136
10
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
TP2098 |
Echistatin
Echistatin, α1 isoform |
||
Potent irreversible αVβ3 integrin antagonist (Ki = 0.27 nM). Disrupts attachment of osteoclasts to bone and inhibits bone reabsorption (IC50 = 0.1 nM). Prevents ADP-induced platelet aggregation via inhibition of glycoprotein IIb/IIIa (GpIIb/IIIa, αIIbβ3) | |||
T16129 |
MPI_5a
|
HDAC | Chromatin/Epigenetic; DNA Damage/DNA Repair |
MPI_5a 是高效的 HDAC6选择性抑制剂,IC50=36 nM,对其他 HDAC 酶几乎无抑制作用。MPI_5a 抑制细胞内酰基微管蛋白积累, IC50为 210 nM。 | |||
T76655 |
Prokineticin 2 Isoform 2 (human)
|
||
Prokineticin 2 Isoform 2 (human) 为一下丘脑神经肽,能减少食物摄入,并在啮齿动物的体温调节与能量代谢中发挥作用。此外,Prokineticin 2 对高血糖、代谢综合征 (MetS) 及肥胖研究具有潜在价值。 | |||
T76064 |
Beta-defensin 103 isoform X1, pig
|
||
Beta-defensin 103 isoform X1, pig 是一种抗菌肽、在多种生物体内被发现,参与了先天性免疫防线。 | |||
T76064L |
Beta-defensin 103 isoform X1, pig TFA
|
||
Beta-defensin 103 isoform X1, pig TFA 是一种抗菌肽、在多种生物体内被发现,参与了先天性免疫防线。 | |||
T12103 |
MR-L2
|
PDE | Metabolism |
MR-L2 是可逆的、非竞争性的长型异构体磷酸二酯酶 -4激活剂,可以激活代表性的 PDE4 长型异构体 (PDE4A4、PDE4B1、PDE4C3、PDE4D5)。它可抑制 PGE2- 诱导的 MDCK 细胞囊肿形成,其EC50=1.2 µM。 | |||
T6704 |
TG 100713
TG100713 |
PI3K | PI3K/Akt/mTOR signaling |
TG 100713 是一种PI3K 的抑制剂,抑制PI3Kδ,γ,α和β的IC50值分别为24、50、165 和 215 nM。 | |||
T2256 |
CNX-1351
1-[4-[[2-(1H-吲唑-4-基)-4-(4-吗啉基)噻吩并[3,2-D]嘧啶-6-基]甲基]-1-哌嗪基]-6-甲基-5-庚烯-1,4-二酮 |
PI3K | PI3K/Akt/mTOR signaling |
CNX1351 是有效的、选择性的 PI3Kα 抑制剂,其 IC50=6.8 nM。 | |||
T22774L |
eukaryotic translation elongation factor 1 alpha 1 (EEF1A1) (387-394) [Multiple species](TFA)
|
Others | Others |
eukaryotic translation elongation factor 1 alpha 1 (EEF1A1) (387-394) [Multiple species](TFA) 是延伸因子 1 亚基。真核翻译延伸因子 1 alpha 1 (EEF1A1) 编码延伸因子 alpha 亚基的同种型- 1 复合物,负责将氨酰 tRNA 酶促递送至核糖体。这种亚型(α 1)在脑、胎盘、肺、肝、肾和胰腺中表达,另一种亚型(α 2)在脑、心脏和骨骼肌中表达。这种亚型在 66% 的 Felty 综合征患者中被鉴定为自身抗原。已发现该基因在许多染色体上具有多个拷贝,其中一些(如果不是全部)代表不同的假基因。 | |||
T14089 |
AC-261066
AC 261066 |
Retinoid Receptor | Metabolism |
AC-261066是一种口服的RARβ2的同型选择性激动剂,pEC50为8.0。 | |||
T8584 |
6-Phenyldihydropyrimidine-2,4(1h,3h)-dione
2,4(1H,3H)-Pyrimidinedione,dihydro-6-phenyl- |
Others | Others |
6-Phenyldihydropyrimidine-2,4(1h,3h)-dione 靶向多嘧啶束结合蛋白 1 亚型 a(人)。 | |||
T3985 |
GDC-0326
GDC 0326,GDC0326 |
PI3K | PI3K/Akt/mTOR signaling |
GDC-0326是一种有效,选择性的 PI3Kα抑制剂,Ki=0.2 nM。 | |||
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. | |||
T21529 |
(S)-Mephenytoin
|
Others | Others |
(S)-Mephenytoin 是一种抗惊厥剂。(S)-Mephenytoin 作为细胞色素 P450 (CYP) 同种型 CYP2C19 的底物,可用于分析细胞色素 P450 代谢。 | |||
T35501 |
5,6-trans-Vitamin D3
5,6-trans-Colecalciferol,5,6-trans-Cholecalciferol,Cholecalciferol EP Impurity A |
