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39

抑制剂 & 化合物

5

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T70030	SPR-00305
	SPR-00305 is a novel potent inhibitor of the mvfr pathway
T70679	Spr 210
	Spr 210 is an aldose reductase (AR) inhibitor with potential uses as a therapeutic agent for preventing and improving some diabetic complications.
T16924	SPR inhibitor 3 SPRi3	Others	Others
	SPR inhibitor 3 is an effective sepiapterin reductase inhibitor. SPR inhibitor 3 decreases neuropathic and inflammatory pain through a reduction of BH4 levels. SPR inhibitor 3 shows a high binding affinity to human SPR in a cell-free assay (IC50=74 nM) an
T39983	SPR206 acetate
	SPR206 acetate is a polymyxin analog that exhibits antibiotic activity against Gram-negative pathogens, including multidrug-resistant (MDR) variants. By interacting with the outer membrane of the bacterium, SPR206 acetate effectively combats bacterial infections. Notably, SPR206 acetate demonstrates significant efficacy with minimum inhibitory concentration (MIC) values of 0.125 mg/L against Pseudomonas aeruginosa Pa14 and Acinetobacter baumannii NCTC13301.
T12992	SPR741 acetate SPR741 acetate,NAB741 acetate,SPR741 acetate (1179330-52-9 free base)	Antibacterial	Microbiology/Virology
	SPR741 acetate 是衍生自多粘菌素 B 的阳离子肽，通过增加革兰氏阴性细菌外膜的通透性来抑制严重的革兰氏阴性细菌感从而展现出对革兰氏阴性菌的抗菌活性。SPR741 acetate 常与抗生素联合使用来治疗一些疾病。
T12991	SPR206	Others	Others
	SPR206 is a polymyxin analogue and an important class of antibiotic for the treatment of bacterial infections due to multidrug resistant Gram-negative pathogen.
T4340	SPI-112	Phosphatase	Metabolism
	SPI 112 是一种选择性的、有效的、竞争性的SHP2 (PTPN11)抑制剂，对SHP2，蛋白酪氨酸磷酸酶 (PTP) 和 PTP1B 的IC50分别为 1 μM，18.3 μM 和 14.5 μM。
TP1090	SPR741 NAB741
	SPR741, formerly NAB741 (12), is a cationic peptide derived from polymyxin B and is one such potentiator molecule that is under development for the treatment of serious Gram-negative bacterial infections.
T13326	SPR719 VXc-486	Others	Others
	SPR719 is an inhibitor of gyrase B, has bactericidal activity.
T38801	Fobrepodacin SPR720,pVXc-486
	Fobrepodacin (SPR720) is an orally active and potent phosphate prodrug of SPR719 (VXc-486). Fobrepodacin has potent bactericidal activities in vivo.
T70790	Pateamine A
	Pateamine A is a marine macrolide that is isolated from the sponge Mycale hentscheli and exhibits anticancer and antiviral properties. It has a role as a marine metabolite, an antiviral agent, an antineoplastic agent, and a eukaryotic initiation factor 4F inhibitor. It is a macrolide, a member of 1,3-thiazoles, a tertiary amino compound, a primary amino compound, and an olefinic compound. Pateamine A an inhibitor of eukaryotic translation.
