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抑制剂 & 化合物

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Cat. No.	Product Name	Target	Signaling Pathways
T15371	Gardiquimod	TLR; HIV Protease	Immunology/Inflammation; Microbiology/Virology; Proteases/Proteasome
	Gardiquimod 可抑制巨噬细胞和活化的外周血单个核细胞的HIV-1感染。它是一种咪唑喹啉类似物，是一种 TLR7/8 激动剂。
T11465	Lenacapavir GS-6207	Others; HIV Protease	Microbiology/Virology; Others; Proteases/Proteasome
	Lenacapavir (GS-6207) 是一种有效的靶向衣壳的 HIV 复制抑制剂。 Lenacapavir 在 MT-4 细胞中显示出抗 HIV 活性，EC50 为 100 pM。
T12079	ML604440	Proteasome	Proteases/Proteasome; Ubiquitination
	ML604440 是一种特异性的、有效的、细胞可渗透的蛋白酶体 β1i (LMP2) 亚基抑制剂，能够破坏 MHC I 类细胞表面表达，IL-6 分泌以及 naïve T helper 向 17 T helper 细胞的分化。它可以改善实验性结肠炎和 EAE 疾病。
T2384	Pomalidomide CC-4047,泊马度胺	Apoptosis; TNF; Ligand for E3 Ligase; Molecular Glues	Apoptosis; PROTAC
	Pomalidomide (CC-4047) 是一种抗血管生成剂和免疫调节剂，以分子胶的方式作用。它与 E3 连接酶 cereblon 相互作用，诱导必需的 Ikaros 转录因子的降解。
TQ0174	Mavorixafor AMD-070	CXCR	Autophagy; GPCR/G Protein; Immunology/Inflammation
	Mavorixafor (AMD-070) 是一种有效的特异性 CXCR4 拮抗剂，对 CXCR4 125I-SDF 结合的 IC50 值为 13 nM。 Mavorixafor 在 MT-4 细胞 (IC50 = 1 nM) 和 PBMC (IC50 = 9 nM) 中抑制 T-tropic HIV-1 (NL4.3 株) 的复制。
T37292	M62812	TLR	Immunology/Inflammation
	M62812是一种 TLR4抑制剂，可在 HEK239细胞中抑制 LPS 诱导的NF-κB 活化。
T8311	Obefazimod ABX-464,ABX464	HIV Protease	Microbiology/Virology; Proteases/Proteasome
	Obefazimod (ABX-464) 是一种抗HIV 剂。它抑制受刺激的外周血单核细胞中的 HIV-1 复制，IC50值为 0.1 μM 至 0.5 μM。
T28946	Tenofovir exalidex Tenofovir,HDP-Tenofovir,CMX-157,CMX157,CMX 157	Antiviral	Immunology/Inflammation
	Tenofovir exalidex (CMX 157) 是一种非环核苷酸类似物 Tenofovir 的脂质结合物，对野生型和抗逆转录病毒耐药的 HIV 毒株，包括多药核苷/核苷酸类似物耐药病毒，都有活性。Tenofovir exalidex 对人外周血单个核细胞中所有主要的HIV-1和HIV-2亚型以及单核细胞来源的巨噬细胞中所有 HIV-1 菌株具有活性，EC50 范围在 0.2 和 7.2 nM 之间。Tenofovir exalidex 具有口服活性，无明显毒性。Tenofovir exalidex 对 HBV 也有活性。
T11035	diABZI STING agonist-1 (Tautomerism) diABZI STING agonist (Compound 3)	STING	Immunology/Inflammation
	diABZI STING agonist-1 (Tautomerism) (diABZI STING agonist (Compound 3)) 是一个选择性的干扰素基因刺激受体 (STING) 的激动剂，其在人和小鼠中的 EC50 值分别为 130 nM 和 186 nM。。
T27967	M199
	M199, a novel inhibitor of TLR3/9 activation, induces secretion of IL-6, IL-8 and TNFalpha in human PBMCs.
T10296	Mavorixafor trihydrochloride AMD-070 trihydrochloride	HIV Protease	Microbiology/Virology; Proteases/Proteasome
	Mavorixafor trihydrochloride is a selective and orally available CXCR4 antagonist (IC50: 13 nM against CXCR4 125I-SDF binding) and also inhibits the replication of T-tropic HIV-1 (NL4.3 strain) in MT-4 cells and PBMCs (IC50s: 1 and 9 nM).
T27030	CK176 HIV-1 inhibitor-34,HIV-1 inhibitor 34,CK 176,CK-176,HIV-1 inhibitor34