Vitamin | Metabolism |
5,6-trans-Vitamin D3(5,6-trans-Cholecalciferol)是维生素 D3 的异构体,经光照后在皮肤表面由 Vitamin D3 转化而来。 | |||
T14090 |
AC-55649
|
Retinoid Receptor | Metabolism |
AC-55649是一种有效的、高度亚型选择性的人 RARβ2受体激动剂,pEC50为6.9。 | |||
T9608 |
KL201
|
Others | Others |
KL201 是一种昼夜节律调制器,是 CRY1选择性的 稳定剂, 对 CRY2 没有稳定作用。KL201 延长了细胞和组织中的昼夜节律周期。 | |||
T2057 |
BVT 2733
|
Dehydrogenase | Metabolism |
BVT 2733 是具有口服活性的、强效的、非甾体类11β-HSD1选择性抑制剂。它对小鼠 11β-HSD1 酶的作用 (IC50:96 nM) 比对人 11β-HSD1 酶 (IC50:3341 nM) 的作用强。它对关节炎和肥胖相关疾病具有潜在的研究价值。 | |||
T1999 |
Taselisib
RG-7604,GDC-0032 |
PI3K; Carbonic Anhydrase | Metabolism; PI3K/Akt/mTOR signaling |
Taselisib (GDC-0032) 是 PI3K 抑制剂,靶向作用于突变 PI3KCA。它能够抑制 PI3Kα (IC50:0.29 nM),PI3Kβ (IC50:0.91 nM) 和 PI3Kγ (IC50:0.97 nM)。 | |||
T2002 |
PF-4708671
PF4708671 |
S6 Kinase; Autophagy | Autophagy; MAPK; PI3K/Akt/mTOR signaling |
PF-4708671 是一种可渗透细胞的 p70 核糖体 S6 激酶抑制剂,对 S6K1的Ki 为 20 nM,IC50为 160 nM。 | |||
T2287 |
PIK-75 hydrochloride
PIK-75 HCl,2-甲基-5-硝基苯磺酸 [(6-溴咪唑并[1,2-a]吡啶-3-基)亚甲基]甲基肼盐酸盐,PIK-75 |
Apoptosis; DNA-PK; PI3K | Apoptosis; DNA Damage/DNA Repair; PI3K/Akt/mTOR signaling |
PIK-75 hydrochloride (PIK-75 HCl) 是一种可逆的 DNA-PK 和 p110α-选择性抑制剂,抑制 DNA-PK,p110α和 p110γ,可诱导凋亡。 | |||
T8840 |
PF-543 hydrochloride
PF-543 |
Apoptosis; S1P Receptor; Autophagy; LPL Receptor | Apoptosis; Autophagy; GPCR/G Protein |
PF-543 hydrochloride (PF-543) 是一种选择性可逆和鞘氨醇竞争性SPHK1抑制剂,对SPHK1的选择性是 SPHK2 的 100 倍以上。它还是全血中 1-磷酸鞘氨醇形成的有效抑制剂,诱导细胞凋亡、坏死和自噬。 | |||
T64377 |
AGI-41998 tautomers
|
Others | Others |
AGI-41998 tautomers 是pyrido[4,3-d]pyrimidin-7(6H)-one, 8-(4-bromophenyl)-6-(4-methoxyphenyl)-2-[(2,2,2-trifluoroethyl)amino]-. pyrido[4,3-d]pyrimidin-7(6H)-one 的互变异构体。pyrido[4,3-d]pyrimidin-7(6H)-one, 8-(4-bromophenyl)-6-(4-methoxyphenyl)-2-[(2,2,2-trifluoroethyl)amino]-. pyrido[4,3-d]pyrimidin-7(6H)-one 是S-adenosylmethionine synthase isoform type-2抑制剂, IC50= 0.022μM。 | |||
T16333 |
NKY80
Adenylyl cyclase type V Inhibitor |
Adenylyl cyclase | Neuroscience |
NKY80 调节心脏和肺组织中的腺苷酸环化酶催化活性。 NKY80 是腺苷酸环化酶 V 型亚型的非竞争性抑制剂(IC50 值:V、III 和 II 型分别为 8.3 µM、132 µM 和 1.7 mM)。 | |||
T27371 |
FR-167356
FR167356,FR 167356 |
ATPase | Membrane transporter/Ion channel |
FR-167356 是 a3 异构体液泡型 H+-ATPase 的特异性抑制剂,对破骨细胞质膜、肾刷状缘膜和巨噬细胞微粒体的 IC50 分别为 170 nM、370 nM 和 220 nM。 FR-167356 减少 B16-F10 细胞的骨转移。 | |||
T21938 |
AS-041164
|
PI3K | PI3K/Akt/mTOR signaling |
AS-041164 是选择性的,具有口服活性的PI3Kγ亚型抑制剂,IC50=70 nM。它对 PI3Kα (IC50:240 μM),PI3Kβ (IC50:1.45 μM) 和 PI3Kδ (IC50:1.70 μM) 的活性较低。它具有抗炎活性。 | |||
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)。 | |||
T4281 |
Endoxifen
(E/Z)-N-desmethyl-4-hydroxy Tamoxifen,N-去甲基-4-羟基-,(E/Z)-Endoxifen |
