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46

抑制剂 & 化合物

3

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T7378	BRD9539	Histone Methyltransferase	Chromatin/Epigenetic
	BRD9539 是一种组蛋白甲基转移酶G9a 抑制剂，IC50为 6.3 μM，还抑制PRC2活性。
T2354	UNC 0631 UNC0631	Histone Methyltransferase	Chromatin/Epigenetic
	UNC 0631 是一种有效的组蛋白甲基转移酶 G9a 抑制剂，IC50值为 4 nM。它有效降低 MDA-MB-231 细胞中 H3K9me2的水平，IC50为 25 nM。
T1923	BRD4770	Histone Methyltransferase	Chromatin/Epigenetic
	BRD4770 是组蛋白甲基转移酶G9a 抑制剂，可激活共济失调毛细血管扩张突变途径并诱导细胞衰老。它可抑制H3K9的二甲基和三甲基化，EC50为 5 µM。
T17203	UNC0224	Histone Methyltransferase	Chromatin/Epigenetic
	UNC0224 是 G9a 的特异性抑制剂，Ki 为 2.6 nM，IC50 为 15 nM。 UNC0224 还有效抑制 GLP，IC50 值为 20-58 nM。
TQ0232	UNC0646 UNC 0646	Histone Methyltransferase	Chromatin/Epigenetic
	UNC0646 是一种有效的、选择性的同源蛋白赖氨酸甲基转移酶 G9a 和 GLP 抑制剂，IC50分别为 6 和 15 nM，对 G9a/GLP 的选择性比 SETD7、SUV39H2、SETD8 和 PRMT3 高。它降低 MDA-MB-231 细胞中H3K9me2的水平，IC50为 26 nM。
T5443	JQ-1 (carboxylic acid) JQ-1 carboxylic acid	Epigenetic Reader Domain	Chromatin/Epigenetic
	JQ-1 (carboxylic acid) 是一种细胞渗透性 BRD4 抑制剂，对 BRD4(1) 和 BRD4(2) 的 IC50 分别为 77 和 33 nM。它是一种 (+)-JQ1 衍生物，可作为合成 PROTACs 的前体。
T15212	Emamectin Benzoate MK-244,甲胺基阿维菌素苯甲酸盐	Apoptosis; Reactive Oxygen Species; GABA Receptor; Parasite	Apoptosis; Immunology/Inflammation; Membrane transporter/Ion channel; Metabolism; Microbiology/Virology; Neuroscience; NF-κB
	Emamectin Benzoate (MK-244) 是口服有效的神经系统毒物，其通过结合昆虫中的 GABA 受体发挥作用。它是阿维菌素的半合成衍生物之一，具有广谱的杀虫和杀螨活性。它诱导ROS 介导的 DNA 损伤和细胞凋亡。
T3661	Citarinostat ACY241,HDAC-IN-2	HDAC	Chromatin/Epigenetic; DNA Damage/DNA Repair
	Citarinostat (ACY241) 是一种强效、选择性和口服组蛋白脱乙酰酶 (HDAC) 抑制剂，具有抗肿瘤活性，对 HDAC1、HDAC2、HDAC3、HDAC6 和 HDAC8 的 IC50分别为 35、45、46、2.6 和 137 nM。
T8955	PCNA-I1	Others	Others
	PCNA-I1 是PCNA(增殖细胞核抗原)抑制剂。它能够直接与 PCNA 三聚体结合(Kd:0.41 μM)，在体内外均表现出抗肿瘤活性。
T15784	LP99	Epigenetic Reader Domain	Chromatin/Epigenetic
	LP99 是一种表观遗传探针，可破坏 BRD7 和 BRD9 与细胞中染色质的结合。它是一种选择性的 BRD7 和 BRD9 溴结构域抑制剂，对 BRD9 的 Kd 为 99 nM。
T13974	ZL0580	Epigenetic Reader Domain; HIV Protease	Chromatin/Epigenetic; Microbiology/Virology; Proteases/Proteasome
	ZL0580 通过抑制 Tat 反式激活和转录延伸以及通过在 HIV 启动子处诱导抑制性染色质结构来诱导 HIV 抑制。
T10616	BRM/BRG1 ATP Inhibitor-1	Epigenetic Reader Domain	Chromatin/Epigenetic
	BRM/BRG1 ATP Inhibitor-1 是变构双 Brahma 同源物 (BRM)/SWI/SNF 相关的基质相关肌动蛋白依赖性调节剂，染色质亚家族 A 成员 2 和 BRG1/SMARCA4 ATP 酶活性抑制剂，IC50值低于 0.005 μM。
T3712	Mivebresib ABBV-075,米维布塞	Apoptosis; Epigenetic Reader Domain	Apoptosis; Chromatin/Epigenetic
	Mivebresib (ABBV-075) 是一种有效的，口服活性的溴结构域和末端结构域 (BET) 抑制剂，结合BRD4的Ki 值是 1.5 nM。
T27083	Crebinostat	Epigenetic Reader Domain; Histone Acetyltransferase; HDAC	Chromatin/Epigenetic; DNA Damage/DNA Repair
	Crebinostat 是一种有效的组蛋白去乙酰化酶 (HDAC) 抑制剂，对 HDAC1、HDAC2、HDAC3 和 HDAC6 有抑制作用， IC50 分别为 0.7 nM、1.0 nM、2.0 nM 和 9.3 nM。Crebinostat 可增加在体外神经元的突触蛋白 1 斑点沿树突 (synapsin-1 punctae along dendrites) 的密度。Crebinostat 可调节染色质介导的神经可塑性，增强小鼠的记忆。Crebinostat 可诱导组蛋白 H3 和组蛋白 H4 乙酰化，并增强 cAMP 反应元件结合蛋白 (CREB) 靶基因 Egr1 的表达。
T4126	CBL0137 Curaxin 137,CBLC137	NF-κB; p53	Apoptosis; NF-κB
	CBL0137 (Curaxin 137) 是一种代谢稳定的 curaxin，可激活 p53 (EC50: 0.37 μM) 并抑制 NF-κB (EC50: 0.47 μM)。它在功能上使促进染色质转录复合物 (FACT) 失活，从而驱动对 p53 和 NF-κB 的影响并促进癌细胞死亡。口服 CBL0137 在小鼠体内具有广泛的抗癌活性，可根除耐药性癌症干细胞，并增强吉西他滨在胰腺癌临床前模型中的疗效。
T22845	I-BET151 dihydrochloride I-BET 151 hydrochloride	Others	Others
	I-BET 151 dihydrochloride is a BET bromodomain inhibitor that prevents BET from recruiting to chromatin.
T13342	WDR5-IN-4 WIN site inhibitor 1	Others	Others
	WIN site inhibitor 1 is a WIN site of chromatin-associated WD repeat-containing protein 5 (WDR5) inhibitor (Kd: 0.1 nM), with anti-cancer activity.