	CK176 is a capsid targeted inhibitor of HIV-1 replication. CK176 shows an 11-fold improvement over I-XW-053 in blocking HIV-1 replication in primary human peripheral blood mononuclear cells (PBMCs).
T74062	PROTAC IRAK4 degrader-2
	PROTACIRAK4 degrader-2 (Compound 9) 是一种 PROTACIRAK4降解剂，在外周血单个核细胞 (PBMC) 中，降解 IRAK4，DC50为 151 nM。PROTACIRAK4 Degrader-2 在 PBMC 细胞中诱导 IRAK4蛋白水平降低，DC50为 36 nM。PROTACIRAK4 degrader-2 还抑制 PBMC 中多种细胞因子释放。
T77851	INX-SM-6
	INX-SM-6适用于靶向输送抗炎药物。它能在PBMCS细胞中抑制LPS引发的IL-1β产生。
T71009	Dolutegravir SR Isomer
	Dolutegravir SR Isomer is an isomeric derivative of Dolutegravir -- a second generation HIV-1 integrase strand transfer inhibitor. Dolutegravir has been shown to potently inhibit HIV replication in cells such as peripheral blood mononuclear cells (PBMCs), MT-4 cells and CIP4 cells infected with a self-inactivating PHIV lentiviral vector.
TQ0297	Cenicriviroc TAK-652,TBR-652	HIV Protease; CCR	Immunology/Inflammation; Microbiology/Virology; Proteases/Proteasome
	Cenicriviroc (TAK-652) 是一种可口服的CCR2/CCR5拮抗剂，可抑制 HIV-1 和 HIV-2，具有抗炎、抗感染作用。
T70881	Dolutegravir RR Isomer
	Dolutegravir RR Isomer is an isomer of Dolutegravir -- a second generation HIV-1 integrase strand transfer inhibitor. Dolutegravir has been shown to potently inhibit HIV replication in cells such as peripheral blood mononuclear cells (PBMCs), MT-4 cells and CIP4 cells infected with a self-inactivating PHIV lentiviral vector.
T74915	ODN D-SL03
	ODN D-SL03是C类CpG寡核苷酸，能诱导PBMCs产生高水平IFN-α，激活人B细胞、NK细胞和单个核细胞，同时上调PBMCs亚群表面CD80、CD86和HLA-DR的表达，还能抑制肿瘤生长。ODN D-SL03序列：5'-tcgcgaacgttcgccgcgttcgaacgcgg-3'。
T5499	gardiquimod TFA salt
	Gardiquimod diTFA，咪唑啉类似物TLR7/8激动剂，可特异性抑制巨噬细胞和活化外周血单个核细胞(PBMCs)的HIV-1感染。在浓度低于10 μM时，该化合物特异性激活TLR7。
T36885	BMSpep-57 hydrochloride
	BMSpep-57 hydrochloride, a potent macrocyclic peptide, competitively inhibits PD-1/PD-L1 interaction, exhibiting an IC50 value of 7.68 nM. It binds to PD-L1 with dissociation constants (Kds) of 19 nM and 19.88 nM as determined by MST and SPR assays, respectively. This compound enhances T cell functionality by promoting IL-2 production in PBMCs[1].
T63329	PD-1/PD-L1-IN-25
	PD-1/PD-L1-IN-25 是一种 PD-1/PD-L1 互作的抑制剂 (IC50: 16.17 nM)，可有效激活 PBMCs 中 T 细胞的抗肿瘤免疫。PD-1/PD-L1-IN-25 能够用于研究癌症。
T83698	Cathelicidin-2 (128-153) (chicken) TFA Fowlicidin-2 (128-153),CATH-2 (128-153),Myeloid Antimicrobial Peptide 27 (128-153)
	Cathelicidin-2 (CATH-2) (128-153) 是一种合成抗菌肽，对应于鸡CATH-2的128至153个氨基酸。该化合物对E. coli、S. aureus、S. enteritidis和B. globigii展示出浓度依赖性的活性。CATH-2 (128-153) (40 µM) 可诱导孤立的鸡红细胞溶解，但对孤立的人外周血单个核细胞(PBMCs)无细胞毒性。它能促进化学因子(C-C-基序)配体2 (CCL2)的产生，并抑制LPS诱导的TNF-α、IL-6、IL-8和IL-10在孤立的人PBMCs中的产生。
