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33

抑制剂 & 化合物

2

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T8233	BRD3308	Apoptosis; HIV Protease; HDAC	Apoptosis; Chromatin/Epigenetic; DNA Damage/DNA Repair; Microbiology/Virology; Proteases/Proteasome
	BRD3308 是一种高选择性的HDAC3抑制剂，IC50为 54 nM。它可激活HIV-1转录并破坏HIV-1潜伏期。它抑制由炎性细胞因子或糖脂毒性应激诱导的胰腺 β 细胞凋亡，并增加功能性胰岛素释放。
T70692	ST7612AA1	HIV Protease	Microbiology/Virology; Proteases/Proteasome
	ST7612AA1 是一种新型有效且可口服的 HDAC 抑制剂，作为作为HIV-1潜伏期再激活剂。ST7612AA1 在体内外实验中低浓度显示出显著的抗肿瘤活性。ST7612AA1 具有潜在的抗癌活性，可用于研究疟疾。
T38294	4-Deoxypyridoxine hydrochloride	S1P Receptor	GPCR/G Protein
	4-Deoxypyridoxine hydrochloride 通过抑制 S1P 裂解酶 (SPL) 活性来抑制细胞内 S1P 的降解，与 S1P 一样，减少化学诱导的胰岛素瘤细胞系的细胞凋亡。
T61670	HIV-1 inhibitor-38
	HIV-1 inhibitor-38 (Compound 91) is a powerful agent that inhibits the activity of HIV-1. It exhibits great potential as a novel latency reversing agent, making it a promising candidate for further development [1].
T61134	HIV-1 inhibitor-36
	HIV-1 inhibitor-36 (Compound 2) is a potent HIV-1 inhibitor with significant potential as a novel latency reversing agent [1].
T38209	Hodgkinsine
	Hodgkinsine is a pyrrolidinoindoline alkaloid that has been found inP. colorataand has analgesic activity.1It increases latency to paw licking in the hot plate test and latency to tail withdrawal in the tail-flick test in mice when administered at a dose of 5 mg/kg. 1.Amador, T.A., Verotta, L., Nunes, D.S., et al.Antinociceptive profile of hodgkinsinePlanta Med.66(8)770-772(2000)
TP2147	LSKL, Inhibitor of Thrombospondin (TSP-1) (TFA)	Others	Others
	LSKL, Inhibitor of Thrombospondin (TSP-1) TFA, a latency-associated protein (LAP)-TGFβ derived tetrapeptide, is a competitive antagonist of TGF-β1.
T10605	BRD-K98645985	Others	Others
	BRD-K98645985 is a BAF transcriptional repression inhibitor (EC50: ~2.37 µM). It binds ARID1A-specific BAF complexes, potently reverses HIV-1 latency and prevents nucleosomal positioning.
T29938	AM-3102 KDS-5104,AM 3102,Methyl oleoylethanolamide
	AM-3102 is an OEA analog that stimulates PPARα transcriptional activity and prolongs feeding latency. It is resistant to enzymatic hydrolysis and is as potent as OEA in enhancing transcriptional activity of PPARα and reducing food intake in free-feeding r
T38210	Hodgkinsine B
	Hodgkinsine B is an alkaloid and isomer of hodgkinsine that has analgesic activity.1It increases the latency to tail withdrawal in the tail-flick test in mice when administered at a dose of 10 mg/kg. 1.Kodanko, J.J., Hiebert, S., Peterson, E.A., et al.Synthesis of all low-energy stereoisomers of the tris(pyrrolidinoindoline) alkaloid hodgkinsine and preliminary assessment of their antinociceptive activityJ. Org. Chem.72(21)7909-7914(2007)
T70425	Amiperone
	Amiperone is a neuroleptic drug. It prolonged the latency and reduced the frequency of the noise escape response rate in rats. It also inhibited lever-press response and reduced the shock-avoidance rate at very low dose levels in rats.
T76498	H-Leu-Ser-Lys-Leu-OH