Estrogen Receptor/ERR; Aromatase; Estrogen/progestogen Receptor; Parasite; Drug Metabolite | Endocrinology/Hormones; Metabolism; Microbiology/Virology |
Endoxifen ((E/Z)-Endoxifen) 是 Tamoxifen 的关键活性代谢物,能抑制芳香酶的活性,与雌激素受体有较高的亲和力和特异性。它有潜力研究乳腺癌。 | |||
T27787L |
L-797,591 hydrochloride
L-797,591 hydrochloride(217480-24-5 Free base) |
||
L-797,591 hydrochloride 对生长抑素受体亚型 1 (SSTR1)有活性。L-797,591 hydrochloride 常与 AG1478 联合使用来增强表达 SSTR1的细胞中 p-ERK5的表达。L-797,591 hydrochloride 在共转染的细胞中显著增强了 p38的磷酸化,这一作用在与 AG1478联合处理时被逆转。 | |||
T24873 |
TGX-115
TGX 115 |
PI3K | PI3K/Akt/mTOR signaling |
TGX-115是一种细胞渗透性和有效的PI 3-K 异构体p110β/p110δ抑制剂(对p110β IC50值为 0.13 μM, 对p110δ值为0.63 μM),是一种调节血小板粘附过程的酶,可抑制磷酸肌苷(PI)3-激酶,可用来治疗冠状动脉闭塞、中风、急性冠状动脉综合征、急性心肌梗塞、血管再狭窄、动脉硬化和不稳定心绞痛等心血管疾病 。 | |||
T8944 |
TTA-A2
|
Calcium Channel | Membrane transporter/Ion channel; Metabolism |
TTA-A2 是一种选择性 T 型钙通道拮抗剂,是一种有效的抗惊厥药,可减少孕烷 X 受体的激活。它对 Cav3.1 (a1G) 和 Cav3.2 (a1H) 通道在 -80 mV 和- 100 mV 保持电位上具有同样的作用,IC50 值分别为 89 和 92 nM。它可用于多种人类神经系统疾病的研究,包括睡眠障碍和癫痫。 | |||
T36696 |
DMBA
|
||
7,12-Dimethylbenz[a]anthracene (DMBA) is a polycyclic aromatic hydrocarbon (PAH) that has been found in tobacco smoke and diesel exhaust and has carcinogenic activity.1,2It undergoes metabolic activation by numerous enzymes, including the cytochrome P450 (CYP450) isoform CYP1B1, as well as microsomal epoxide hydrolase (mEH), producing a variety of reactive metabolites that form DNA adductsin vivo, and it has been commonly used to induce tumor formation in various rodent models.2,3,1DMBA increase... | |||
T26960 |
CB7833407
|
||
CB7833407 is a selective Adenylyl Cyclase isoform-2 (AC2) inhibitor. | |||
T2238L |
Cariporide Mesylate
Cariporide Mesylate salt,HOE-642,HOE 642,HOE642 |
||
Cariporide Mesylate is a selective inhibitor of the Na+/H+ exchanger isoform 1. | |||
T23566 |
Zoniporide dihydrochloride
|
Others | Others |
Sodium-hydrogen exchanger isoform 1 (NHE1) inhibitor | |||
TP2241 |
[Des-octanoyl]-Ghrelin (human)
|
Others | Others |
[Des-octanoyl]-Ghrelin (human) is a Non-acylated, major circulating isoform of ghrelin. | |||
T13113 |
Teglicar
|
Others | Others |
Teglicar is a selective and reversible liver isoform of carnitine palmitoyl-transferase 1 (L-CPT1) inhibitor. | |||
TP2242 |
[Des-octanoyl]-Ghrelin (rat)
|
Others | Others |
[Des-octanoyl]-Ghrelin (rat) is a Non-acylated, major circulating isoform of ghrelin. | |||
T24020 |
DTS
Dibenzyl trisulfide |
||
DTS is a selective and isoform-specific RSK1 kinase inhibitor. It also has broad cancer therapeutic potential. | |||
T11702 | J30-8 | Others | Others |
