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37

抑制剂 & 化合物

10

天然产物

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Cat. No. Product Name Target Signaling Pathways
T16133 MRK-560

Gamma-secretase Neuroscience; Proteases/Proteasome; Stem Cells
MRK-560 是高效的、口服有效的 γ- 分泌酶抑制剂抑制剂,具有大脑屏障渗透性。
T9079 Apostatin-1

Apt-1

Others Others
Apostatin-1 (Apt-1) 是一种新型 TRADD 抑制剂。 Apostatin-1 可以与 TRADD 的 N 末端 TRAF2 结合域上的口袋结合。
T37558 Necrostatin-5

Nec-5

RIP kinase; Necroptosis Apoptosis; NF-κB
Necrostatin-5 (Nec-5)是一种RIP1激酶的选择性抑制剂,也是一种细胞坏死抑制剂,可防止TNF-α处理的fadd 缺陷Jurkat 细胞死亡,EC50值为240 nM。
T35569 CTA 056

Apoptosis Apoptosis
CTA 056 是白细胞介素-2 诱导的 T 细胞激酶(ITK)抑制剂,抑制小鼠 MOLT-4 异种移植肿瘤的生长,诱导 Jurkat 细胞凋亡,可用于研究自身免疫性疾病和T细胞恶性肿瘤。
T1847 Necrostatin-1

Nec-1,Necrostatin 1

Indoleamine 2,3-Dioxygenase (IDO); Ferroptosis; Autophagy; RIP kinase Apoptosis; Autophagy; Metabolism; NF-κB
Necrostatin-1 (Nec-1) 是一种坏死性凋亡抑制剂和 RIP1 抑制剂,具有特异性。Necrostatin-1 抑制 TNF-α 诱导的坏死性凋亡。Necrostatin-1 也可以抑制 IDO。
T73149 HPK1-IN-33

HPK1-IN-33(化合物21)是造血祖细胞激酶1(HPK1)的高效抑制剂,其Ki值为1.7 µM。此化合物在Jurkat WT细胞中抑制IL-2产生的EC50为286 nM,而在Jurkat HPK1 KO细胞中的EC50则大于10000 nM。
T36286 Protease-Activated Receptor-3 (PAR-3) (1-6), human

TFRGAP-amide, human PAR-3-derived tethered ligand sequence which does not activate PAR-3 but rather activates PAR-1 and PAR-2, either in Jurkat or in other PAR-expressing cells.
T12203L Necrostatin 2

Others Others
Necrostatin 2 is an effective necroptosis inhibitor. Necrostatin 2 is also a RIPK1 inhibitor. EC50 for inhibition of necroptosis in FADD-deficient Jurkat T cells treated with TNF-α is 0.05 μM.
T80497 KTX-Sp2

Potassium Channel Membrane transporter/Ion channel
KTX-Sp2为钾通道毒素,能高效阻断三种外源电压门控钾通道Kv1.1、Kv1.2和Kv1.3。该化合物还能抑制内源性Kv1.3通道,降低Jurkat T细胞内Ca2+信号并抑制其活化后的IL-2分泌。
T39342 4-Maleimidosalicylic acid

4-Maleimidosalicylic acid is a polar maleimide compound that does not exhibit suppressive effects on IL-2 production in JURKAT T cells.
T81394 PRO-HD1

HDAC Chromatin/Epigenetic; DNA Damage/DNA Repair
PRO-HD1,一种PROTAC HDAC6降解剂(IC50:5.8 μM),能够在A549细胞中降解HDAC6并在Jurkat细胞中抑制增殖(IC50:5.8 μM)。
T72586 Lck Inhibitor III

Lck Inhibitor III 是一种有效的 Lck 抑制剂,IC50为 867 nM。 Lck Inhibitor III 抑制 Jurkat 细胞中的 IL-2合成,IC50为 1.270 μM。
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。
T39913 TMX-4100

TMX-4100 is a potent degrader of phosphodiesterase 6D (PDE6D), exhibiting high degradation selectivity towards PDE6D with DC50 values below 200 nM in MOLT4, Jurkat, and MM.1S cells. This compound holds significant potential for research pertaining to multiple myeloma.
T78189 JAK-IN-26