	H-Leu-Ser-Lys-Leu-OH 是一种与LATENCY-ASSOCIATED PEPTIDE (LAP) 氨基端相关的延迟肽，能够抑制TGF-β1的激活。当与KRFK结合时，H-Leu-Ser-Lys-Leu-OH 可以阻断TGF-β1的信号转导，进而防止肝损伤和纤维化的发展。
T25698	Levoprotiline Levoprotilinum
	Levoprotiline 一种抗抑郁的化合物，它是 Oxaprotiline 的 R-（-）对映体，作用与 Oxaprotiline 相当，并且作用起效潜伏期较短。它是第二代抗抑郁药马普替林的继任者。
T81953	LANA-DNA-IN-2
	LANA-DNA-IN-2 (Compound 20) 是抑制潜伏期相关核抗原 (LANA) 与 DNA 相互作用的化合物。它适用于研究卡波西肉瘤相关疱疹病毒 (KSHV) 感染。
T61801	HIV-1 inhibitor-35
	HIV-1 inhibitor-35 (compound 74) is a highly potent inhibitor of the HIV-1 virus, exhibiting EC50 values of 80 nM and 70 nM for LTR and CMV, respectively, in HEK293 cells. Additionally, HIV-1 inhibitor-35 demonstrates inhibitory activity against HepG2 liver cancer cells, with a CC50 value of 40 nM. Moreover, HIV-1 inhibitor-35 shows promise as a potential HIV-1 latency reversing agent [1].
T79493	HIV-1 protease-IN-10	PKC	Chromatin/Epigenetic; Cytoskeletal Signaling
	HIV-1protease-IN-10（化合物2）显示出对HIV-1潜伏期的逆转活性，IC50值为0.22 μM。该化合物通过与PKCδC1b结构域结合展现活性，IC50值为0.69 μM。此外，HIV-1protease-IN-10对于酯酶介导的水解表现出稳定性。
T75954	Mambalgin 1 TFA
	Mambalgin 1 TFA, a selective inhibitor of ASIC1a (with IC50 values of 192 nM for human ASIC1a and 72 nM for the ASIC1a/1b dimer), preferentially binds to the channel in its closed/inactive state. It demonstrates selectivity for ASIC1a over a range of other channels, including ASIC2a, ASIC3, TRPV1, P2X2, 5-HT3, Nav1.8, Cav3.2, and Kv1.2. In vivo, Mambalgin 1 TFA effectively prolongs the latency of the withdrawal response in mouse tail-flick and paw-flick tests.
TP2003	Mambalgin 1
	Selective ASIC1a inhibitor (IC50 values are 192 and 72 nM for human ASIC1a and ASIC1a/1b dimer, respectively). Binds to closed/inactive channel. Selective for ASIC1a over ASIC2a, ASIC3, TRPV1, P2X2, 5-HT3, Nav1.8, Cav3.2 and Kv1.2 channels. Increases late
T70063	GYKI 52466 HCl
	GYKI 52466 is an allosteric AMPA receptor antagonist. It selectively inhibits AMPA-induced inward currents (IC50 = 7.5 µM) over NMDA- or GABA-induced inward currents in primary rat hippocampal neurons at 50 µM but also inhibits kainate-induced inward currents in the same cells (IC50 = 11 µM).2 GYKI 52466 (10 µM) reduces the amplitude of spontaneous excitatory postsynaptic currents (EPSCs) in the same cells. It increases the latency to seizure onset and reduces mortality in a rat model of general...
T37167	Reduced Haloperidol
	Reduced haloperidol is an active metabolite of haloperidol . It is formed via reduction of haloperidol by ketone reductase. Reduced haloperidol inhibits radioligand binding to sigma-1 and dopamine D2 receptors (Kis = 1.4 and 31 nM, respectively) and stimulates brain-derived neurotrophic factor (BDNF) secretion from CCF-SSTG1 and U87MG astrocytic glial cells. It also inhibits norepinephrine, dopamine, and serotonin (5-HT) reuptake (Kis = 21, 25, and 33 μM, respectively, in COS-7 cells expressing ...
T38224	2,3-Dehydro-2-deoxy-N-acetylneuraminic acid
	N-acetyl-2,3-dehydro-2-Deoxyneuraminic acid (DANA) is an inhibitor of human neuriminidases (sialidases) NEU1-4 (IC50s = 143, 43, 61, and 74 μM, respectively). In vivo, DANA (30 μL of a 5 mM solution) reduces latency to first seizure and increases seizure duration in a rat model of potassium-induced seizures.