T10810	Chromomycin A3	Others	Others
	Chromomycin A3 is an aureolic acid-type antitumor antibiotic. Chromomycin A3 has a variety of utilities as a staining agent for human sperm chromatin, autophagy inducing agent, and apoptosis inhibitor.
T73724	WDR5-IN-4 TFA
	WDR5-IN-4 TFA 是一种染色质相关 WD 重复结构域 5 蛋白 (WDR5) 的 WIN 位点抑制剂，Kd 值为 0.1 nM。WDR5-IN-4 TFA 能够从染色质中取代 WDR5，并降低相关基因的表达，引起翻译抑制和核仁应激。具有抗癌作用。
T38766	Histone H3 (1-35) Histone H3 (1-35)
	Histone H3 (1-35) is a 35-residue peptide derived from histone H3, which is a key member of the five main histones participating in the formation of chromatin within eukaryotic cells.
T39810	CEM114
	CEM114 is a potent chemical compound known as a chemical epigenetic modifier (CEM). It functions by employing CRISPR-Cas9 systems to harness endogenous chromatin machinery, thereby exerting its epigenetic modifying effects.
T13342L	WIN site inhibitor 1 TFA (2407457-36-5 free base) WIN site inhibitor 1 TFA	Others	Others
	WIN site inhibitor 1 TFA is a WIN site of chromatin-associated WD repeat-containing protein 5 (WDR5) inhibitor (Kd: 0.1 nM).
T72013	Epigenetic Multiple Ligand
	Epigenetic Multiple Ligand is a cell-permeable inhibitor of substrate processing by several chromatin-associated enzymes, including SIRT1/2, H3/SET7, H3/p300/CBP, H4/RmtA, PABP1/CARM1, and H4/PRMT1. It acts by inducing either apoptosis or granulocytic differentiation.
T35820	CAY10685
	CAY10685 is a cell-active analog of the lysine acetyltransferase inhibitor CPTH2 that contains an alkyne moiety for use in click chemistry reactions. Its ability to inhibit N-acetyltransferase 10 activity has been used to modulate chromatin organization in order to study changes in nuclear architecture associated with cancer and certain laminopathies.
T78520	CYT296	Others	Others
	CYT296是一种靶向染色质去凝集的化合物，能增强定义因子(OSKM)介导诱导多能干细胞(iPSC)的生成，并通过诱导小鼠胚胎成纤维细胞(MEFs)染色质的开放状态来促进体细胞的重编程，适用于细胞替代治疗和药物筛选的研究领域。
T71110	Nanatinostat TFA
	Nanatinostat, also known as Tractinostat, CHR-3996 and VRx-3996, is an orally bioavailable, second-generation hydroxamic acid-based inhibitor of histone deacetylase (HDAC) with potential antineoplastic activity. HDAC inhibitor CHR-3996 inhibits HDAC, resulting in an accumulation of highly acetylated histones, the induction of chromatin remodeling, and the selective transcription of tumor suppressor genes; these events may result in the inhibition of tumor cell division and the induction of tumor...
T39785	TH5427 hydrochloride
	TH5427 hydrochloride is a potent and selective inhibitor of NUDT5 with an IC50 of 29 nM. It demonstrates a remarkable 690-fold selectivity towards NUDT5 compared to MTH1. Moreover, TH5427 hydrochloride effectively inhibits progestin-dependent, PAR-derived nuclear ATP synthesis in breast cancer cells, thereby impeding chromatin remodeling, gene regulation, and ultimately suppressing proliferation.
T37584	Tryptoquivaline D
	Tryptoquivaline D is a fungal metabolite that has been found inNeosartorya siamensisand has anticancer activity.1,2It induces nuclear chromatin condensation, a marker of apoptosis, in HCT116 colon and HepG2 liver cancer cells when used at a concentration of 150 μM.1Tryptoquivaline D (1-100 μM), alone or in combination with doxorubicin , reduces the viability of A549 lung cancer cells.2
T71925	Isonanangenine B
	Isonanangenine B is a drimane sesquiterpene lactone that has been found in Aspergillus. It decreases survivin mRNA expression in a reporter assay when used at concentrations of 13.6, 18.42, and 26.31 µM. Isonanagenine B (18.42 µM) inhibits STAT3 and NF-κB binding to the survivin promoter in chromatin immunoprecipitation (ChIP) assays. It also induces apoptosis in COLO 320DM cells.