T70029	Ibrexafungerp citrate
	Ibrexafungerp citrate is a triterpenoid antifungal. Similarly to echinocandins, it inhibits the synthesis of 1,3-β-d-glucan. However, it binds to a different site on the enzyme than echinocandins, resulting in limited cross-resistance. Ibrexafungerp exerts concentration-dependent fungicidal activity against Candida species and retains in vitro activity against most fluconazole-resistant strains.
T19532	Fobrepodacin disodium pVXc-486 disodium,SPR720 disodium	Others	Others
	SPR720 disodium is an orally active and potent phosphate VXc-486 prodrug,has potent bactericidal activities in vivo.
T63610	SPR7
	SPR7 是有效的、选择性的 rhodesain 抑制剂 (Ki: 0.51 nM)。SPR7 对 T. b. brucei 表现出抗寄生虫效果 (EC50: 1.65 μM)。
T73553	SPR39
	SPR39 是一种有效的 SARS-CoV-2 主要蛋白酶抑制剂，对 SARS-CoV-2 Mpro, hCatL, hCatB 的 Ki 值分别为 0.252、3.38、7.88 µM。SPR39 具有抗病毒和细胞毒性。
T70792	SPR519
	SPR519 is a potent dual inhibitor of PI3Kα and mTOR kinases with IC50 (PI3Kalpha) = 30 nM and IC50 (mTOR) = 10 nM. SPR519 exhibits an EC50 of low sub-micromolar range among various tested cancer cell lines such as A2780 (0.23 μM), PC3 (0.48 μM), and SKOV3 (0.50 μM).
T75994	SPR741 TFA
	SPR741 TFA (NAB741 TFA)，一种源自多粘菌素B的阳离子肽增效剂，通过提升革兰氏阴性细菌外膜通透性用于对抗重度革兰氏阴性细菌感染。它能够抑制多重耐药性革兰氏阴性细菌，并在与抗生素联用时扩大抗生素的活性谱。
T73555	SPR41
	SPR41 是一种有效的 SARS-CoV-2 主要蛋白酶抑制剂，对 SARS-CoV-2 Mpro, hCatL, hCatB 的 Ki 值分别为 0.184, 0.252, 14.4 µM。SPR41 具有抗病毒和细胞毒性。
T73554	SPR38
	SPR38 是一种有效的 SARS-CoV-2 主要蛋白酶 (SARS-CoV-2 main protease) 抑制剂，Ki 为 0.260 μM。SPR38 还抑制hCatL 和hCatB，Ki 值分别为 1.92 μM 和 11.1 μM。
T70677	PLS-123
	PLS-123 is a novel covalent irreversible Btk inhibitor with potential anti-proliferative activity. PLS-123 exhibited more potent anti-proliferative effects than ibrutinib in multiple cellular and in vivo preclinical models of B-cell lineage malignancy, including 14 kinds of cell lines, patients’ primary tumor cells and mouse xenograft model.
TP1089	SPR741 TFA (1179330-52-9 free base) NAB741 TFA,SPR741 TFA
	SPR741 TFA (NAB741 TFA) is a cationic peptide derived from polymyxin B and is a potentiator molecule.
T27636	Ispronicline AZD-3480,RJR-1734,AZD 3480,TC 1734,AZD3480,TC-01734,TC-1734-112	AChR	Neuroscience
	Ispronicline (TC-1734) 是一种具有口服活性、选择性和有效性的 α4β2 nAChR 部分激动剂，具有抗抑郁、神经保护和持久的认知作用。Ispronicline 对 α4β2 nAChR 具有很高的亲和力，Ki= 11 nM。
T76540	Insulin peglispro
	Insulinpeglispro(BIL)为一种基础胰岛素，展现平坦、延长的活性特性，相较于传统胰岛素，可提供更优血糖控制。
T27286L	Esprolol