T63088	NOD2 antagonist 1
	NOD2 antagonist 1 (compound 32) 是一种有效的、选择性的 NOD2 拮抗剂 (IC50: 5.23 μM)。NOD2 antagonist 1 在 THP-1 细胞，对 Muramyl dipeptide (MDP) 诱导的 IL-8 分泌表现出抑制作用。NOD2 antagonist 1 在 PBMCs 细胞，可以抑制 MDP 诱导的 IL-6、IL-10 和 TNF-α 的水平升高。
T79151	TLR8 agonist 6
	TLR8 agonist6 (Compound A)，具有EC50值为0.052 μM的TLR8激动特性，能够以EC50为0.031 μM的效力促进人PBMC中的IL-12p40生成。适用于抗病毒、抗感染、自身免疫和肿瘤相关研究领域。
T83846	HOXB7 (8-25) TFA Homeobox B7 (8-25)
	HOXB7 (8-25) 是 homeobox B7 (HOXB7) 的肽段，是细胞增殖的主要调控因子和肿瘤基因途径的激活剂。通过 HOXB7 (8-25) 肽脉冲的树突状细胞展示抗原，这些树突状细胞来源于分离的人类外周血单核细胞（PBMCs），刺激CD4+辅助T细胞的激活和IFN-γ的产生，从而引发特异性和多向性肿瘤反应性的抗肿瘤反应。
T39106	BMSpep-57
	BMSpep-57, a potent macrocyclic peptide inhibitor, competitively disrupts the PD-1/PD-L1 interaction, demonstrating a significant inhibitory concentration (IC50) of 7.68 nM. It exhibits binding affinity towards PD-L1 with dissociation constants (Kd) of 19 nM and 19.88 nM in MicroScale Thermophoresis (MST) and Surface Plasmon Resonance (SPR) assays, respectively. This compound enhances T cell functionality by promoting Interleukin-2 (IL-2) production within Peripheral Blood Mononuclear Cells (PBM...
T78755	PD-1/PD-L1-IN-31	PD-1/PD-L1	Apoptosis; Cell Cycle/Checkpoint; Immunology/Inflammation
	PD-1/PD-L1-IN-31为具高效PD-1/PD-L1抑制能力的化合物（IC50=2.2 nM），能激进IFN-γ分泌及激活外周血单核细胞（PBMC），进而抑制肿瘤细胞生长。
T74990	ICeD-2
	ICeD-2 是一种细胞死亡诱导剂，可诱导HIV-1感染的细胞死亡。 ICeD-2 介导的HIV-1感染细胞杀伤依赖于HIV-1蛋白酶活性。ICeD-2 可有效阻断二肽基肽酶DPP8和DPP9对 Gly-Pro-AMC 的水解。ICeD-2 显示 PBMC 中 DPP9 的强稳定性。
T69009	Gnidimacrin
	Gnidimacrin activated HIV-1 replication and killed persistently-infected cells at picomolar concentrations. In addition to its potential to purge HIV-1 from latently infected cells, gnidimacrin potently inhibited a panel of HIV-1 R5 virus infection of peripheral blood mononuclear cells (PBMCs) at an average concentration lower than 10 pM. These results suggest that gnidimacrin could activate latent HIV-1, specifically kill HIV-1 persistently infected cells, and inhibit R5 viruses at picomolar c...
T35929	O-Demethyl Apremilast
	O-Demethyl apremilast is an active metabolite of the phosphodiesterase 4 (PDE4) inhibitor apremilast .1It inhibits the activity of PDE4 isolated from U937 cells and LPS-induced TNF-α production in isolated human peripheral blood mononuclear cells (PBMCs; IC50s = 8.3 and 5.6 μM, respectively). O-Demethyl apremilast is also an oxidative degradation product of apremilast.2,3 1.Hoffmann, M., Kumar, G., Schafer, P., et al.Disposition, metabolism and mass balance of [14C]apremilast following oral admi...
T82254	GSK-LSD1	Histone Demethylase	Chromatin/Epigenetic
