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41

抑制剂 & 化合物

3

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T3560	Desmethylanethol trithione ADT-OH	VEGFR; Akt	Angiogenesis; Cytoskeletal Signaling; PI3K/Akt/mTOR signaling; Tyrosine Kinase/Adaptors
	Desmethylanethol trithione (ADT-OH) 是合成硫化氢的供体。它利用上调 FADD 诱导细胞凋亡，并对体内黑色素瘤的形成具有一定的抑制作用，可用于研究癌症疾病。
T60060	ACSS2-IN-2 MTB-9655	Fatty Acid Synthase	Metabolism
	ACSS2-IN-2 (MTB-9655) 是酰基辅酶 A 合成酶短链家族成员 2 (ACSS2) 抑制剂。ACSS2-IN-2 可抑制 ACSS2 活性，IC50 为 3.8 nM。ACSS2-IN-2 可用于多种疾病的研究，如病毒感染、代谢紊乱、神经精神疾病、炎症/自身免疫疾病和癌症。
T5337	IACS-010759 IACS-10759,IACS 10759,IACS10759	Apoptosis; Others; Mitochondrial Metabolism	Apoptosis; Metabolism; Others
	IACS-010759 是一种口服有效的线粒体氧化磷酸化复合物 I 抑制剂。它在依赖 OXPHOS 的脑癌和急性髓性白血病模型中抑制增殖并诱导细胞凋亡，有研究复发/难治性 AML 和实体瘤潜力。
T9196	IACS-13909 BBP-398	Phosphatase	Metabolism
	IACS-13909 (BBP-398) 是具有口服活性的、选择性的 SHP2变构抑制剂，其 IC50=15.7 nM，Kd=32 nM。与其他磷酸酶相比，它对 SHP2的选择性更高。它能够抑制受体酪氨酸激酶 (RTK)/MAPK 途径的信号传导，并具有抗癌作用。
T11595	IACS-8779	Others	Others
	IACS-8779 is a potent STING agonist that efficiently stimulates interferon gene activity and exhibits strong systemic antitumor effects.
T62298	PHD2/HDACs-IN-1
	PHD2/HDACs-IN-1 是一种有效的 PHD2/HDACs 混合抑制剂，能够作用于 PHD2 (IC50: 1.15 μM)、HDAC1 (IC50: 19.75 μM)、HDAC2 (IC50: 26.60 μM)、HDAC16 (IC50: 15.98 μM)。PHD2/HDACs-IN-1 是一种低毒性肾保护剂，能够用于顺铂诱导的急性肾损伤 (AKI) 的研究。
T11627	IACS-8968 R-enantiomer IDO/TDO Inhibitor (R-enantiomer)	IDO	Metabolism
	IACS-8968 R-enantiomer is the R-enantiomer of IACS-8968. IACS-8968 is a dual IDO and TDO inhibitor (pIC50s: 6.43 for IDO and <5 for TDO).
T11596	IACS-8803	Others	Others
	IACS-8803 is a potent cyclic dinucleotide STING agonist that exhibits strong systemic antitumor efficacy.
T69759	IACS-9439	c-Fms	Tyrosine Kinase/Adaptors
	IACS-9439是一种CSF1R抑制剂，具有高效、选择性和口服活性，Ki值仅为1 nM。适用于研究晚期实体肿瘤。
T72274	IACS-9571 hydrochloride ASIS-P040 hydrochloride
	IACS-9571 (ASIS-P040) hydrochloride 是溴结构域蛋白 TRIM24和 BRPF1的抑制剂，对 TRIM24 的 IC50和 Kd 值分别为 8 nM 和 31 nM，对 BRPF1的 Kd 值为 14 nM。
T39999	IACS-15414
	IACS-15414 is a potent SHP2 inhibitor that is effective when administered orally, demonstrating an IC50 value of 122 nM.
T63397	ACSS2-IN-1
	ACSS2-IN-1 是 ACSS2 的有效抑制剂，能够抑制 ACSS2 活性，其IC50值为 0.01 nM 到 <1 nM，能够用于研究癌症。
T70091	IACS-4759
	IACS-4759 is a novel potent and selective MTH1 inhibitor with excellent cell permeability and good metabolic stability in microsomes.
T78566	GlcNAcstatin
	GlcNAcstatin，一种基于葡萄糖咪唑的选择性细菌O-GlcNAcase抑制剂，其Ki值为4.6 pM，对HexA/B的选择性高出100000倍。
T27568	IACS-010759 hydrochloride IACS-010759 HCl,IACS-010759,IACS10759,IACS-10759,IACS 10759
	IACS-010759 is a potent inhibitor of complex I of OXPHOS with orally bioavailable. IACS-10759 effectively inhibits ATP production and oxygen consumption in isolated mitochondria, and inhibits the conversion of NADH to NAD+ in immunoprecipitated complex I
T73939	IACS-8803 diammonium
	IACS-8803 diammonium 是一种高效环状二核苷酸的STING 激动剂，具有强大的全身抗肿瘤作用。
T73938	IACS-8803 disodium
	IACS-8803 disodium 是一种高效环状二核苷酸的STING 激动剂，具有强大的全身抗肿瘤作用。
T22551	ACSF	Others	Others
	ACSF is often used as a replacement of CSF for perfusion of brain slices to preserve interneurons. ACSF is invented to reduce the incidence of cerebral edema and further suppress brain cell disorders. And ACSF is often used as an irrigation fluid or perfu
T79303	IACS-52825
	IACS-52825是一种选择性DLK抑制剂，具有1.3 nM的Kd值，适用于研究化疗引起的周围神经病变。
T27289	Etacstil GW 5638,GW-5638,GW5638,DPC974,DPC 974,DPC-974