JAK Angiogenesis; Chromatin/Epigenetic; JAK/STAT signaling; Stem Cells
JAK-IN-26(化合物2)为口服活性JAK抑制剂,展现优良药代动力学特性。该化合物有效抑制Jurkat细胞中IFN-α2B诱导的STAT3磷酸化(IC50=17.2 nM)。
T36331 Z-AEVD-FMK

Z-AEVD-FMK,Z-Ala-Glu-Val-Asp-Fluoromethyl Ketone

Z-AEVD-FMK is an irreversible inhibitor of caspase-10 and related caspases.[1] At 10 &#181M, it can prevent the initiation of Fas signaling by caspase-10 in Jurkat T lymphoma cells, preventing Bid cleavage into its active form, caspase cascade activation, and apoptosis.[2]
T40958 Milategrast

E6007

Milategrast is a chemical compound that functions as a potent cell adhesion inhibitor and cell infiltration inhibitor. In vitro studies have demonstrated its ability to effectively inhibit the adhesion of Jurkat cells to human fibronectin, with an IC50 value of less than 5 μM.
T61754 TMX-4116

TMX-4116为酪蛋白激酶1α (CK1α) 降解剂,具有显著的选择性,尤其是在MOLT4、Jurkat 和 MM.1S 细胞系中,其对CK1α的降解活性强,DC50值低于200 nM。因此,TMX-4116被用于多发性骨髓瘤相关研究。
T83947 HDAC4 CHDI Degrader 11

HDAC4 CHDI Degrader 11是一种高效且选择性的HDAC4降解剂(PROTAC),其在Jurkat E6-1细胞和Jurkat细胞中的DC50值分别为4 nM和6 nM。该化合物由类IIa HDAC抑制剂三氟甲基噁二唑通过连接体与Von Hippel-Lindau (VHL) 蛋白的配体连接而成。在亨廷顿病小鼠细胞模型中,HDAC4 CHDI Degrader 11能强效地降解HDAC4(DC50= 1nM)。在神经母细胞瘤细胞系中,可与P-糖蛋白抑制剂Elacridar联用以实现更有效的降解。
T61202 TDO-IN-1

Others Others
TDO-IN-1 是一种具有口服活性、有效性和选择性的色氨酸 2,3-双加氧酶 (TDO)抑制剂 ,对吲哚胺-2,3-双加氧酶 具有抑制作用。TDO-IN-1 具有抗肿瘤活性, 能够通过逆转肿瘤组织的局部免疫耐受来发挥作用。
T79705 LP23

PD-1/PD-L1 Apoptosis; Cell Cycle/Checkpoint; Immunology/Inflammation
LP23为非芳基甲胺类PD-1/PD-L1抑制剂(IC50:16.7 nM),展现出抗肿瘤效果。能恢复HepG2/Jurkat T细胞的免疫功能并促进HepG2细胞凋亡。在B16-F10肿瘤模型中,LP23表现出体内活性,在剂量为30 mg/kg时TGI达到88.6%。
T37276 2,5-Deoxyfructosazine (hydrochloride)

2,5-Deoxyfructosazine is a pyrazine derivative that can be found in cured tobacco and is used as a flavoring agent in the food and tobacco industry. Pyrazines, including 2,5-deoxyfructosazine, can be produced either by pyrolytic decomposition of natural compounds or by the reaction of sugars with alcoholic ammonia. 2,5-Deoxyfructosazine is also formed by the breakdown of D-glucosamine at neutral pH. Like glucosamine, 2,5-deoxyfructosazine has DNA strand breakage activity and strongly inhibits IL...
T36291 Integrin modulator 1

Integrin modulator 1 is a potent and selective α4β1 integrin agonist, with an IC50 of 9.8 nM for RGD-binding α4β1. Integrin modulator 1 increases cell adhesion mediated by α4β1 integrin, with an EC50 of 12.9 nM[1]. Integrin modulator 1 (2-10 μg/mL; 30 min) significantly increases Jurkat E6.1 cell adhesion[1].Integrin modulator 1 (1-100 nM; 1 h) strongly and significantly increases ERK1/2 phosphorylation in Jurkat E6.1 cells[1].Integrin modulator 1 (1 nM-10 μM; 30 min) significantly increases the...
T36047 LH1307