	GSK-LSD1是一种LSD1抑制剂，能够降低肥胖小鼠模型的摄食量和体重，同时提升胰岛素敏感性与血糖控制。此外，GSK-LSD1对NAFLD也有改善作用，并能抑制COVID-19患者PBMC中SARS-CoV-2诱导的细胞因子释放。GSK-LSD1对抑制癌症的生长与转移也显示出潜在效果。
T81181	sEH/FLAP-IN-1	FLAP	Immunology/Inflammation
	sEH/FLAP-IN-1（Compound 46A）是一sEH/FLAP抑制剂，具有阻断SACM刺激PBMC中5-LOX产物形成的活性（EC50: 11 nM），并能抑制sEH活性（EC50: 18 nM）及血栓素产生。该化合物适用于炎症性疾病研究领域。
T11693L	IT1t dihydrochloride	CXCR	Autophagy; GPCR/G Protein; Immunology/Inflammation
	IT1t dihydrochloride 抑制 CXCL12/CXCR4 相互作用，IC50 为 2.1 nM。 IT1t dihydrochloride 是 CXCR4 的拮抗剂。
T37523	Tenofovir diphosphate (sodium salt)
	Tenofovir diphosphate is an inhibitor of HIV reverse transcriptase (Kis = 0.022 and 1.55 μM for RNA and DNA, respectively) and hepatitis B virus (HBV) polymerase (Ki = 0.18 μM). It is selective for these enzymes over DNA polymerase α and β, as well as mitochondrial DNA polymerase γ (Kis = 5.2, 81.7, and 59.5 μM, respectively). Tenofovir diphosphate is formed intracellularly through phosphorylation of the prodrugs tenofovir and tenofovir disoproxil by nucleotide kinases. Increased levels of tenof...
T81314	Rademikibart CBP-201
	Rademikibart (CBP-201) 是一款针对IL-4Rα的人源化单克隆抗体，其与人IL-4Rα的结合亲和力KD值为20.7 pM。该抗体不与其他物种的IL-4Rα发生交互作用。Rademikibart 能够抑制PBMC中IL-4及IL-13介导的STAT6信号通路、TF-1细胞的增殖以及TARC的产生，显示出其在中到重度Th2型炎症性疾病研究中的应用潜力。
T83852	EGFRvIII Peptide TFA PEGFRvIII (9-mer),Epidermal Growth Factor Receptor Variant III Peptide
	EGFRvIII peptide是一种合成肽，对应于特异性肿瘤、具有持续激活性的EGFR变体EGFRvIII的融合接头，该变体缺少野生型EGFR的第6至273个氨基酸。在25 µg/ml的浓度下，它能与MHC I类亚型HLA-A0201阳性的T2细胞结合。在用于分离的人外周血单个核细胞（PBMCs*）衍生的树突状细胞中，EGFRvIII peptide可诱导抗原呈递，进而刺激CD8+细胞毒性T淋巴细胞的激活和IFN-γ产生。与toll样受体5（TLR5）激动剂鞭毛蛋白B共同免疫EGFRvIII peptide（15 µg/动物），在正交GL261胶质母细胞瘤小鼠异种移植模型中，增加了CD8+ T细胞数量，减少了调节性T细胞（Tregs）数量，减少了肿瘤体积，并提高了生存率。
T36862	Ganglioside GT1b Mixture (sodium salt) Ganglioside GT1b Mixture (sodium salt),Ganglioside G1 Mixture
	Ganglioside GT1b is a trisialoganglioside that is characterized by having two sialic residues linked to the inner galactose unit. It binds to the neurotoxins botulinum toxin serotype A (BTxA), BTxA heavy chain, and tetanus toxin with IC50 values of 11, 0.74, and 7.2 μM, respectively.[1] Ganglioside GT1b-containing liposomes bind to the major coat protein VP1 from Merkel cell polyomavirus (MCPyV), which has been identified in Merkel cell carcinomas, identifying ganglioside GT1b as a putative MCP...
T36461	CAY10748 CAY10748
	CAY10748 is an agonist of stimulator of interferon genes (STING; IC50= 0.3794 μM in a competition binding assay).1It activates STING in STING-expressing, but not STING knockout, THP-1 cells (EC50s = 0.287 and >100 μM, respectively, in a reporter assay). It induces phosphorylation of STING at the serine in position 366, as well as phosphorylation of TBK1 and IFN regulatory factor 3 (IRF3), indicating activation of the STING-TBK1-IRF3 signaling pathway. CAY10748 increases the secretion of IFN-β an...