J30-8 exhibits neuroprotective activity in vitro and potential for the treatment of neurodegenerative diseases. J30-8 is a potent and isoform-selective inhibitor of c-Jun N-terminal kinase 3 (JNK3) with an IC50 of 40 nM, which 2500-fold isoform selectivit | |||
T16908 |
Sonolisib
PX-866 |
PI3K | PI3K/Akt/mTOR signaling |
Sonolisib is an irreversible and pan-isoform inhibitor of PI3K (IC50=0.1 nM (p110α), 1.0 nM (p120γ), 2.9 nM (p110δ)). | |||
T12616 |
(R)-CE3F4
|
Others | Others |
(R)-CE3F4 is a selective inhibitor of exchange protein directly activated by cAMP isoform 1 (Epac1)(IC50 of 4.2 μM), | |||
T71513 |
GK-136901
|
||
GK-136901 is a first-in-class, potent, and orally bioavailable NADPH oxidase isoform 4 (Nox4) inhibitor. | |||
T13359 |
XPC-6444
|
Others | Others |
XPC-6444 is a isoform-selective, and CNS-penetrant inhibitor of NaV1.6 with IC50 of41 nM for hNaV1.6,with anticonvulsant activity. | |||
T61874 | DN02 | ||
DN02 is a highly potent and selective probe for the BRD8 bromodomain. It demonstrates a marked affinity for the BRD8(1) isoform with a Ki value of 32 nM, exhibiting a 30-fold greater affinity compared to BRD8(2) isoform with a Ki value greater than 1000 nM [1]. | |||
T22774 |
eukaryotic translation elongation factor 1 alpha 1 (EEF1A1) (387-394) [Multiple species]
|
Others | Others |
eukaryotic translation elongation factor 1 alpha 1 (EEF1A1) encodes an isoform of the alpha subunit of the elongation factor-1 complex, which is responsible for the enzymatic delivery of aminoacyl tRNAs to the ribosome. This isoform (alpha 1) is expressed | |||
T14566 | BI-9627 | Others | Others |
BI-9627 is an inhibitor of sodium-hydrogen exchanger isoform 1 (NHE1) (EC50: 31 nM). | |||
T24224 |
JTT-010
JTT010 |
||
JTT-010 is a selective inhibitor of protein kinase C-beta isoform. | |||
T40852 |
(Rac)-γ-Tocopherol
(Rac)-γ-Tocopherol,DMPBQ |
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(Rac)-γ-Tocopherol (DMPBQ) is an isoform of Vitamin E that undergoes conversion to γ-Tocopherol through the action of tocopherol cyclase. | |||
T37306 |
6-hydroxy Chlorzoxazone
6-hydroxy Chlorzoxazone,NSC 24955 |
||
6-hydroxy Chlorzoxazone is a metabolite of chlorzoxazone. [1] It is formed by metabolism of chlorzoxazone by the cytochrome P450 (CYP) isoform CYP2E1 in human hepatic microsomes. |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T2S1797 |
Santalol
檀香醇;白檀油萜醇;檀香脑,檀香醇 |
Antioxidant; Antifungal | Microbiology/Virology; oxidation-reduction |
Santalol 是一种檀香醇的 α 和 β-异构体混合物。 其中α-santalol 分离自檀香油中,是一种有前途的抗癌药,能够预防口腔癌、前列腺癌、乳腺癌和皮肤癌。 | |||
TN1778 |
Isoformononetin
异刺芒柄花素,黄豆苷元杂质 |
