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898

抑制剂 & 化合物

22

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Cat. No. Product Name Target Signaling Pathways
T9339 Stafia-1

STAT JAK/STAT signaling; Stem Cells
Stafia-1 是STAT5a 抑制剂,Ki 为 10.9 μM,IC50 为 22.2 μM。它与 STAT5b 和其他 STAT 家族成员相比,显示出高选择性。
T11960 MBM-55

GSK-3; MAPK; DYRK; Akt; Chk; Bcr-Abl; CDK; S6 Kinase; Aurora Kinase Angiogenesis; Cell Cycle/Checkpoint; Chromatin/Epigenetic; Cytoskeletal Signaling; MAPK; PI3K/Akt/mTOR signaling; Stem Cells; Tyrosine Kinase/Adaptors
MBM-55 是一种有效的中心体相关激酶 2 (NEK2) 抑制剂,IC50 为 1 nM。 MBM-55 通过诱导细胞周期停滞和凋亡有效抑制癌细胞的增殖。
T9470 HPK1-IN-7

MAPK MAPK
HPK1-IN-7 是一种口服有活性的、有效的HPK1(造血祖细胞激酶1, MAP4K1) 抑制剂,其IC50值为2.6 nM,具有强大的家族及激酶组选择性。它对 IRAK4 (59 nM) 和 GLK (140 nM) 具有选择性。当它与抗 PD1联合使用时,对 MC38 同基因肿瘤模型表现出极大的疗效。
T4199 Desmethyl-VS-5584

PI3K; mTOR PI3K/Akt/mTOR signaling
Desmethyl-VS-5584 是 VS-5584 的二甲基类似物。其中VS-5584 是mTOR/PI3K 抑制剂,专门针对于吡啶 [2,3-d] 嘧啶结构。
T28352 PDE9-IN-(S)-C33

(S)-C33

PDE Metabolism
PDE9-IN-(S)-C33 ((S)-C33) 是一种有效的选择性 PDE9 抑制剂 (IC50 = 11 nM)。 PDE9-IN-(S)-C33 可用于中枢神经系统疾病和糖尿病的相关研究。
T9020 GSK620

Epigenetic Reader Domain Chromatin/Epigenetic
GSK620 是一种有口服活性的泛BD2抑制剂,在人全血中表现出抗炎表型,有良好的广谱选择性、可开发性和体内口服药代动力学。它对 BET-BD2 家族蛋白具有高度选择性,其选择性超过所有其他 BET 溴结构域 200 倍以上。
T28628 RVX-297

RVX297

Epigenetic Reader Domain Chromatin/Epigenetic
RVX-297 是口服具有活性的,对BD2有选择性的BET 高效抑制剂,作用于BRD2(BD2)、BRD3(BD2)、BRD4(BD2) 的IC50分别为 0.08、0.05、0.02 μM。它能够阻碍多种免疫细胞炎症基因的表达,对临床前模型急性炎症及自身免疫均有效。
T11696 Ivachtin

Caspase-3 Inhibitor VII

Caspase Apoptosis; Proteases/Proteasome
Ivachtin (Caspase-3 Inhibitor VII) 是一种非肽,非竞争性和可逆的caspase-3抑制剂,IC50为 23 nM。它是其余胱天蛋白酶的适度抑制剂。
T21331 SAR-020106

Chk Cell Cycle/Checkpoint
SAR-020106 是一种强效、ATP 竞争性和选择性 CHK1 抑制剂,IC50为 13.3 nM。它对 CHK2 具有良好的选择性,可通过选择抗癌药物增强抗肿瘤活性。
T9564 IRE1α kinase-IN-1

IRE1 Cell Cycle/Checkpoint
IRE1α kinase-IN-1 是IRE1α 的选择性抑制剂(IC50为 77 nM),对 IRE1α 的选择性高于 IRE1β 亚型 100 倍。它抑制内质网诱导的 IRE1α 寡聚和自磷酸化,并抑制 IRE1α RNase 活性 (IC50=80 nM)。
T5405 BI-1347

CDK Cell Cycle/Checkpoint
BI-1347 是一种有效的、选择性的 CDK8/cyclinC 抑制剂,IC50值为 1 nM,可抑制肿瘤生存。
T1885 Siramesine hydrochloride