TP2257	Histone-H2A-(107-122)-Ac-OH	Others	Others
	Histone-H2A-(107-122)-Ac-OH is a peptide with the sequence Ac-Gly-Val-Leu-Pro-Asn-Ile-Gln-Ala-Val-Leu-Leu-Pro-Lys-Lys-Thr-Glu-OH, MW= 1762.1. Histone H2A is one of the five main histone proteins involved in the structure of chromatin in eukaryotic cells.
T39916	GNE-274
	GNE-274, a non-degrader compound structurally similar to GDC-0927 (an ER degrader), serves as a partial ER agonist in breast cancer cell lines without triggering ER turnover. Notably, GNE-274 enhances chromatin accessibility at ER-DNA binding sites, unlike GDC-0927. Acting as a potent inhibitor of the ER-ligand binding domain (LBD), GNE-274 exhibits potential for cancer research purposes.
T60606	Giemsa stain
	Giemsa stain 可对染色质和核膜进行染色，可用于组织学和微生物学。Giemsa stain 可用于如组织浆体、利什曼原虫和肺囊虫等疟疾及其他微生物的组织病理学检测。
T61433	HDAC1-IN-5
	HDAC1-IN-5, a potent inhibitor of HDAC1 with an IC50 value of 15 nM, also exhibits inhibitory activity towards HDAC6 with an IC50 value of 20 nM. In cancer cells, HDAC1-IN-5 enhances the acetylation of both histone H3 and α-tubulin, leading to the activation of caspase 3 and induction of apoptosis. Additionally, HDAC1-IN-5 binds with DNA, causing chromatin damage. Furthermore, it demonstrated strong inhibitory activity against tumor growth in xenograft mice. [1]
T70748	Bisthianostat
	Bisthianostat, also known as CF367 or CF367;-C, is a novel Orally Efficacious Pan-HDAC Inhibitor. Bisthianostat selectively binds to and inhibits HDACs, which inhibits deacetylation of histone proteins and leads to the accumulation of highly acetylated histones. This may result in an induction of chromatin remodeling, the inhibition of tumor oncogene transcription, and the selective transcription of tumor suppressor genes. This prevents cell division, induces cell cycle arrest and apoptosis. Thi...
T30304	BAY-850 HCl BAY-850,BAY850,BAY 850
	BAY-850 is a chemical probe for the bromine domain of Atad2A. It replaces acetylated H4 peptides from the bromine domain of Atad2. AY-850 shows superior selectivity to all other bromine domains (not hit in 10 μm Bromoscan). Full-length ATAD2 was replaced
T77973	YD23	PROTACs	PROTAC
	YD23是一种SMARCA2PROTAC，其作用机理为诱导SMARCA2蛋白的降解。鉴于SMARCA2与SMARCA4具有合成致死关系，YD23进一步能减少多个基因（包涵细胞周期以及细胞生长调控基因）增强子的染色质可及性，特别是在缺乏SMARCA4的细胞中。
T70210	FT-1101 free base
	FT-1101 is an orally bioavailable, potent and selective BET inhibitor. FT-1101 binds to the acetylated lysine recognition motifs in the bromodomain sites of BET proteins, thereby preventing the interaction between the BET proteins and acetylated histones. This disrupts chromatin remodeling and gene expression. Prevention of the expression of certain growth-promoting genes may lead to the inhibition of tumor cell growth. BET proteins, comprised of BRD2, BRD3, BRD4 and BRDT, are transcriptional r...
T36798L	SW2_110A acetate	Histone Methyltransferase	Chromatin/Epigenetic
	SW2_110A acetate 是一种选择性的，细胞渗透性的chromobox 同源蛋白CBX8抑制剂（Kd = 800 nM），结合CBX8 N 端色域(ChD)。SW2_110A acetate 对CBX8 N 有很高的亲和力，抑制CBX8与细胞染色质的关联，抑制MLL-AF9诱导的THP1白血病细胞增殖。
T37469	Sitamaquine tosylate
	Sitamaquine is an antileishmanial agent.1It is active againstL. donovani,L. infantum,L. mexicana,L. braziliensis, andL. tropica(EC50s = 9.5-19.8 μM). It inhibits mitochondrial complex II, also known as succinate dehydrogenase (SDH), in a cell-free assay when used at concentrations ranging from 10 to 200 μM.2Sitamaquine (100 μM) increases intracellular levels of reactive oxygen species (ROS) and decreases intracellular ATP levels, as well as induces phosphatidylserine externalization, chromatin f...