T37791	A-971432
	A-971432 is a sphingosine-1-phosphate receptor 5 (S1P5) agonist that is selective for S1P5 over S1P1 and S1P3 (IC50s = 0.006, 0.362, and >10 &#181M, respectively). It inhibits forskolin-induced cAMP production in CHO cells expressing S1P5 (EC50 = 4.1 nM). A-971432 (1 &#181M) increases electrical resistance of hCMEC/D3 cells in an in vitro blood-brain barrier model, indicating enhanced barrier integrity, and attenuates blood-brain barrier leakage in an R6/2 transgenic mouse model of Huntington’s ...
T37215	5α,6β-Dihydroxycholestanol
	5α,6β-Dihydroxycholestanol is an oxysterol metabolite of cholesterol formed from conversion of cholesterol epoxides by 5,6-epoxysterol hydrolase. It inhibits NMDA-mediated calcium influx in HEK293 cells expressing NR1/NR2B NMDA receptors in a concentration-dependent manner. It also binds to voltage-gated sodium (Nav) channels and decreases action potentials in hippocampal neurons in vitro when used at a concentration of 10 uM. It increases survival of spinal cord motoneurons, cortical neurons, a...
T36722	Deltorphin II (trifluoroacetate salt)
	Deltorphin II is a peptide agonist of δ2-opioid receptors.1,2It is selective for δ-opioid receptors over μ- and κ-opioid receptors in radioligand bindings assays (Kis = 0.0033, >1, and >1 μM, respectively) and induces [35S]GTPγS binding in mouse brain membrane preparations (EC50= 0.034 μM). Deltorphin II (0.12 mg/kg) decreases the infarction zone:risk zone ratio in a rat model of myocardial ischemia-reperfusion injury induced by coronary occlusion, an effect that can be reversed by the δ2-opioid...
T38193	β-Endorphin (1-27) (human) (trifluoroacetate salt)
	β-Endorphin (1-27) is an endogenous peptide that binds to μ-, δ-, and κ-opioid receptors (Kis = 5.31, 6.17, and 39.82 nM, respectively, in COS-1 cells expressing rat receptors). It binds to rat and mouse brain membrane preparations (IC50s = 1.1 and 5.7 nM, respectively) and induces chemotaxis of human monocytes in vitro when used at a concentration of 1 nM. Intracerebroventricular administration of β-endorphin (1-27) increases the latency to tail withdrawal in response to thermal stimulation in ...
T36570	KUS121
	KUS121 is a valosin-containing protein (VCP) modulator that inhibits VCP ATPase activity (IC50= 330 nM).1It inhibits cell death, ATP depletion, and upregulation of C/EBP-homologous protein (CHOP) induced by tunicamycin, an inducer of ER stress, in HeLa cells when used at concentrations of 20, 50, and 50 μM, respectively. KUS121 (100 μM) inhibits ATP depletion and cell death induced by oxygen-glucose deprivation (OGD) in rat primary cortical neurons in anin vitromodel of cerebral ischemia.2It red...
T83728	Tat-AKAP79 (326-336) TFA Tat-A-kinase Anchor Protein 79 (326-336)
	Tat-AKAP79 (326-336) 是一种肽，由HIV-1 Tat蛋白质转导域与对应于A-kinase anchor protein 79 (AKAP79) 326至336残基的11个氨基酸肽链相连组成。在200 µM浓度下，能抑制蛋白激酶A (PKA) 或PKC激活诱导的瞬时受体电位钒通道1 (TRPV1) 在分离的大鼠背根神经节 (DRG) 神经元中的敏感化。在体内，Tat-AKAP79 (326-336) 抑制小鼠由甲醛或phorbol 12-myristate 13-acetate (PMA014) 引发的伤害性行为。它还延长了小鼠对辐射热刺激爪子撤回的潜伏期，并在卡拉胶诱导的炎症性疼痛小鼠模型中增加了爪子撤回的机械阈力。