Lu 28-179 hydrochloride,西拉美新盐酸盐

Ferroptosis; Sigma receptor; lysosomal autophagy Apoptosis; Autophagy; GPCR/G Protein
Siramesine hydrochloride (Lu 28-179 hydrochloride) 是一种选择性 sigma-2 受体激动剂,可引发 Y 细胞的细胞死亡并在体内表现出有效的抗癌活性。Siramesine 对 sigma-2 受体具有亚纳摩尔亲和力,并且对 sigma-2 受体的选择性是 sigma-1 受体的 140 倍。
T6658 SB-408124

N-(6,8-二氟-2-甲基-4-喹啉)- N-[4-(二甲氨基)苯基]尿素

OX Receptor GPCR/G Protein; Neuroscience
SB408124 是一种 OX1 受体的非肽拮抗剂,在全细胞和膜中的 Ki 值分别为 57 和 27 nM,其选择性是 OX2 受体的 50 倍。
T15418 GS-6201

CVT-6883

Adenosine Receptor GPCR/G Protein; Neuroscience
GS-6201 (CVT-6883) 是选择性腺苷 A2B 受体拮抗剂。它对人腺苷 A2B 受体具有高亲和力和选择性 (Ki=22 nM)。它降低了小鼠急性心肌梗死后心脏中 caspase-1 的活性,并减弱了心脏重塑。它减弱了致敏小鼠 NECA,AMP 或变应原诱导的气道反应性。
T6493 Escitalopram Oxalate

草酸右旋西酞普兰,依他普仑草酸盐,Cipralex,(S)-(+)Citalopram oxalate

Others; 5-HT Receptor; Serotonin Transporter GPCR/G Protein; Neuroscience; Others
Escitalopram Oxalate ((S)-(+)Citalopram oxalate) 是一种外消旋 Citalopram 的 S-对映体,是一种选择性 5-羟色胺再摄取抑制剂,Ki=0.89 nM,比 R(-)-enantiomer 结合亲和力高 30 倍。它对多巴胺转运体和去甲肾上腺素转运体均有选择性,是一种研究抑郁症的抗抑郁药。
T4620 Siramesine

西拉美新,Lu 28-179

Sigma receptor GPCR/G Protein
Siramesine (Lu 28-179) 是sigma-2受体激动剂,通过线粒体的不稳定溶酶体触发细胞死亡,有强大的抗癌活性。它对 sigma-2 受体具有亚纳摩尔亲和力,IC50为 0.12 nM。它对 sigma-2 受体的选择性是 sigma-1 受体的 140倍,IC50为 17 nM。
T14547 JWG-071

JWG071,JWG 071

ERK; Epigenetic Reader Domain Chromatin/Epigenetic; MAPK
JWG-071 是首次报道的 ERK5 激酶选择性化学探针,是一种具有1μM BRD4 IC的BET选择性抑制剂,可提高了 ERK5 活性和 BRD4 选择性。
T6940 PHA-767491 hydrochloride

CAY10572,PHA-767491,PHA767491 HCl,CAY-10572 hydrochloride

Apoptosis; GSK-3; CDK Apoptosis; Cell Cycle/Checkpoint; PI3K/Akt/mTOR signaling; Stem Cells
PHA-767491 hydrochloride (CAY-10572 hydrochloride) 是一种Cdc7-Dbf4(DDK)/Cdk9的双重抑制剂,IC50值分别为 10 nM 和 34 nM。
T16989 Tarafenacin D-tartrate

SVT-40776 D-tartrate

Others Others
Tarafenacin D-tartrate is a highly selective M3 muscarinic receptor antagonist (Ki= 0.19 nM), ~200 fold selectivity over the M2 receptor.
T39573 GSK251

PI3K PI3K/Akt/mTOR signaling
GSK251 is a novel, orally bioavailable inhibitor of PI3Kδ, exhibiting high potency and selectivity, with a unique binding mode.
T10277 AL 8697

p38 MAPK MAPK
AL 8697 是一种特异性 p38α MAPK 抑制剂 (IC50 = 6 nM),其特异性是 p38β (IC50 = 82 nM) 的 14 倍,是其他 91 种激酶的 300 倍。 AL 8697 具有抗炎活性。
T2435 EPZ011989

Histone Methyltransferase Chromatin/Epigenetic
EPZ011989是一种高选择性可口服的 EZH2抑制剂,对wt EZH2以及EZH2突变型Ki 值<3nM。
T14947 CHDI-390576