T37151	NVS-CECR2-1 NVS-CECR2-1
	NVS-CECR2-1 is a potent inhibitor of CECR2 (cat eye syndrome chromosome region, candidate 2), a component of chromatin complexes that regulate gene expression controlling development. It binds CECR2 with high affinity (IC50 = 0.047 μM by Alpha screen, Kd = 0.80 μM by ITC). NVS-CECR2-1 demonstrates no crossreactivity in a panel of 48 bromodomains and has no major activity in kinase, protease, and receptor panels. It shows robust activity in cells by FRAP assay, due to its slow off-rate, and has n...
T35783	Zearalenone-13C18 Zearalenone-13C18
	Zearalenone-13C18is intended for use as an internal standard for the quantification of zearalenone by GC- or LC-MS. Zearalenone is a mycotoxin that has been found inFusariumand has estrogenic activities.1It binds to human estrogen receptor α (ERα) and ERβ (IC50s = 9 and 5.8 nM, respectively).2Zearalenone induces precocious development of mammary tissues in young female pigs and prepucial enlargement in young male pigs.3Zearalenone (1.5-5 mg/kg of diet) induces hyperestrogenism in pigs. It also i...
T69963	Birabresib dihydrate
	Birabresib dihydrate was initially developed by Mitsubishi Tanabe Pharma Corporation, but then was licensed by OncoEthix, privately held biotechnology company. OTX015 is a selective bromodomains: BRD2, BRD3, and BRD4 inhibitor and inhibits their binding to AcH4. Bromodomains have an important role in the targeting of chromatin-modifying enzymes to specific sites, including methyltransferases, HATs and transcription factors and regulate diverse biological processes from cell proliferation and dif...
T78855	Anticancer agent 157	NO Synthase	Immunology/Inflammation
	Anticanceragent 157（compound 15）是一种NO抑制剂，具有抗炎和抗癌特性，IC50值为0.62 μg/mL。它能够与iNOS和caspase 8结合，进而导致核断裂和染色质浓缩，从而诱导细胞凋亡。此外，Anticanceragent 157在不同癌细胞系中展现出显著的抑制活性，对HT29结肠癌细胞的IC50为2.45 μg/mL，对Hep-G2肝癌细胞的IC50为3.25 μg/mL，以及对B16-F10鼠黑色素瘤细胞的IC50为3.84 μg/mL。
TP2182	Lamin fragment	Others	Others
	Lamin fragment has a peptide sequence of Lys-Ala-Gly-Gln-Val-Val-Thr-Ile-Trp. Lamin polypeptides have an almost complete α-helical conformation with multiple α-helical domains separated by non-α-helical linkers that are highly conserved in length and amin
T35658	3'-Deoxyuridine-5'-triphosphate trisodium
	3'-Deoxyuridine-5'-triphosphate trisodium (3'-dUTP trisodium) is a nucleotide analogue that inhibits DNA-dependent RNA polymerases I and II. 3'-Deoxyuridine-5'-triphosphate trisodium strongly and competitively inhibits the incorporations of UTP into RNA with a Ki value of 2.0 μM[1]. 3'-Deoxyuridine-5'-triphosphate (3'-dUTP) is synthesized starting from cordycepin in good yield. 3'-Deoxyuridine-5'-triphosphate strongly and competitively inhibits the incorporations of UTP into RNA by the RNA polym...
T35657	3'-Deoxyuridine-5'-triphosphate
	3'-Deoxyuridine-5'-triphosphate (3'-dUTP) is a nucleotide analogue that inhibits DNA-dependent RNA polymerases I and II. 3'-Deoxyuridine-5'-triphosphate strongly and competitively inhibits the incorporations of UTP into RNA with a Ki value of 2.0 μM[1]. 3'-Deoxyuridine-5'-triphosphate (3'-dUTP) is synthesized starting from cordycepin in good yield. 3'-Deoxyuridine-5'-triphosphate strongly and competitively inhibits the incorporations of UTP into RNA by the RNA polymerases. 3'-Deoxyuridine-5'-tri...