T34699	Sprodiamide S 043,S043,S-043
	Sprodiamide is a magnetic susceptibility-based MRI contrast agent.
T61319	Onfasprodil
	Onfasprodil, a negative allosteric modulator of NR2B, has been identified as a potential compound for researching Alzheimer's disease. This compound, in combination with a GABA receptor regulator.[1]
T19728	SPRC S-Propargyl-cysteine
	SPRC is a novel synthetic molecule exerting antioxidant effects via elevating the generation of endogenous H2S. SPRC activates Gp130-mediated STAT3 and prevents doxorubicin-induced cardiotoxicity.
T27286	Esprolol hydrochloride ACC9369,ACC 9369,ACC-9369
	Esprolol is a β-adrenergic receptor antagonist.
T69595	Ispronicline hemigalactarate
	Ispronicline, also known as AZD3480; TC 1734; TC-0173, and RJR 1734, is a alpha4beta2 nicotinic acetylcholine receptor-selective agonist with cognition-enhancing and neuroprotective properties. Ispronicline is potentially useful for the treatment of attention-deficit/hyperactivity disorder in adults.
T78070	Despropylene gatifloxacin
	Despropylene gatifloxacin为AM-1155的代谢产物，后者显示出较强的抗菌活性及良好的药代动力学特性。
T3175	LDHA-IN-4 AZ 33,AZ-33,LDHA Inhibitor,AZ33	Dehydrogenase	Metabolism
	LDHA-IN-4 (AZ33) 是乳酸脱氢酶 A 选择性抑制剂，IC50=0.5 μM，Kd=0.093 μM。
T10896L	CSRM617 hydrochloride CSRM617 hydrochloride(787504-88-5 Free base)	Apoptosis; Others; Androgen Receptor	Apoptosis; Endocrinology/Hormones; Others
	CSRM617 hydrochloride 是转录因子ONECUT2(OC2，雄激素受体 AR 的主要调节剂) 的选择性小分子抑制剂，在 SPR 测定中Kd 为 7.43 uM，直接与 OC2-HOX 结构域结合。CSRM617 hydrochloride 通过裂解 Caspase-3 和 PARP 诱导细胞凋亡 (apoptosis)。CSRM617 hydrochloride 在小鼠的前列腺癌模型中具有良好的耐受性。
T4288	hVEGF-IN-1	VEGFR	Angiogenesis; Tyrosine Kinase/Adaptors
	hVEGF-IN-1 是一种喹唑啉衍生物，可以特异性结合内部核糖体进入位点 A 中富含 G 的序列，并会使 G-四链体结构不稳定。在 SPR 实验中，它与 IRES-A (WT) 结合的Kd 值为 0.928 μM。它能够抑制VEGF-A 蛋白表达，阻止肿瘤细胞迁移，抑制肿瘤生长。
T12600	QM385	Others	Others
	QM385 is a potent inhibitor of sepiapterin reductase (SPR)(IC50 of 1.49 nM).
T10434	AZD-5991	BCL	Apoptosis
	AZD-5991 is a potent and selective Mcl-1 inhibitor (IC50: 0.7 nM in FRET assay; Kd: 0.17 nM in SPR assay).
T37036	hnRNPK-IN-1
	hnRNPK-IN-1 is a specific ligand that binds to the heterogeneous nuclear ribonucleoprotein K (hnRNPK) with high affinity, evidenced by Kd values of 4.6 μM and 2.6 μM determined using surface plasmon resonance (SPR) and microscale thermophoresis (MST), respectively. This binding event leads to the disruption of hnRNPK's interaction with the c-myc promoter, resulting in the inhibition of c-myc transcription. Additionally, hnRNPK-IN-1 induces apoptosis in Hela cells and exhibits potent anti-tumor a...
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].
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...
T10896	CSRM617	Others	Others
	CSRM617 is a selective small molecule inhibitor of the transcription factor ONECUT2 (OC2, the main regulator of androgen receptor). The Kd in SPR analysis is 7.43 uM, which can directly bind to the OC2-HOX domain. CSRM617 induces apoptosis by cleaving the