HDAC Chromatin/Epigenetic; DNA Damage/DNA Repair
CHDI-390576 is a CNS penetrant class IIa HDAC inhibitor (IC50s: 54 nM, 60 nM, 31 nM, 50 nM for class IIa HDAC4, HDAC5, HDAC7, HDAC9). It shows >500-fold selectivity over class I HDACs (1, 2, 3) and ~150-fold selectivity over HDAC8 and the class IIb HDAC6 isoform.
T19671 AZ31

AZ 31,AZ-31

ATM/ATR DNA Damage/DNA Repair; PI3K/Akt/mTOR signaling
AZ31 是一种 ATM 抑制剂,具有有效性、高选择性、和口服活性。AZ31对 ATM 酶、细胞内 ATM 具有抑制作用,IC50 值 分别为<1.2 nM 和 46 nM。AZ31 表现出优异的 ATR 选择性 、PIKK 家族选择性和泛激酶选择性。AZ31 是一种强效的体外放射增敏剂,可用于研究癌症。
T6286 RGFP966 (E-isomer)

HDAC Chromatin/Epigenetic; DNA Damage/DNA Repair
RGFP966 是一种 HDAC3 抑制剂,IC50 为 0.08 μM,比其他 HDAC 选择性高 200 倍以上。
T2356 Ro-3306

Apoptosis; ERK; SGK; PKA; CDK; PKC Apoptosis; Cell Cycle/Checkpoint; Chromatin/Epigenetic; Cytoskeletal Signaling; MAPK; Metabolism; Tyrosine Kinase/Adaptors
Ro 3306 是一种选择性 ATP 竞争性CDK1抑制剂,对 CDK1、CDK1/cyclin B1 和 CDK2/cyclin E 的Ki 值为分别为 20 nM、35 nM 和 340 nM。
T10778 CGP 20712 A

CGP 20712 mesylate

Adrenergic Receptor GPCR/G Protein; Neuroscience
CGP 20712 A (CGP 20712 mesylate) is a highly selective antagonist of β1-adrenoceptor (IC50: 0.7 nM). It shows ~10,000-fold selectivity over β2-adrenoceptors.
T3049 TPCA-1

GW683965,IKK2 Inhibitor IV,TPCA1

Apoptosis; IκB/IKK; STAT Apoptosis; JAK/STAT signaling; NF-κB; Stem Cells
TPCA-1 (TPCA1) 是一种选择性IKK-2抑制剂,IC50值为 17.9 nM。它也是反式激活、DNA 结合以及STAT3磷酸化的一种抑制剂。
T6054 GSK256066

PDE Metabolism
GSK256066 是高亲和力的、选择性的PDE4抑制剂,IC50=3.2 pM,被开发用于慢性阻塞性肺病的研究。
T6064 UK-383367

UK 383367

Procollagen C Proteinase Metabolism
UK-383367 是一种有效、选择性的 BMP-1 抑制剂,IC50=44 nM,对其选择性远高于 MMP 1,2,3,9 和 14。
T26109 Robenacoxib

Onsior

COX Immunology/Inflammation; Neuroscience
Robenacoxib (Onsior) 是一种对环氧化酶-2 有很强的选择性的非甾体化合物,具有抗炎活性。
T1830 BX795

IκB/IKK; Chk; CDK; c-Kit; PDK; Autophagy Autophagy; Cell Cycle/Checkpoint; NF-κB; PI3K/Akt/mTOR signaling; Tyrosine Kinase/Adaptors
BX795 是一种选择性PDK1抑制剂,也是相对特异性的TBK1和IKKɛ 抑制剂。它抑制 S6K1,Akt,PKCδ 和 GSK3β 的磷酸化,可调节自噬。
T21703 4-Chlorophenylguanidine hydrochloride

Others Others
4-Chlorophenylguanidine hydrochloride 是一种有效的尿激酶选择性抑制剂。
T22990 ML-090

Fluoflavine

NADPH-oxidase; Others Immunology/Inflammation; Others
ML-090 是 NOX1 特异性抑制剂 (IC50 = 90 nM),对 NOX1 的特异性高于 NOX2、NOX3、NOX4(所有 IC50 > 10 μM)100倍。
T19917 Gepirone

5-HT Receptor GPCR/G Protein; Neuroscience
Gepirone 属于丁螺环酮家族的 5-HT1A 受体激动剂。它对 5-HT1A 受体的选择性高于 SSRIs。
T13312L Seviteronel

