) to neuronal precursor and glial cells via activation of the ERK1/2 pathway. It also induces differentiation of murine keratinocytes throu...
T35592	SB 202190 hydrochloride
	SB 202190 hydrochloride 是一种 p38 MAPK 抑制剂，可以抑制 p38α 和 p38β2 (IC50=50/100 nM)，具有选择性和细胞渗透性。SB 202190 hydrochloride 具有抗肿瘤活性，还可以诱导人胚胎干细胞向心肌细胞分化。
T62417	MELK-8a
	MELK-8a (NVS-MELK8a) 是一种高效的、选择性的母体胚胎亮氨酸拉链激酶 (MELK) 抑制剂 (IC50: 2 nM)。MELK-8a 也能够抑制 Flt3 (ITD) (IC50: 0.18 μM)、Haspin (IC50: 0.19 μM)、PDGFRα (IC50: 0.42 μM)。其中 MELK 在调节癌细胞的细胞有丝分裂中具有重要作用。
T35922	NAADP (sodium salt)
	Nicotinic acid adenine dinucleotide phosphate (NAADP) is a secondary messenger that induces calcium mobilization. It induces calcium release from endosomes and lysosomes via two-pore channel 2 (TPC2) and TPC1, which then stimulates large-scale calcium release from granules and the endoplasmic reticulum mediated by type 1 ryanodine receptors (RyR2s), RyR3s, and inositol-(1,4,5)-triphosphate receptors (IP3Rs). NAADP induces calcium mobilization in sea urchin and starfish eggs post fertilization to...
T80514	TAT-SAMβA	PKC	Chromatin/Epigenetic; Cytoskeletal Signaling
	TAT-SAMβA为RNAENFDRF (SAMβA) 与TAT47-57蛋白衍生肽结合形成的肽类化合物，作为Mfn1-βIIPKC结合的选择性拮抗剂。该化合物能够保护小鼠胚胎成纤维细胞(MEFs)免遭氧化应激诱导的细胞毒性。
T37079	VEGFR2 Kinase Inhibitor II
	Vascular endothelial growth factor receptor 2 (VEGFR2, also known as KDR and FLK1) is a receptor tyrosine kinase that regulates angiogenesis, vascular development, and embryonic hematopoiesis in response to VEGF isoforms A, C, and D. VEGFR2 kinase inhibitor II is a reversible, cell-permeable inhibitor of VEGFR2's kinase activity (IC50 = 70 nM). It less potently inhibits the platelet-derived growth factor receptor β (PDGFRβ; IC50 = 920 nM) and related receptor and non-receptor tyrosine kinases. V...
T76052	ELA-32(human) TFA
	ELA-32(human) TFA is a potent, high affinityapelin receptoragonist (IC50=0.27 nM; Kd=0.51 nM). ELA-32(human) TFA exhibits no binding GPR15 and GPR25. ELA-32(human) TFA activates the PI3K/AKT pathway and promotes self-renewal of hESCs via cell-cycle progression and protein translation. ELA-32(human) TFA also potentiates the TGFβ pathway, priming hESCs toward the endoderm lineage. ELA-32(human) TFA stimulates angiogenesis in HUVEC cells.
T76068	Cyclo(Arg-Gly-Asp-D-Phe-Cys) TFA
	Cyclo(Arg-Gly-Asp-D-Phe-Cys) TFA 是一种环状RGD多肽，对αvβ3有高亲和性，能干扰细胞整合素之间的相互作用。此化合物能抑制胚胎干细胞(ESC)的多潜能性基因表达，并可在体内减少mESC的致瘤潜力，因此适用于肿瘤研究领域。
T36321	C6 Urea Ceramide
	C6 urea ceramide is an inhibitor of neutral ceramidase.1 It increases total ceramide levels in wild-type mouse embryonic fibroblasts (MEFs) and in HT-29 colon cancer cells but not in MEFs lacking neutral ceramidase. It inhibits proliferation of, and induces apoptosis and autophagy in HT-29, but not non-cancerous RIE-1, cells when used at concentrations of 5 and 10 μM. C6 urea ceramide decreases total β-catenin, increases phosphorylated β-catenin, and induces colocalization of β-catenin with the ...
T71618	Oxocarbazate
	Oxocarbazate, also known as CID23631927, is an inhibitor of human cathepsin L. In the cathepsin L inhibition assay, The oxocarbazate caused a time-dependent 17-fold drop in IC50 from 6.9 nM (no preincubation) to 0.4 nM (4-h preincubation). Slowly reversible inhibition was demonstrated in a dilution assay. CID23631927 demonstrate activity in blocking both SARS-CoV (IC50 = 273 nM) and Ebola virus (IC50 = 193 nM) entry into human embryonic. CID 23631927 was a subnanomolar, slow-binding, reversible...
T37669	CAY10498
	The A1, A2A, A2B, and A3 adenosine receptors (ARs) are ubiquitous G protein-coupled receptors. The four AR subtypes have been implicated in several areas of therapeutic interest such as stroke and other ischemic conditions, as well as inflammation, neurodegenerative diseases, diabetes, and sleep regulation. A3 AR antagonists are of interest as therapeutic agents in glaucoma agents and inflammation. CAY10498 is a potent and selective A3 AR antagonist exhibiting a Ki of 37 nM with 60 and 200-fold ...
T36490	AZT triphosphate TEA
	AZT triphosphate TFA (3'-Azido-3'-deoxythymidine-5'-triphosphate TFA) is a active triphosphate metabolite of Zidovudine (AZT). AZT triphosphate TFA exhibits antiretroviral activity and inhibits replication of HIV. AZT triphosphate TFA also inhibits the DNA polymerase of HBV. AZT triphosphate TFA activates the mitochondria-mediated apoptosis pathway[1][2][3]. Treatment with 100 μM Zidovudine (AZT) for 48h disrupts the mitochondrial tubular network via accumulation of AZT triphosphate (AZT-TP) in ...