T35672	SMU127
	SMU127 is an agonist of the toll-like receptor 1/2 (TLR1/2) heterodimer.1It induces NF-κB signaling in cells expressing human TLR2 (EC50= 0.55 μM) but not cells expressing human TLR3, -4, -5, -7, or -8 when used at concentrations ranging from 0.1 to 100 μM. SMU127 induces the production of TNF-α in isolated human peripheral blood mononuclear cells (PBMCs) when used at concentrations ranging from 0.01 to 1 μM.In vivo, SMU127 (0.1 mg/animal) reduces tumor volume in a 4T1 murine mammary carcinoma m...
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...
T7499	TAK-779 Takeda 779	HIV Protease; CXCR; CCR	Autophagy; GPCR/G Protein; Immunology/Inflammation; Microbiology/Virology; Proteases/Proteasome
	TAK-779 (Takeda 779) 是一种非肽类CCR5和CXCR3 拮抗剂，对CCR5的Ki 值为 1.1 nM，并选择性抑制R5 HIV-1。
T35829	CC-90005
	CC-90005 is a potent, selective and orally active inhibitor of protein kinase C-θ (PKC-θ), with an IC50 of 8 nM. CC-90005 shows selectivity for PKC-θ over PKC-δ (IC50=4440 nM). CC-90005 can inhibit T cell activation by IL-2 expression[1]. CC-90005 shows the exquisite selectivity of CC-90005, with IC50s for all other family members of >3 μM[1].CC-90005 is a moderate inhibitor of both CYP2C9 (IC50=8 μM) and CYP2C19 (IC50=5.9 μM) in human liver microsomes[1].CC-90005 inhibits IL-2 expression in LRS...
T16973	TAK-220	HIV Protease	Microbiology/Virology; Proteases/Proteasome
	TAK-220 is a selective and orally bioavailable CCR5 antagonist (IC50s: 3.5 nM and 1.4 nM for inhibition on the binding of RANTES and MIP-1α to CCR5, respectively).
T36629	Givinostat
	Givinostat (ITF-2357) is a HDAC inhibitor with an IC50 of 198 and 157 nM for HDAC1 and HDAC3, respectively. Givinostat (ITF2357) suppresses total LPS-induced IL-1β production robustly compared with the reduction by ITF3056. At 25, 50, and 100 nM, Givinostat reduced IL-1β secretion more than 70%. Givinostat (ITF-2357) suppresses the production of IL-6 in PBMCs stimulated with TLR agonists as well as the combination of IL-12 plus IL-18. IL-6 secretion decreases to 50% at 50 nM Givinostat, but at 1...
T10756	Cenicriviroc Mesylate TBR-652 Mesylate,TAK-652 Mesylate	CCR	Immunology/Inflammation; Microbiology/Virology
	Cenicriviroc Mesylate is a dual CCR2/CCR5 antagonist, also inhibits both HIV-1 and HIV-2 with anti-inflammatory and antiinfective activity.
T11693	IT1t	Others	Others
	IT1t inhibits CXCL12/CXCR4 interaction with an IC50 of 2.1 nM. is a potent CXCR4 antagonist.