VT-464

Others Others
Seviteronel is an effective CYP17 lyase inhibitor (h-Lyase IC50=69 nM). In a hamster model of androgen biosynthesis inhibition, it demonstrated both exceptional in vitro lyase/hydroxylase selectivity (~10-fold) and oral activity.
T36287 Pirtobrutinib

BTK Angiogenesis; Tyrosine Kinase/Adaptors
Pirtobrutinib (LOXO-305) is an advanced BTK inhibitor that displays high selectivity and operates through a non-covalent mechanism. This compound effectively inhibits various BTK C481 substitution mutations, leading to tumor regression in BTK-dependent lymphoma tumors in mouse xenograft models. Furthermore, Pirtobrutinib exhibits remarkable selectivity for BTK, with more than a 300-fold difference compared to 370 other kinases tested. Notably, at a concentration of 1 μM, Pirtobrutinib demonstrat...
T6306 Erteberel

LY500307

Estrogen Receptor/ERR; Estrogen/progestogen Receptor Endocrinology/Hormones
Erteberel (LY500307) 是一种选择性的雌激素受体 β(ERβ) 激动剂,其Ki=1.54 nM,EC50=3.61 nM。具有抗肿瘤作用。
T16936 SS-208

HDAC Chromatin/Epigenetic; DNA Damage/DNA Repair
SS-208 是一种选择性的 HDAC6 抑制剂 (IC50 = 12 nM),具有抗肿瘤活性。 SS-208 显示出对其他 HDAC 亚型的选择性。
T10299 AMG PERK 44

ERK MAPK
AMG PERK 44 is an orally active and selective PERK inhibitor (IC50: 6 nM) and induces autophagy. It has 1000-fold and 160-fold selectivity over GCN2 (IC50: 7300 nM) and B-Raf (IC50 >1000 nM), respectively.
T8651 CAL-101

(S)-2-(1-(9H-Purin-6-ylamino)ethyl)-5-fluoro-3-phenylquinazolin-4(3H)-one,GS-1101,Idelalisib

PI3K PI3K/Akt/mTOR signaling
CAL-101 (Idelalisib) 是 p110δ 的选择性抑制剂(IC50:2.5 nM;在无细胞试验中);显示对 p110δ 的选择性比 p110α/β/γ 高 40 到 300 倍,对 p110δ 的选择性比 C2β、hVPS34、DNA-PK 和 mTOR 高 400 到 4000 倍。
T6378 AMG-458

AMG 458

c-Met/HGFR Tyrosine Kinase/Adaptors
AMG-458 是一种口服有活力的c-Met 选择性抑制剂,其对人和小鼠的Ki 分别为 1.2 nM 和 2.0 nM。
T68134 Ro-3201195

p38 MAPK MAPK
Ro-3201195是一种新型可口服的p38 MAPK 抑制剂,具有很高的选择性。
T6358 1-Azakenpaullone

1-氮杂坎帕罗酮,azakenpaullone

GSK-3 PI3K/Akt/mTOR signaling; Stem Cells
1-Azakenpaullone (azakenpaullone) 是一种 ATP 竞争性的、具有高度选择性的糖原合成酶激酶3 β (GSK-3β)的抑制剂,其 IC50=18 nM。
T16777 ROC-325

Apoptosis; Autophagy Apoptosis; Autophagy
ROC-325 是一种有效的口服活性自噬抑制剂,具有抗癌活性。 ROC-325 诱导肾细胞癌凋亡并表现出良好的特异性。
T6757 AMG319

PI3K PI3K/Akt/mTOR signaling
AMG319 是一种PI3Kδ选择性抑制剂,其 IC50=18 nM。
T6578 ME0328

PARP Chromatin/Epigenetic; DNA Damage/DNA Repair
ME0328 是一种有效的选择性 PARP 抑制剂,对 PARP3 的 IC50 为 0.89 μM。
T36631 BAY-6035

MEK; Histone Methyltransferase Chromatin/Epigenetic; MAPK
BAY-6035 是 SET 和 MYND 结构域蛋白 3 (SMYD3) 的抑制剂。 BAY-6035 的选择性比其他组蛋白甲基转移酶高 100 倍以上。
T26531 ABT-963