LH1307 is an inhibitor of the interaction between programmed cell death 1 (PD-1) and its ligand PD-L1 that has an IC50 value of 3 nM in a homologous time-resolved fluorescence (HTRF) assay.1 It increases the activation of Jurkat cells expressing PD-1 in co-culture with U2OS or CHO cells expressing PD-L1 (EC50s = 79 and 763 nM, respectively, in reporter assays). |1. Basu, S., Yang, J., Xu, B., et al. Design, synthesis, evaluation, and structural studies of C2-symmetric small molecule inhibitors o...
T79110 JAK-IN-27

JAK Angiogenesis; Chromatin/Epigenetic; JAK/STAT signaling; Stem Cells
JAK-IN-27(化合物1)是JAK家族激酶的口服有效抑制剂,对TYK2、JAK1和JAK3的IC50分别为3.0 nM、7.7 nM和629.6 nM。此外,JAK-IN-27能够抑制Jurkat细胞内由IFN-α2B诱导的STAT3磷酸化,其IC50为23.7 nM。
T36073 S-Acetyl-L-glutathione

S-Acetyl-L-glutathione is a derivative of glutathione .1 It increases intracellular GSH levels in primary fibroblasts derived from patients with glutathione synthetase deficiency when used at a concentration of 50 μM. S-Acetyl-L-glutathione (5 mM) induces apoptosis in Daudi, Raji, and Jurkat lymphoma cells.2 It inhibits the replication of herpes simplex virus 1 (HSV-1) in human foreskin fibroblasts when used at concentrations of 5 and 10 mM.3 S-Acetyl-L-glutathione (6.25 μg/g per day) increases ...
T36046 LH1306

LH1306 is an inhibitor of the interaction between programmed cell death 1 (PD-1) and its ligand PD-L1 that has an IC50 value of 25 nM in a homologous time-resolved fluorescence (HTRF) assay.1 It increases the activation of Jurkat cells expressing PD-1 in co-culture with U2OS or CHO cells expressing PD-L1 (EC50s = 334 and 4,214 nM, respectively, in reporter assays). |1. Basu, S., Yang, J., Xu, B., et al. Design, synthesis, evaluation, and structural studies of C2-symmetric small molecule inhibito...
T36034 CAY10774

CAY10774 is an inhibitor of the protein-protein interaction between programmed cell death 1 (PD-1) and its ligand PD-L1 (IC50= 15 nM in a homologous time-resolved fret (HTRF) assay).1It increases the activation of Jurkat cells expressing PD-1 in co-culture with artificial antigen-presenting cells (aAPCs) expressing PD-L1 (EC50= 6.6 μM in a reporter assay). CAY10774 increases surface expression of PD-1 on primary human CD4+and CD8+T cells co-cultured with aAPCs. 1.Konieczny, M., Musielak, B., Koc...
T74843 ITK degrader 1

ITKdegrader 1 是一种高度选择性的白细胞介素 2 诱导的 T 细胞激酶 (ITK) 降解剂 (DC50=3.6 nM)。ITKdegrader 1 快速、持久地诱导 ITK 降解,并抑制体内抗 CD3抗体刺激的 IL-2分泌 (EC50=35.2 nM,Jurkat 细胞)。ITKdegrader 1 也显示出良好的血浆暴露水平。
T37851 Chlorido[N,N'-disalicylidene-1,2-phenylenediamine]iron(III)

Chlorido[N,N'-disalicylidene-1,2-phenylenediamine]iron(III) is an inducer of ferroptosis.1 It induces ferroptosis, but not apoptosis or necroptosis, in NB1 cancer cells when used at a concentration of 3 μM.1 Chlorido[N,N'-disalicylidene-1,2-phenylenediamine]iron(III) inhibits proliferation of BJAB, NALM-6, Jurkat, MelHO, and MCF-7 cancer cells (IC50s = 0.07, 2.5, 1.5, 3, and 5 μM, respectively), as well as NALM-6 cells resistant to daunorubicin and vincristine when used at concentrations ranging...
T83946 CHDI 00484077