化合物

Cat.No: T15371

Target: TLR, HIV Protease

Cat.No: T11465

Synonym: GS-6207

Target: Others, HIV Protease

Cat.No: T12079

Target: Proteasome

Cat.No: T2384

Synonym: CC-4047,泊马度胺

Target: Apoptosis, TNF, Ligand for E3 Ligase, Molecular Glues

Cat.No: TQ0174

Synonym: AMD-070

Target: CXCR

Cat.No: T37292

Target: TLR

Cat.No: T8311

Synonym: ABX-464,ABX464

Target: HIV Protease

Tenofovir exalidex

Cat.No: T28946

Synonym: Tenofovir,HDP-Tenofovir,CMX-157,CMX157,CMX 157

Target: Antiviral

diABZI STING agonist-1 (Tautomerism)

Cat.No: T11035

Synonym: diABZI STING agonist (Compound 3)

Target: STING

Cat.No: T27967

Mavorixafor trihydrochloride

Cat.No: T10296

Synonym: AMD-070 trihydrochloride

Target: HIV Protease

Cat.No: T27030

Synonym: HIV-1 inhibitor-34,HIV-1 inhibitor 34,CK 176,CK-176,HIV-1 inhibitor34

PROTAC IRAK4 degrader-2

Cat.No: T74062

Cat.No: T77851

Dolutegravir SR Isomer

Cat.No: T71009

Cat.No: TQ0297

Synonym: TAK-652,TBR-652

Target: HIV Protease, CCR

Dolutegravir RR Isomer

Cat.No: T70881

Cat.No: T74915

gardiquimod TFA salt

Cat.No: T5499

BMSpep-57 hydrochloride

Cat.No: T36885

PD-1/PD-L1-IN-25

Cat.No: T63329

Cathelicidin-2 (128-153) (chicken) TFA

Cat.No: T83698

Synonym: Fowlicidin-2 (128-153),CATH-2 (128-153),Myeloid Antimicrobial Peptide 27 (128-153)

NOD2 antagonist 1

Cat.No: T63088

Cat.No: T79151

HOXB7 (8-25) TFA

Cat.No: T83846

Synonym: Homeobox B7 (8-25)

Cat.No: T39106

PD-1/PD-L1-IN-31

Cat.No: T78755

Target: PD-1/PD-L1

Cat.No: T74990

Cat.No: T69009

O-Demethyl Apremilast

Cat.No: T35929

Cat.No: T82254

Target: Histone Demethylase

Cat.No: T81181

Target: FLAP

IT1t dihydrochloride

Cat.No: T11693L

Target: CXCR

Tenofovir diphosphate (sodium salt)

Cat.No: T37523

Cat.No: T81314

Synonym: CBP-201

EGFRvIII Peptide TFA

Cat.No: T83852

Synonym: PEGFRvIII (9-mer),Epidermal Growth Factor Receptor Variant III Peptide

Ganglioside GT1b Mixture (sodium salt)

Cat.No: T36862

Synonym: Ganglioside GT1b Mixture (sodium salt),Ganglioside G1 Mixture

Cat.No: T36461

Synonym: CAY10748

Cat.No: T35672

Cat.No: T36659

Cat.No: T7499

Synonym: Takeda 779

Target: HIV Protease, CXCR, CCR

Cat.No: T35829

Cat.No: T16973

Target: HIV Protease

Cat.No: T36629

Cenicriviroc Mesylate

Cat.No: T10756

Synonym: TBR-652 Mesylate,TAK-652 Mesylate

Target: CCR

Cat.No: T11693

Target: Others

Cat. No.	Product Name	Target	Signaling Pathways
TN6054	Norglaucine hydrochloride
	(+)-Norglaucine shows cytotoxic activity toward the tumor cell lines B16-F10 (mouse melanoma), HepG2 (human hepatocellular carcinoma), K562 (human chronic myelocytic leukemia) and HL-60 (human promyelocytic leukemia) and non-tumor peripheral blood mononuc

天然产物

Norglaucine hydrochloride

Cat.No: TN6054

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