ABT963

ABT-963 is a cyclooxygenase 2 (COX-2) inhibitor potentially for the treatment of osteoarthritis and pain. ABT-963 has excellent selectivity in human whole blood, high oral anti-inflammatory potency in vivo, and gastric safety in the animal studies.
T5503 IPSU

OX Receptor GPCR/G Protein; Neuroscience
IPSU 是可口服和脑渗透性的选择性OX2R 拮抗剂,pKi 值为7.85。

化合物

Stafia-1
Cat.No: T9339
Synonym:
Target: STAT
MBM-55
Cat.No: T11960
Synonym:
Target: GSK-3, MAPK, DYRK, Akt, Chk, Bcr-Abl, CDK, S6 Kinase, Aurora Kinase
HPK1-IN-7
Cat.No: T9470
Synonym:
Target: MAPK
Desmethyl-VS-5584
Cat.No: T4199
Synonym:
Target: PI3K, mTOR
PDE9-IN-(S)-C33
Cat.No: T28352
Synonym: (S)-C33
Target: PDE
GSK620
Cat.No: T9020
Synonym:
Target: Epigenetic Reader Domain
RVX-297
Cat.No: T28628
Synonym: RVX297
Target: Epigenetic Reader Domain
Ivachtin
Cat.No: T11696
Synonym: Caspase-3 Inhibitor VII
Target: Caspase
SAR-020106
Cat.No: T21331
Synonym:
Target: Chk
IRE1α kinase-IN-1
Cat.No: T9564
Synonym:
Target: IRE1
BI-1347
Cat.No: T5405
Synonym:
Target: CDK
Siramesine hydrochloride
Cat.No: T1885
Synonym: Lu 28-179 hydrochloride,西拉美新盐酸盐
Target: Ferroptosis, Sigma receptor, lysosomal autophagy
SB-408124
Cat.No: T6658
Synonym: N-(6,8-二氟-2-甲基-4-喹啉)- N-[4-(二甲氨基)苯基]尿素
Target: OX Receptor
GS-6201
Cat.No: T15418
Synonym: CVT-6883
Target: Adenosine Receptor
Escitalopram Oxalate
Cat.No: T6493
Synonym: 草酸右旋西酞普兰,依他普仑草酸盐,Cipralex,(S)-(+)Citalopram oxalate
Target: Others, 5-HT Receptor, Serotonin Transporter
Siramesine
Cat.No: T4620
Synonym: 西拉美新,Lu 28-179
Target: Sigma receptor
JWG-071
Cat.No: T14547
Synonym: JWG071,JWG 071
Target: ERK, Epigenetic Reader Domain
PHA-767491 hydrochloride
Cat.No: T6940
Synonym: CAY10572,PHA-767491,PHA767491 HCl,CAY-10572 hydrochloride
Target: Apoptosis, GSK-3, CDK
Tarafenacin D-tartrate
Cat.No: T16989
Synonym: SVT-40776 D-tartrate
Target: Others
GSK251
Cat.No: T39573
Synonym:
Target: PI3K
AL 8697
Cat.No: T10277
Synonym:
Target: p38 MAPK
EPZ011989
Cat.No: T2435
Synonym:
Target: Histone Methyltransferase
CHDI-390576
Cat.No: T14947
Synonym:
Target: HDAC
AZ31
Cat.No: T19671
Synonym: AZ 31,AZ-31
Target: ATM/ATR
RGFP966 (E-isomer)
Cat.No: T6286
Synonym:
Target: HDAC
Ro-3306
Cat.No: T2356
Synonym:
Target: Apoptosis, ERK, SGK, PKA, CDK, PKC
CGP 20712 A
Cat.No: T10778
Synonym: CGP 20712 mesylate
Target: Adrenergic Receptor
TPCA-1
Cat.No: T3049
Synonym: GW683965,IKK2 Inhibitor IV,TPCA1
Target: Apoptosis, IκB/IKK, STAT
GSK256066
Cat.No: T6054
Synonym:
Target: PDE
UK-383367
Cat.No: T6064
Synonym: UK 383367
Target: Procollagen C Proteinase
Robenacoxib
Cat.No: T26109
Synonym: Onsior
Target: COX
BX795
Cat.No: T1830
Synonym:
Target: IκB/IKK, Chk, CDK, c-Kit, PDK, Autophagy
4-Chlorophenylguanidine hydrochloride
Cat.No: T21703
Synonym:
Target: Others
ML-090
Cat.No: T22990
Synonym: Fluoflavine
Target: NADPH-oxidase, Others
Gepirone
Cat.No: T19917
Synonym:
Target: 5-HT Receptor
Seviteronel
Cat.No: T13312L
Synonym: VT-464
Target: Others
Pirtobrutinib
Cat.No: T36287
Synonym:
Target: BTK
Erteberel
Cat.No: T6306
Synonym: LY500307
Target: Estrogen Receptor/ERR, Estrogen/progestogen Receptor
SS-208
Cat.No: T16936
Synonym:
Target: HDAC
AMG PERK 44
Cat.No: T10299
Synonym:
Target: ERK
CAL-101
Cat.No: T8651
Synonym: (S)-2-(1-(9H-Purin-6-ylamino)ethyl)-5-fluoro-3-phenylquinazolin-4(3H)-one,GS-1101,Idelalisib
Target: PI3K
AMG-458
Cat.No: T6378
Synonym: AMG 458
Target: c-Met/HGFR
Ro-3201195
Cat.No: T68134
Synonym:
Target: p38 MAPK
1-Azakenpaullone
Cat.No: T6358
Synonym: 1-氮杂坎帕罗酮,azakenpaullone
Target: GSK-3
ROC-325
Cat.No: T16777
Synonym:
Target: Apoptosis, Autophagy
AMG319
Cat.No: T6757
Synonym:
Target: PI3K
ME0328
Cat.No: T6578
Synonym:
Target: PARP
BAY-6035
Cat.No: T36631
Synonym:
Target: MEK, Histone Methyltransferase
ABT-963
Cat.No: T26531
Synonym: ABT963
Target:
IPSU
Cat.No: T5503
Synonym:
Target: OX Receptor
Cat. No. Product Name Target Signaling Pathways
T0185 Escitalopram