化合物

Cat.No: T7378

Target: Histone Methyltransferase

Cat.No: T2354

Synonym: UNC0631

Target: Histone Methyltransferase

Cat.No: T1923

Target: Histone Methyltransferase

Cat.No: T17203

Target: Histone Methyltransferase

Cat.No: TQ0232

Synonym: UNC 0646

Target: Histone Methyltransferase

JQ-1 (carboxylic acid)

Cat.No: T5443

Synonym: JQ-1 carboxylic acid

Target: Epigenetic Reader Domain

Emamectin Benzoate

Cat.No: T15212

Synonym: MK-244,甲胺基阿维菌素苯甲酸盐

Target: Apoptosis, Reactive Oxygen Species, GABA Receptor, Parasite

Cat.No: T3661

Synonym: ACY241,HDAC-IN-2

Target: HDAC

Cat.No: T8955

Target: Others

Cat.No: T15784

Target: Epigenetic Reader Domain

Cat.No: T13974

Target: Epigenetic Reader Domain, HIV Protease

BRM/BRG1 ATP Inhibitor-1

Cat.No: T10616

Target: Epigenetic Reader Domain

Cat.No: T3712

Synonym: ABBV-075,米维布塞

Target: Apoptosis, Epigenetic Reader Domain

Cat.No: T27083

Target: Epigenetic Reader Domain, Histone Acetyltransferase, HDAC

Cat.No: T4126

Synonym: Curaxin 137,CBLC137

Target: NF-κB, p53

I-BET151 dihydrochloride

Cat.No: T22845

Synonym: I-BET 151 hydrochloride

Target: Others

Cat.No: T13342

Synonym: WIN site inhibitor 1

Target: Others

Cat.No: T10810

Target: Others

Cat.No: T73724

Histone H3 (1-35)