CHDI 00484077是一种强效且选择性的IIa类组蛋白去乙酰化酶(HDAC)抑制剂,其体内IC50值为10-30 nM,而在HEK293和Jurkat细胞中的IC50值分别为0.01 nM和0.04 nM。在细胞中对IIa类HDACs具有150倍的选择性,优于I/IIb类HDACs。具有口服生物可用性和中枢神经系统(CNS)穿透能力。
T35940 Darinaparsin

Dimethylarsinic glutathione,Darinaparsin

Darinaparsin is a dimethylated arsenic linked to glutathione. It is cytotoxic to DU145, LNCaP, and PC3 prostate cancer cells (IC50s = 5-10 &#181M) and patient-derived primary prostate cancer cells (IC50s = 2.5-20 &#181M), as well as Jurkat T cell lymphoma and L540 Hodgkin lymphoma cells (IC50s = 2.7 and 1.3 &#181M, respectively). [1][2] It decreases the tumor-initiating subpopulation in DU145 and PC3 cells and halts the cell cycle in the G2/M phase. Darinaparsin decreases transcription of Gli-2,...
T36659 Boromycin

Boromycin is a boron-containing macrolide antibiotic that has been found in Streptomyces. Boromycin inhibits growth of B. subtilis (MIC = 0.05 μg/ml) and induces efflux of potassium ions from B. subtilis without affecting Na+/K+-ATPase activity. It decreases the synthesis of protein, RNA, and DNA in B. subtilis when used at a concentration of 0.05 μg/ml. It inhibits the growth of B. halodurans (MIC = 10 ng/ml) and inhibits the futalosine pathway of menaquinone synthesis in B. halodurans. Boromyc...
T83763 EPI-X4 TFA

Endogenous Peptide Inhibitor of CXCR4

EPI-X4是一种源于人血清白蛋白408-423氨基酸的内源性肽段,是趋化因子(C-X-C基序)受体4 (CXCR4)的拮抗剂。在0.8至1,000µM的浓度范围内,EPI-X4能抑制表达CXCR4的HEK293细胞中由趋化因子(C-X-C基序)配体12 (CXCL12)诱发的钙离子动员和受体内化。EPI-X4还能抑制CXCL12诱导的Jurkat T细胞和人类CD34+造血干细胞的迁移。体内实验中,EPI-X4(16µmol/kg)在急性过敏性气道高嗜酸性粒细胞疾病的小鼠模型中减少了Cxcr4依赖的炎症细胞气道浸润。慢性肾脏病患者尿液中EPI-X4的水平增高,并与肾小球滤过率(GFR)成反比。
T69221 BMS-554417

BMS-554417 is a novel inhibitor of IGF-IR, which inhibits IGF-IR and insulin receptor kinase activity and proliferation in vitro, and reduces tumor xenograft size in vivo. In a series of carcinoma cell lines, the IC50 for proliferation ranged from 120 nmol/L (Colo205) to >8.5 micromol/L (OV202). BMS-554417 treatment inhibited IGF-IR and insulin receptor signaling through extracellular signal-related kinase as well as the phosphoinositide 3-kinase/Akt pathway, as evidenced by decreased Akt phosph...
T35775 HT-2 Toxin-13C22

HT-2 Toxin-13C22

HT-2 toxin-13C22is intended for use as an internal standard for the quantification of HT-2 toxin by GC- or LC-MS. HT-2 toxin is a type A trichothecene mycotoxin and an active, deacetylated metabolite of the trichothecene mycotoxin T-2 toxin .1,2Like T-2 toxin, HT-2 toxin inhibits protein synthesis and cell proliferation in plants.2HT-2 toxin also reduces viability of HepG2, A549, HEp-2, Caco-2, A-204, U937, Jurkat, and RPMI-8226 cancer cells with IC50values ranging from 3.1 to 23 ng/ml and human...
T36649 AN3661

AN3661, a potent antimalarial lead compound, targets a Plasmodium falciparum cleavage and polyadenylation specificity factor homologue subunit 3 (PfCPSF3). AN3661 inhibits Plasmodium falciparum laboratory-adapted strains, Ugandan field isolates, and murine P. berghei and P. falciparum infections[1]. AN3661 is active at nanomolar (IC50=20-56 nM) concentrations against P. falciparum laboratory strains known to be sensitive (3D7) or resistant (W2, Dd2, K1, HB3, FCR3 and TM90C2B), and AN3661 is simi...