T83685	UFP101 TFA
	UFP101是一种合成肽类物质，作为nociceptin受体的拮抗剂（Ki为0.06 nM，测试于表达人类受体的CHO细胞中）。它对nociceptin受体的选择性高于κ-opioid受体（Ki为204 nM，测试于表达大鼠受体的CHO细胞中）。UFP101能抑制表达于CHO细胞膜的nociceptin受体释放GTPγS（EC50为1.86 nM）。通过脑室内给药，UFP101（10 nmol/每只动物）能延长小鼠尾巴甩动试验中的尾巴撤回潜伏期。在由盲肠结扎和穿刺诱发的小鼠败血症模型中，UFP101（0.003、0.03及0.3 mg/kg）能提高生存率。
T83688	R 715 TFA [Ac-Lys-[D-βNal7,Ile8]des-Arg9]-BK,Ac-Lys-Arg-Pro-Pro-Gly-Phe-Ser-D2Nal-Ile-OH
	R 715是一种布拉迪肾上腺素B1受体拮抗剂。它抑制在表达布拉迪肾上腺素B1受体的孤立人类脐带中由布拉迪肾上腺素引发的收缩（pA2 = 8.49）。R 715（200、400及600 µg/kg）通过尾部闪烁测试减少了由链脲佐菌素（STZ）诱导的糖尿病神经病变小鼠模型中尾部撤回的潜伏期。它还在以髓磷脂少突胶质细胞糖蛋白（MOG）（35-55）（MOG35-55）抗原肽诱导的实验性自体免疫性脑炎（EAE）小鼠模型中，通过每天1 mg/kg的剂量减少了后肢无力和瘫痪的发病率，改善对称步态，并减少脊髓炎症灶点数、神经元脱髓鞘以及病灶单核细胞侵袭。R 715（0.01 nmol/动物，脑室内）能在自发性高血压大鼠中降低平均动脉血压并增加心率。
T37718	Galanin (rat, mouse) (trifluoroacetate salt) GAL (rat, mouse),Galanin (rat, mouse) (trifluoroacetate salt)
	Galanin is a neuropeptide with diverse biological activities. [1][2][3][4][5] It binds to rat galanin (GAL) receptor subtypes GAL1-3 (IC50s = 0.339, 1.35, and 3.31 nM, respectively) and human GAL1-3 (IC50s = 0.288, 1.62, and 12.3 nM, respectively). [1] Galanin binds to and inhibits contraction of guinea pig gastric smooth muscle cells induced by carbachol . [2] In vivo, Galanin (6 nmol, i.c.v.) increases feeding behavior in rats and increases latency to hindpaw withdrawal in response to heat and...
T37201	CAY10787
	CAY10787 is an oxysterol and a negative allosteric modulator of GABAAreceptors.1,2It reduces GABA-induced currents in HEK cells expressing α1β1γ2or α4β3γ2subunit-containing GABAAreceptors (IC50s = 1.5 and 1 μM, respectively).2CAY10787 (500 nM) reduces GABA-induced depolarization of peptidergic and non-peptidergic nociceptors, C-LTMRs, and cold thermosensors in isolated mouse dorsal root ganglion (DRG) neurons.In vivo, CAY10787 (2, 10, and 50 mg/kg) increases latency to nocifensive behaviors in t...
T37127	L-AP4 monohydrate L-AP4 monohydrate
	L-AP4 (L-APB) monohydrate is a potent and specific agonist for the group III mGluRs, with EC50s of 0.13, 0.29, 1.0, 249 μM for mGlu4, mGlu8, mGlu6 and mGlu7 receptors, respectively[1][2]. L-AP4 (5-30 μg, intrathecal inhection 4-5 days) significantly increases the paw withdrawal threshold in response to application of von Frey filaments in eight nerve-ligated rats in a dose-dependent manner. Intrathecal administration of different doses of L-AP4 is not associated with any evident motor dysfunctio...
T35762	MC1742
	MC1742 is an inhibitor of class I histone deacetylases (HDACs; IC50s = 0.1, 0.11, 0.02, and 0.61 μM for HDAC1, -2, -3, and -8, respectively) and class IIb HDACs (IC50s = 7 and 40 nM for HDAC6 and HDAC10, respectively).1 It is selective for class I and class IIb over class IIa HDACs (IC50s = >50 μM for HDAC4, -5, -7, and -9). MC1742 reduces proliferation of HOS, MG-63, RD, A204, SK-ES-1, and A673 sarcoma cancer stem cells (CSCs). It increases levels of acetylated histone H3 and acetylated tubulin...