Seroplex,依他普仑,S-(+)-Citalopram,艾司西酞普兰,(S)-Citalopram

Dopamine Receptor; 5-HT Receptor; Serotonin Transporter; Adrenergic Receptor; AChR; Norepinephrine; Histamine Receptor GPCR/G Protein; Immunology/Inflammation; Neuroscience
Escitalopram (Seroplex) 是一种外消旋 Citalopram 的 S-对映体,是一种选择性 5-羟色胺再摄取抑制剂,Ki=0.89 nM,比 R(-)-enantiomer 结合亲和力高 30 倍。它对多巴胺转运体和去甲肾上腺素转运体均有选择性,是一种研究抑郁症的抗抑郁药。
T2826 Asaraldehyde

Asarylaldehyde,2,4,5-trimethoxy-Benzaldehyde,Asaronaldehyde,细辛醛

COX Immunology/Inflammation; Neuroscience
Asaraldehyde (2,4,5-trimethoxy-Benzaldehyde) 是COX-2抑制剂,能够明显降低环加氧酶 II (COX-2) 的活性(IC50:100 μg/mL)。
T3S1251 Neoruscogenin

ROR Metabolism
Neoruscogenin 是甾体 sapogenin 家族的成员,是一种可生物利用且具有高亲和力的核受体RORα (NR1F1)激动剂。
T6512 G-418 disulfate

Geneticin,G418 Sulfate,Antibiotic G-418 sulfate,遗传霉素,Geneticin sulfate

Antibacterial; Antibiotic Microbiology/Virology
G-418 disulfate (Geneticin sulfate) 属于氨基糖苷类抗生素,是一种蛋白质合成的抑制剂,具有真核细胞选择性。G-418 disulfate 通过抑制肽链的延伸来阻断多肽合成。
T7472 7-Hydroxyflavone

7-羟基黄酮,7羟基黄酮

P450 Metabolism
7-Hydroxyflavone 是一种黄酮类化合物,从M. indica 中分离得到,具有抗炎活性。它利用 ERK/Nrf2/HO-1 通路保护肾细胞,使其免受尼古丁诱导的细胞毒性。
T0665 Xanthine

2,6-Dihydroxypurine,海生丁(黄嘌呤),黄嘌呤,Isoxanthine

Endogenous Metabolite; Adenosine Receptor GPCR/G Protein; Metabolism; Neuroscience
Xanthine (Isoxanthine) 是一种植物生物碱,存在于茶、咖啡和可可中。Xanthine 是温和的中枢神经系统激活剂,也是嘌呤降解途径的中间产物。
T11041 Dihydro-β-erythroidine hydrobromide