化合物

MRK-560
Cat.No: T16133
Synonym:
Target: Gamma-secretase
Apostatin-1
Cat.No: T9079
Synonym: Apt-1
Target: Others
Necrostatin-5
Cat.No: T37558
Synonym: Nec-5
Target: RIP kinase, Necroptosis
CTA 056
Cat.No: T35569
Synonym:
Target: Apoptosis
Necrostatin-1
Cat.No: T1847
Synonym: Nec-1,Necrostatin 1
Target: Indoleamine 2,3-Dioxygenase (IDO), Ferroptosis, Autophagy, RIP kinase
HPK1-IN-33
Cat.No: T73149
Synonym:
Target:
Protease-Activated Receptor-3 (PAR-3) (1-6), human
Cat.No: T36286
Synonym:
Target:
Necrostatin 2
Cat.No: T12203L
Synonym:
Target: Others
KTX-Sp2
Cat.No: T80497
Synonym:
Target: Potassium Channel
4-Maleimidosalicylic acid
Cat.No: T39342
Synonym:
Target:
PRO-HD1
Cat.No: T81394
Synonym:
Target: HDAC
Lck Inhibitor III
Cat.No: T72586
Synonym:
Target:
(R)-MLT-985
Cat.No: T62680
Synonym:
Target:
TMX-4100
Cat.No: T39913
Synonym:
Target:
JAK-IN-26
Cat.No: T78189
Synonym:
Target: JAK
Z-AEVD-FMK
Cat.No: T36331
Synonym: Z-AEVD-FMK,Z-Ala-Glu-Val-Asp-Fluoromethyl Ketone
Target:
Milategrast
Cat.No: T40958
Synonym: E6007
Target:
TMX-4116
Cat.No: T61754
Synonym:
Target:
HDAC4 CHDI Degrader 11
Cat.No: T83947
Synonym:
Target:
TDO-IN-1
Cat.No: T61202
Synonym:
Target: Others
LP23
Cat.No: T79705
Synonym:
Target: PD-1/PD-L1
2,5-Deoxyfructosazine (hydrochloride)
Cat.No: T37276
Synonym:
Target:
Integrin modulator 1
Cat.No: T36291
Synonym:
Target:
LH1307
Cat.No: T36047
Synonym:
Target:
JAK-IN-27
Cat.No: T79110
Synonym:
Target: JAK
S-Acetyl-L-glutathione
Cat.No: T36073
Synonym:
Target:
LH1306
Cat.No: T36046
Synonym:
Target:
CAY10774
Cat.No: T36034
Synonym:
Target:
ITK degrader 1
Cat.No: T74843
Synonym:
Target:
Chlorido[N,N'-disalicylidene-1,2-phenylenediamine]iron(III)
Cat.No: T37851
Synonym:
Target:
CHDI 00484077
Cat.No: T83946
Synonym:
Target:
Darinaparsin
Cat.No: T35940
Synonym: Dimethylarsinic glutathione,Darinaparsin
Target:
Boromycin
Cat.No: T36659
Synonym:
Target:
EPI-X4 TFA
Cat.No: T83763
Synonym: Endogenous Peptide Inhibitor of CXCR4
Target:
BMS-554417
Cat.No: T69221
Synonym:
Target:
HT-2 Toxin-13C22
Cat.No: T35775
Synonym: HT-2 Toxin-13C22
Target:
AN3661
Cat.No: T36649
Synonym:
Target:
Cat. No. Product Name Target Signaling Pathways
T3884 Neoandrographolide

Neoandrographiside,新穿心莲内酯

NOS; COX Immunology/Inflammation; Neuroscience
Neoandrographolide (Neoandrographiside) 是一种二萜类化合物,从穿心莲中分离得到。
TL0013 Heraclenin

独活内酯

Anti-infection; Immunology/Inflammation related Immunology/Inflammation; Microbiology/Virology
Heraclenin 是一种天然呋喃香豆素。它浓度依赖性的靶向激活的 T 细胞核因子 (NFAT) ,抑制人原代 T 细胞中 T 细胞受体介导的增殖。
T16075 (Rac)-Idroxioleic acid