化合物

Cat.No: T8233

Target: Apoptosis, HIV Protease, HDAC

Cat.No: T70692

Target: HIV Protease

4-Deoxypyridoxine hydrochloride

Cat.No: T38294

Target: S1P Receptor

HIV-1 inhibitor-38

Cat.No: T61670

HIV-1 inhibitor-36

Cat.No: T61134

Cat.No: T38209

LSKL, Inhibitor of Thrombospondin (TSP-1) (TFA)

Cat.No: TP2147

Target: Others

Cat.No: T10605

Target: Others

Cat.No: T29938

Synonym: KDS-5104,AM 3102,Methyl oleoylethanolamide

Cat.No: T38210

Cat.No: T70425

H-Leu-Ser-Lys-Leu-OH

Cat.No: T76498

Cat.No: T25698

Synonym: Levoprotilinum

Cat.No: T81953

HIV-1 inhibitor-35

Cat.No: T61801

HIV-1 protease-IN-10

Cat.No: T79493

Target: PKC

Mambalgin 1 TFA

Cat.No: T75954

Cat.No: TP2003

Cat.No: T70063

Reduced Haloperidol

Cat.No: T37167

2,3-Dehydro-2-deoxy-N-acetylneuraminic acid

Cat.No: T38224

Cat.No: T37791

5α,6β-Dihydroxycholestanol

Cat.No: T37215

Deltorphin II (trifluoroacetate salt)

Cat.No: T36722

β-Endorphin (1-27) (human) (trifluoroacetate salt)

Cat.No: T38193

Cat.No: T36570

Tat-AKAP79 (326-336) TFA

Cat.No: T83728

Synonym: Tat-A-kinase Anchor Protein 79 (326-336)

Cat.No: T83685

Cat.No: T83688

Synonym: [Ac-Lys-[D-βNal7,Ile8]des-Arg9]-BK,Ac-Lys-Arg-Pro-Pro-Gly-Phe-Ser-D2Nal-Ile-OH

Galanin (rat, mouse) (trifluoroacetate salt)

Cat.No: T37718

Synonym: GAL (rat, mouse),Galanin (rat, mouse) (trifluoroacetate salt)

Cat.No: T37201

L-AP4 monohydrate

Cat.No: T37127

Synonym: L-AP4 monohydrate

Cat.No: T35762

Cat. No.	Product Name	Target	Signaling Pathways
T2S0842	Scutellarin methyl ester Scutellarin methylester,野黄芩苷甲酯	Others	Others
	Scutellarin methyl ester (3-Oxotirucallenoic Acid) 是一种灯盏花素的成分, 其中灯盏花素是灯盏花中几种黄酮类化合物的粗提物。
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。

天然产物

Scutellarin methyl ester

Cat.No: T2S0842

Synonym: Scutellarin methylester,野黄芩苷甲酯

Target: Others

Cat.No: T83913

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