DHβE hydrobromide

Others Others
Dihydro-β-erythroidine hydrobromide(DHβE) is a potent, oral active and competitive antagonist of neuronal nicotinic acetylcholine receptors (nAChRs). Dihydro-β-carotene hydrobromide showed selectivity to α4β4 and α4β2nAChR, with IC50 of 0.19 and 0.37 μM,
TN4788 Pierreione B

mTOR PI3K/Akt/mTOR signaling
Pierreione B is an inhibitor of mTOR signaling with strong anticancer activity. Pierreione A and Pierreione B demonstrate solid tumor selectivity with minimal cytotoxicity.
T74005 Urolithin D

Urolithin D 是EphA 受体的竞争性可逆拮抗剂。Urolithin D 表现出类内选择性。
TN1852 Lancifodilactone F

披针叶五味子二内酯 F

HIV Protease Microbiology/Virology; Proteases/Proteasome
Lancifodilactone F exerts minimal cytotoxicity against C8166 cells (CC50 > 200 microg/mL) and shows anti-HIV activity with EC50 = 20.69 +/- 3.31 microg/mL and a selectivity index > 6.62.
TN3428 Aphadilactone C

Others Others
Aphadilactone C shows significant antimalarial activity with the IC50 value of 170 ± 10 nM. It shows potent and selective inhibition against the diacylglycerol O-acyltransferase-1 (DGAT-1) enzyme (IC50 = 0.46 ± 0.09 uM, selectivity index > 217).
TN2360 Falcarinol

Falcarinol,Panaxynol,人参炔醇

HSP Cytoskeletal Signaling; Metabolism
Falcarinol, also known as Panaxynol, is a naturally occurring compound that acts as an orally active inhibitor of Hsp90. It effectively targets both the N-terminal and C-terminal regions of Hsp90, displaying high selectivity with minimal toxicities. Furthermore, Falcarinol (Panaxynol) demonstrates the ability to induce apoptosis.
T36303 Psammaplin A

Psammaplin A, a marine metabolite, functions as a robust inhibitor of HDAC and DNA methyltransferases, displaying notable potency and selectivity as a DAC1 inhibitor, with an IC50 value of 0.9 nM. It exhibits antimicrobial effects against Gram-positive bacteria and inhibits both DNA synthesis and DNA gyrase activity, also demonstrating antitumor activity[1][2].
T75651 Rivulariapeptolides 988

Rivulariapeptolides 988作为一种高效选择性丝氨酸蛋白酶抑制剂,对胰凝蛋白酶、弹性蛋白酶和蛋白酶K的IC50分别为95.46 nM、15.29 nM和85.50 nM。
T72802 Spongionellol A

Spongionellol A 是一种 MDR1(p-糖蛋白) 抑制剂。Spongionellol A 通过诱导 caspase 依赖性的凋亡 (apoptosis) 而对前列腺癌细胞具有较强的细胞毒活性和选择性。Spongionellol A 可用于癌症的研究,如前列腺癌。
T75630 Ganoderic acid Mf

Ganoderic acid Mf为具有抗肿瘤活性的三萜类化合物,能导致细胞周期在G1期停滞,并在正常细胞与癌细胞中显示高度选择性,通过线粒体介导途径促进细胞凋亡(apoptosis)。
T73072 PTP1B-IN-20

PTP1B-IN-20 是蛋白酪氨酸磷酸酶 1B (PTP1B) 的选择性抑制剂 (IC50=1.05 μM),抑制力超出高度同源 T 细胞蛋白酪氨酸磷酸酶 (TCPTP;IC50=78.0 μM),PTP1B 是抑制 2 型糖尿病的重要靶点。
T79975 Dihydrodehydrodiconiferyl alcohol 9-O-α-L-rhamnopyranoside

HBV Microbiology/Virology
Dihydrodehydrodiconiferyl alcohol 9-O-α-L-rhamnopyranoside(化合物1)是一种具有抗HBV活性的木脂素类化合物。该化合物对HBV表面抗原(HBsAg)的IC50为0.58 mM,而对HBV e抗原(HBeAg)的IC50 > 2.4 mM。其可从八角茴香中提取分离。
T82031 Isoguaiacin