2-Hydroxyoleic acid,2-OHOA,2-羟基乳清酸,Minerval

Apoptosis Apoptosis
(Rac)-Idroxioleic acid (2-Hydroxyoleic acid) 是一种具有抗肿瘤作用的脂肪酸酰胺水解酶抑制剂。 它与质膜结合并改变脂质组织。
TN4131 Germanicol acetate

Others Others
Germanicol acetate shows some slight cytotoxic activity against Jurkat cells .
TN4266 Isobonducellin

Antifection Microbiology/Virology
Isobonducellin exhibits potent cytotoxic activity in Jurkat and HepG2 cells, while moderate growth inhibition against Colon205 cells.
T14003 15-Acetoxyscirpenol

Caspase Apoptosis; Proteases/Proteasome
15-Acetoxyscirpenol, a member of the acetoxyscirpenol moiety mycotoxins (ASMs), potently induces apoptosis and inhibits the growth of Jurkat T cells in a dose-dependent manner. This effect is mediated through the activation of caspases independent of caspase-3[1].
TN3932 ent-11alpha-Hydroxyabieta-8(14),13(15)-dien-16,12alpha-olide

Others Others
ent-11alpha-Hydroxyabieta-8(14),13(15)-dien-16,12alpha-olide shows significant cytotoxic activity against ANA-1 and Jurkat cells with IC50 values 7.12 x 10(-3) and 1.79 x 10(-2) microM.
T36961 Malformin C

Malformin C is a natural fungus-derived bicyclic pentapeptide that has antibacterial properties, particularly against species of Bacillus. Malformin C potently blocks the ability of bleomycin to induce G2 arrest in human T-cell leukemia-derived Jurkat cells (IC50 = 0.9 nM). It less potently abrogates colchicine-induced M phase arrest in Jurkat cells (IC50 = 24 nM). Malformin C inhibits cell growth dose-dependently in Colon 38 and HCT 115 cancer cells (IC50s = 0.27 and 0.18 μM, respectively) but ...
TN5880 Mesuol

Mesuol has antioxidant activity, it shows very high scavenging activity against DPPH radical; it also has immunomodulatory activity, can potentiate percentage neutrophil adhesion in neutrophil adhesion test in rats and phagocytosis in carbon clearance assay. Mesuol can suppress HIV-1 replication in Jurkat T cells, it inhibits TNFα-induced HIV-1-LTR transcriptional activity by targeting the nuclear factor-κB (NF-κB) pathway.
T35741 Gliovirin

Gliovirin is a fungal metabolite that has been found inT. harzianumand has fungicidal, antimicrobial and anti-inflammatory activities.1It is active against the plant pathogenic fungusP. ultimum(MIC = 60 ng/ml) and the parasiteT. brucei brucei(IC50= 90 ng/ml), but has no effect on the plant pathogenic fungiR. solani,P. omnivorum,T. basicola,R. arrhizus, andV. dahliaeor the bacteriaB. thuringiensis,P. fluorescens, andX. malvacearumwhen used at concentrations up to 1,000 ng/ml.2,3Gliovirin decrease...

天然产物

Neoandrographolide
Cat.No: T3884
Synonym: Neoandrographiside,新穿心莲内酯
Target: NOS, COX
Heraclenin
Cat.No: TL0013
Synonym: 独活内酯
Target: Anti-infection, Immunology/Inflammation related
(Rac)-Idroxioleic acid
Cat.No: T16075
Synonym: 2-Hydroxyoleic acid,2-OHOA,2-羟基乳清酸,Minerval
Target: Apoptosis
Germanicol acetate
Cat.No: TN4131
Synonym:
Target: Others
Isobonducellin
Cat.No: TN4266
Synonym:
Target: Antifection
15-Acetoxyscirpenol
Cat.No: T14003
Synonym:
Target: Caspase
ent-11alpha-Hydroxyabieta-8(14),13(15)-dien-16,12alpha-olide
Cat.No: TN3932
Synonym:
Target: Others
Malformin C
Cat.No: T36961
Synonym:
Target:
Mesuol
Cat.No: TN5880
Synonym:
Target:
Gliovirin
Cat.No: T35741
Synonym:
Target:
TargetMol Loading
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