IL Receptor; Antifection | Immunology/Inflammation; Microbiology/Virology |
Isoformononetin shows fungitoxic activity against Cladosporium sphaerospermum; it also has immunomodulatory activity, it inhibits the differentiation of Th17 cells and B-cell lymphopoesis to promote osteogenesis in estrogen-deficient bone loss conditions. | |||
T5743 |
Gymnemagenin
|
Liver X Receptor | Metabolism |
Gymnemagenin 是一种分离自G. sylvestre 的三萜。 它具有抗病毒作用,对糖尿病和肥胖症具有潜在的研究价值。 | |||
T2949 |
Alizarin
Mordant Red 11,Anthraquinonic,茜素 |
P450 | Metabolism |
Alizarin (Mordant Red 11) 是一种天然红色染料,从茜草植物根部提取得到,已广泛用作纺织品和绘画中的颜料。 | |||
T9675 |
α-Tocotrienol
|
Endogenous Metabolite | Metabolism |
α-Tocotrienol 是维生素 E 的一种亚型,存在于蔬菜、水果、种子、坚果、谷物和油脂中。α-Tocotrienol 是抗氧化剂,可以降低胆固醇和其他脂类,也是神经保护和抗癌剂,在心血管疾病的保护中发挥作用。 | |||
T6491 |
(-)-(S)-Equol
(−)-Equol,Equol,4',7-Dihydroxyisoflavan,4',7-Isoflavandiol,雌马酚 |
Estrogen Receptor/ERR; Estrogen/progestogen Receptor; Endogenous Metabolite | Endocrinology/Hormones; Metabolism |
(-)-(S)-Equol (4',7-Dihydroxyisoflavan) 是雌激素受体β的高亲和力配体。 | |||
T16837 |
SAICAR
|
Others | Others |
SAICAR is an intermediate of de novo purine nucleotide biosynthesis, activates pyruvate kinase isoform M2 (PKM2) in an isozyme-selective manner (EC50: 0.3 mM). | |||
TN3910 |
Ecdysone
|
Apoptosis; ATPase; Glucocorticoid Receptor; Potassium Channel; Sodium Channel; Endogenous Metabolite; Autophagy | Apoptosis; Autophagy; Endocrinology/Hormones; Membrane transporter/Ion channel; Metabolism |
Ecdysone 是存在于昆虫和草药中的主要类固醇激素,可以激活盐皮质激素受体并诱导细胞凋亡。Ecdysone 的活性代谢物 20-羟基蜕皮激素在协调发育过渡和体内稳态睡眠调节中起重要作用。 | |||
T36472 |
Tetrahydro-11-deoxy Cortisol
|
||
Tetrahydro-11-deoxy cortisol (THS) is the primary urinary metabolite of 11-deoxycortisol. Urinary excretion of THS is elevated in patients with 11β-hydroxylase deficiency, a condition resulting from mutations in the cytochrome P450 (CYP) isoform CYP11B1. Urinary levels of THS are also elevated in patients with adrenocortical carcinoma (ACC) and adrenocortical adenoma (ACA) but are higher in patients with ACC compared to ACA. | |||
T37810 |
6',7'-Epoxybergamottin
|
||
6'7'-Epoxybergamottin is a furanocoumarin found in grapefruit. It is a potent inhibitor of the cytochrome P450 (CYP) isoform CYP3A4 with an IC50 value of 0.30 ppm in a cell-free assay, 0.33 μM in HL7 human liver cells, and 0.22 μM in S9 human intestine cells. It has been studied in the context of drug interactions with grapefruit constituents. It is found in grapefruit juice at concentrations of 0.1-7.4 μM and inhibits the transport of talinolol , a permeability glycoprotein (P-gp/ABCB1) transpo... |