化合物

Cat.No: T8987

Target: Casein Kinase

Cat.No: T16695

Target: Integrin

Phthalazinone pyrazole

Cat.No: T21981

Target: Aurora Kinase

Cat.No: T11571

Synonym: 4-Ethyl-5-methyl-5,6-dihydro-[1,3]dioxolo[4,5-j]phenanthridine

Target: Wnt/beta-catenin

Cat.No: T7196

Synonym: [4-[[5-氯-4-(甲基氨基)-2-嘧啶基]氨基]-3-甲氧基苯基]-4-吗啉基甲酮

Target: LRRK2

Cardiogenol C hydrochloride

Cat.No: T8005

Synonym: 2-[[2-[(4-甲氧基苯基)氨基]-4-嘧啶基]氨基]乙醇盐酸盐,Cardiogenol C HCl,Cardiogenol C

Target: Wnt/beta-catenin

Oct3/4-inducer-1

Cat.No: T3221

Synonym: 2-(4-(4-methoxybenzyloxy)phenyl)acetonitrile,2-(4-[(4-甲氧基苄基)氧基]苯基)乙腈

Target: Others, OCT

Cat.No: T2161

Target: Wnt/beta-catenin

Cat.No: T3162

Target: Others

Cat.No: T11469

Target: DNA Methyltransferase

Cat.No: T2019

Target: OCT

Cat.No: T2301

Synonym: FHPI,SB202190

Target: Apoptosis, p38 MAPK, Autophagy

Cat.No: T60143

Target: Apoptosis

Cat.No: T2310

Synonym: Laduviglusib,CT99021,CHIR-99021

Target: GSK-3, Wnt/beta-catenin, Autophagy

Cat.No: T28866

Target: Apoptosis

Pifithrin-β hydrobromide

Cat.No: T3637

Synonym: Cyclic PFT-α,PFT-β,Cyclic Pifithrin-α hydrobromide,Pifithrin-β,PFT β (hydrobromide)

Target: Ferroptosis, p53

Cat.No: T77697

Synonym: BML278,BML 278

Target: Sirtuin, Histone Methyltransferase

Cat.No: T2310L

Synonym: CT99021 HCl,Laduviglusib HCl

Target: GSK-3

Cat.No: T70520

Cat.No: T35549

Cat.No: T35561

Cat.No: T69743

Cat.No: T61395

Ganglioside GQ1b Mixture (sodium salt)

Cat.No: T35553

SB 202190 hydrochloride

Cat.No: T35592

Cat.No: T62417

NAADP (sodium salt)

Cat.No: T35922

Cat.No: T80514

Target: PKC

VEGFR2 Kinase Inhibitor II

Cat.No: T37079

ELA-32(human) TFA

Cat.No: T76052

Cyclo(Arg-Gly-Asp-D-Phe-Cys) TFA

Cat.No: T76068

C6 Urea Ceramide

Cat.No: T36321

Cat.No: T71618

Cat.No: T37669

AZT triphosphate TEA

Cat.No: T36490

Cat. No.	Product Name	Target	Signaling Pathways
T75661	Thymopentin acetate
	Thymopentin acetate为胸腺皮质及髓质上皮细胞主要分泌的生物活性肽，是一有效免疫调节剂，具有极短的血浆半衰期(30秒)，能促进自人类胚胎干细胞生成T细胞群。
T36954	Nemorosone
	Nemorosone is a polycyclic polyprenylated acylphloroglucinol (PPAP) originally isolated from C. rosea that has antiproliferative properties.1 Nemorosone inhibits growth of NB69, Kelly, SK-N-AS, and LAN-1 neuroblastoma cells (IC50s = 3.1-6.3 μM), including several drug-resistant clones, but not MRC-5 human embryonic fibroblasts (IC50 = >40 μM).2 It increases DNA fragmentation in LAN-1 cells in a dose-dependent manner, and decreases N-Myc protein levels and phosphorylation of ERK1/2 by MEK1/2. Nem...

天然产物

Thymopentin acetate

Cat.No: T75661

Cat.No: T36954

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