化合物

Cat.No: T70030

Cat.No: T70679

SPR inhibitor 3

Cat.No: T16924

Synonym: SPRi3

Target: Others

SPR206 acetate

Cat.No: T39983

SPR741 acetate

Cat.No: T12992

Synonym: SPR741 acetate,NAB741 acetate,SPR741 acetate (1179330-52-9 free base)

Target: Antibacterial

Cat.No: T12991

Target: Others

Cat.No: T4340

Target: Phosphatase

Cat.No: TP1090

Synonym: NAB741

Cat.No: T13326

Synonym: VXc-486

Target: Others

Cat.No: T38801

Synonym: SPR720,pVXc-486

Cat.No: T70790

Ibrexafungerp citrate

Cat.No: T70029

Fobrepodacin disodium

Cat.No: T19532

Synonym: pVXc-486 disodium,SPR720 disodium

Target: Others

Cat.No: T63610

Cat.No: T73553

Cat.No: T70792

Cat.No: T75994

Cat.No: T73555

Cat.No: T73554

Cat.No: T70677

SPR741 TFA (1179330-52-9 free base)

Cat.No: TP1089

Synonym: NAB741 TFA,SPR741 TFA

Cat.No: T27636

Synonym: AZD-3480,RJR-1734,AZD 3480,TC 1734,AZD3480,TC-01734,TC-1734-112

Target: AChR

Insulin peglispro

Cat.No: T76540

Cat.No: T27286L

Cat.No: T34699

Synonym: S 043,S043,S-043

Cat.No: T61319

Cat.No: T19728

Synonym: S-Propargyl-cysteine

Esprolol hydrochloride

Cat.No: T27286

Synonym: ACC9369,ACC 9369,ACC-9369

Ispronicline hemigalactarate

Cat.No: T69595

Despropylene gatifloxacin

Cat.No: T78070

Cat.No: T3175

Synonym: AZ 33,AZ-33,LDHA Inhibitor,AZ33

Target: Dehydrogenase

CSRM617 hydrochloride

Cat.No: T10896L

Synonym: CSRM617 hydrochloride(787504-88-5 Free base)

Target: Apoptosis, Others, Androgen Receptor

Cat.No: T4288

Target: VEGFR

Cat.No: T12600

Target: Others

Cat.No: T10434

Target: BCL

Cat.No: T37036

BMSpep-57 hydrochloride

Cat.No: T36885

Cat.No: T39106

Cat.No: T10896

Target: Others

Cat. No.	Product Name	Target	Signaling Pathways
TN1195	17-Hydroxy sprengerinin C 17-羟基麦冬皂苷C	BCL; Others; Caspase	Apoptosis; Others; Proteases/Proteasome
	17-Hydroxy sprengerinin C 是从黄精的根茎中分离得到的一种糖苷化合物，具有更强的抗癌活性。17-Hydroxy sprengerinin C 降低 Blc-2 和 pro-caspase3 的表达并增加 Bax 的产生。
T4S1247	14-Hydroxy sprengerinin C 14-羟基麦冬皂苷C,14-羟基麦冬皂苷 C	Others	Others
	14-Hydroxy sprengerinin C 是一种甾体化合物，提取自麦冬。
TN2782	2''-O-Acetylsprengerinin C	Others	Others
	2''-O-Acetylsprengerinin C 是一种天然产物，可用于生命科学领域的相关研究。其产品编号为 TN2782，CAS号为 1220707-33-4。
TN5296	Sprengerinin A
	Sprengerinin A是一种天然产物，属于百合科沿阶草属，其产品编号为 TN5296，CAS号为 88866-99-3。Sprengerinin A可用作对照参考。
TN5050	Sprengerinin C	NADPH-oxidase; VEGFR; p38 MAPK; ROS; Akt; PI3K; mTOR; p53	Angiogenesis; Apoptosis; Cytoskeletal Signaling; Immunology/Inflammation; MAPK; PI3K/Akt/mTOR signaling; Tyrosine Kinase/Adaptors
	Sprengerinin C exerts anti-tumorigenic effects in hepatocellular carcinoma via inhibition of proliferation and angiogenesis and induction of apoptosis, it can strongly suppress tumor angiogenesis in human umbilical vein endothelial cells, it blocks vascul

天然产物

17-Hydroxy sprengerinin C

Cat.No: TN1195

Synonym: 17-羟基麦冬皂苷C

Target: BCL, Others, Caspase

14-Hydroxy sprengerinin C

Cat.No: T4S1247

Synonym: 14-羟基麦冬皂苷C,14-羟基麦冬皂苷 C

Target: Others

2''-O-Acetylsprengerinin C

Cat.No: TN2782

Target: Others

Sprengerinin A

Cat.No: TN5296

Sprengerinin C

Cat.No: TN5050

Target: NADPH-oxidase, VEGFR, p38 MAPK, ROS, Akt, PI3K, mTOR, p53

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