Isoguaiacin为一种天然产物,具有复杂的多环化合物结构,广泛应用于生物医药研究领域。
T75436 Jatrorrhizine hydroxide

Jatrorrhizine hydroxide, 一种从黄连中提取的生物碱,展现了神经保护、抗菌、抗疟原虫及抗氧化的活性。作为一种高效的乙酰胆碱酯酶(AChE)抑制剂(IC50=872 nM),其对BuChE的选择性高达115倍。此外,Jatrorrhizine hydroxide还能通过抑制uptake-2 transporter活性来减少血清素(5-HT)和去甲肾上腺素(NE)的摄取,表现出口服活性。
T83913 Mitraciliatine

Mitraciliatine是一种在M. speciosa(泰国称为Kratom)中发现的生物碱,是μ-阿片受体(MOR)部分激动剂和κ-阿片受体(KOR)激动剂。该化合物对MOR和KOR具有选择性,与δ-阿片受体(DOR; EC50s分别为228, 218, 和 >1,000 nM,针对小鼠受体在GTPγS结合实验中的表现)。Mitraciliatine(100 nmol/动物,脑室内注射)在小鼠的热水尾部缩回实验中延长了撤回潜伏期,这一效果可以通过敲除MOR而非KOR来逆转。与吗啡不同,Mitraciliatine不会诱发过度活动或呼吸抑制。
T37876 Fengycin

Fengycin is a cyclic lipopeptide used as an agricultural fungicide. Fengmycin has an anti-fungal infection effect by damaging the target’s cell membrane[1]. [1]. Sreyoshi Sur, et al. Selectivity and Mechanism of Fengycin, an Antimicrobial Lipopeptide, from Molecular Dynamics. J Phys Chem B. 2018 Mar 1;122(8):2219-2226.

天然产物

Escitalopram
Cat.No: T0185
Synonym: Seroplex,依他普仑,S-(+)-Citalopram,艾司西酞普兰,(S)-Citalopram
Target: Dopamine Receptor, 5-HT Receptor, Serotonin Transporter, Adrenergic Receptor, AChR, Norepinephrine, Histamine Receptor
Asaraldehyde
Cat.No: T2826
Synonym: Asarylaldehyde,2,4,5-trimethoxy-Benzaldehyde,Asaronaldehyde,细辛醛
Target: COX
Neoruscogenin
Cat.No: T3S1251
Synonym:
Target: ROR
G-418 disulfate
Cat.No: T6512
Synonym: Geneticin,G418 Sulfate,Antibiotic G-418 sulfate,遗传霉素,Geneticin sulfate
Target: Antibacterial, Antibiotic
7-Hydroxyflavone
Cat.No: T7472
Synonym: 7-羟基黄酮,7羟基黄酮
Target: P450
Xanthine
Cat.No: T0665
Synonym: 2,6-Dihydroxypurine,海生丁(黄嘌呤),黄嘌呤,Isoxanthine
Target: Endogenous Metabolite, Adenosine Receptor
Dihydro-β-erythroidine hydrobromide
Cat.No: T11041
Synonym: DHβE hydrobromide
Target: Others
Pierreione B
Cat.No: TN4788
Synonym:
Target: mTOR
Urolithin D
Cat.No: T74005
Synonym:
Target:
Lancifodilactone F
Cat.No: TN1852
Synonym: 披针叶五味子二内酯 F
Target: HIV Protease
Aphadilactone C
Cat.No: TN3428
Synonym:
Target: Others
Falcarinol
Cat.No: TN2360
Synonym: Falcarinol,Panaxynol,人参炔醇
Target: HSP
Psammaplin A
Cat.No: T36303
Synonym:
Target:
Rivulariapeptolides 988
Cat.No: T75651
Synonym:
Target:
Spongionellol A
Cat.No: T72802
Synonym:
Target:
Ganoderic acid Mf
Cat.No: T75630
Synonym:
Target:
PTP1B-IN-20
Cat.No: T73072
Synonym:
Target:
Dihydrodehydrodiconiferyl alcohol 9-O-α-L-rhamnopyranoside
Cat.No: T79975
Synonym:
Target: HBV
Isoguaiacin
Cat.No: T82031
Synonym:
Target:
Jatrorrhizine hydroxide
Cat.No: T75436
Synonym:
Target:
Mitraciliatine
Cat.No: T83913
Synonym:
Target:
Fengycin
Cat.No: T37876
Synonym:
Target:
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