Cat.No: T38766

Synonym: Histone H3 (1-35)

Cat.No: T39810

WIN site inhibitor 1 TFA (2407457-36-5 free base)

Cat.No: T13342L

Synonym: WIN site inhibitor 1 TFA

Target: Others

Epigenetic Multiple Ligand

Cat.No: T72013

Cat.No: T35820

Cat.No: T78520

Target: Others

Nanatinostat TFA

Cat.No: T71110

TH5427 hydrochloride

Cat.No: T39785

Tryptoquivaline D

Cat.No: T37584

Isonanangenine B

Cat.No: T71925

Histone-H2A-(107-122)-Ac-OH

Cat.No: TP2257

Target: Others

Cat.No: T39916

Cat.No: T60606

Cat.No: T61433

Cat.No: T70748

Cat.No: T30304

Synonym: BAY-850,BAY850,BAY 850

Cat.No: T77973

Target: PROTACs

FT-1101 free base

Cat.No: T70210

SW2_110A acetate

Cat.No: T36798L

Target: Histone Methyltransferase

Sitamaquine tosylate

Cat.No: T37469

Cat.No: T37151

Synonym: NVS-CECR2-1

Zearalenone-13C18

Cat.No: T35783

Synonym: Zearalenone-13C18

Birabresib dihydrate

Cat.No: T69963

Anticancer agent 157

Cat.No: T78855

Target: NO Synthase

Cat.No: TP2182

Target: Others

3'-Deoxyuridine-5'-triphosphate trisodium

Cat.No: T35658

3'-Deoxyuridine-5'-triphosphate

Cat.No: T35657

Cat. No.	Product Name	Target	Signaling Pathways
T6270	Trichostatin A 曲古柳菌素A,曲古抑菌素A,TSA	HDAC	Chromatin/Epigenetic; DNA Damage/DNA Repair
	Trichostatin A (TSA) 属于二烯异羟肟酸类的天然衍生物。Trichostatin A 是一种组蛋白去乙酰化酶抑制剂 (IC50=1.8 nM)，具有可逆性和特异性。Trichostatin A 导致核心组蛋白过度乙酰化，从而调节染色质结构。
T40834	5-Hydroxymethyl-2'-deoxycytidine 5hmdC,2'-脱氧-5-(羟甲基)胞啶	PARP	Chromatin/Epigenetic; DNA Damage/DNA Repair
	5-Hydroxymethyl-2'-deoxycytidine 是 DNA 中 5-methyl-2'-deoxycytidine (5-mdC) 的氧化衍生物，引起DNA损伤反应，染色体畸变，复制叉损伤和细胞活力丧失。5-Hydroxymethyl-2’-deoxycytidine 复制叉不稳定性与染色质上聚（ADP-核糖）聚合酶1（PARP1）的存在有关。
T6S2391	L-Chicoric Acid (-)-Chicoric acid,trans-Caffeoyltartaric acid,Chicoric acid,L-菊苣酸,dicaffeoyltartaric acid,菊苣酸	Others; HIV Protease	Microbiology/Virology; Others; Proteases/Proteasome
	L-Chicoric Acid (trans-Caffeoyltartaric acid) 是一种二咖啡酰酒石酸，是一种选择性可逆的 HIV-1 整合酶抑制剂，IC50约为 100 nM。它还可抑制 HIV-1 复制。

天然产物

Cat.No: T6270

Synonym: 曲古柳菌素A,曲古抑菌素A,TSA

Target: HDAC

5-Hydroxymethyl-2'-deoxycytidine

Cat.No: T40834

Synonym: 5hmdC,2'-脱氧-5-(羟甲基)胞啶

Target: PARP

L-Chicoric Acid

Cat.No: T6S2391

Synonym: (-)-Chicoric acid,trans-Caffeoyltartaric acid,Chicoric acid,L-菊苣酸,dicaffeoyltartaric acid,菊苣酸

Target: Others, HIV Protease

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