	GW5638 is a estrogen receptor ligand. GW5638 is a prodrug of its active metabolite GW7604. GW5638 appears to act as an antagonist in these in vitro systems, although in a manner distinct from other known ER modulators. GW5638 is also classified as a pseud
T11597L	IACS-9571 Hydrochloride (1800477-30-8 free base) IACS-9571 Hydrochloride,ASIS-P040 Hydrochloride	Epigenetic Reader Domain	Chromatin/Epigenetic
	IACS-9571 Hydrochloride is a selective and potent inhibitor of TRIM24 and BRPF1, (IC50: 8 nM for TRIM24; Kds: 31 nM and 14 nM for TRIM24 and BRPF1).
T11597	IACS-9571 ASIS-P040	Epigenetic Reader Domain	Chromatin/Epigenetic
	IACS-9571 is a selective and potent inhibitor of TRIM24 and BRPF1, (IC50: 8 nM for TRIM24; Kds: 31 nM and 14 nM for TRIM24 and BRPF1).
T11544	HDACs/mTOR Inhibitor 1	HDAC	Chromatin/Epigenetic; DNA Damage/DNA Repair
	HDACs/mTOR Inhibitor 1 is a dual HDACs and mammalian target of Rapamycin (mTOR) target inhibitor for treating hematologic malignancies (IC50s: 0.19 nM, 1.8 nM, 1.2 nM, and >500 nM for HDAC1, HDAC6, mTOR and PI3Kα).
T72516	IACS-8779 disodium
	IACS-8779 disodium 是一种高效的干扰素基因刺激蛋白 (STING) 激动剂，具有强大的全身性抗肿瘤功效。IACS-8779 disodium 在 B16 小鼠黑色素瘤模型中对STING 通路具有强烈活性，且具有卓越的抗肿瘤作用。
T11628	IACS-8968 S-enantiomer IDO/TDO Inhibitor (S-enantiomer)	IDO	Metabolism
	IACS-8968 S-enantiomer is the S-enantiomer of IACS-8968. IACS-8968 is a dual IDO and TDO inhibitor (pIC50s: 6.43 for IDO and <5 for TDO).
T11626	IACS-8968 IDO/TDO Inhibitor	IDO	Metabolism
	IACS-8968 is a dual IDO and TDO inhibitor (pIC50s: 6.43 for IDO and <5 for TDO).
T68088	Iodofiltic acid
	Iodofiltic acid 可用于辅助治疗急性冠脉综合征（Zeus-ACS），可成像以检测心肌缺血。
T21059	Ticagrelor metabolite M5 Ticagrelor metabolite M5,,T437700,替格瑞洛杂质H,AR-C133913XX	P2Y Receptor	GPCR/G Protein; Neuroscience
	Ticagrelor metabolite M5 (T437700) 是 Ticagrelor 的代谢物，是 P2Y12 受体的第一个可逆口服拮抗剂。与氯吡格雷相比，替格瑞洛对 ADP 受体具有更快和更一致的抑制作用。替格瑞洛用于治疗急性冠状动脉综合征(ACS)。
T76124	Acyl coenzyme A synthetase
	Acyl coenzyme A synthetase (ACS)，一种生化研究中常用的酶，主要通过两步硫酯化反应激活脂肪酸与辅酶A结合，形成酰基辅酶A。该过程为脂质代谢中的多种合成与分解代谢途径，以及参与TCA循环中的有氧呼吸提供了关键中间物。
T35674	StRIP16
	Rab8a GTPase-binding stapled peptide (Kd = 12.7 μM). Cell permeable; localizes to the endomembrane system. Cromm et al (2016) Protease-resistant and cell-permeable double-stapled peptides targeting the Rab8a GTPase. ACS Chem.Biol. 11 2375 PMID:27336832
T36016	PF 06260933 dihydrochloride
	MAP4K4 (HGK) inhibitor (IC50 = 140 nM). Also inhibits MINK and TNIK (IC50 values are 8 and 13 nM, respectively). Improves fasting hyperglycemia in mice. Orally active. Ammirati et al (2015) Discovery of an in vivo tool to establish proof-of-concept for MAP4K4-based antidiabetic treatment. ACS Med.Chem.Lett. 6 1128 PMID:26617966
T36782	TAK1-IN-2 TAK1-IN-2
	TAK1-IN-2 is a potent and selective TAK1 inhibitor, with an IC50> of 2 nM[1]. TAK1-IN-2 (compound 54) (10 μM) has no effect on cell viability in TNF-α stimulated HCT-15 cells[1]. [1]. Veerman JJN, et, al. Discovery of 2,4-1 H-Imidazole Carboxamides as Potent and Selective TAK1 Inhibitors. ACS Med Chem Lett. 2021 Mar 3;12(4):555-562.
T36946	PW0464 PW0464
	PW0464, a nanomolar potent complete G protein biased ligand, is a noncatechol D1R agonist, with an EC50 of 5.8 nM (Gs-cAMP)[1]. PW0464 (compound 24) is found to elicit complete G protein bias, showing no activity for D1R-mediated β-arrestin recruitment[1].PW0464 (compound 24), the non-catechol agonist, forms bonds with S1985.42 and S2025.46 via its fluorine atom[2]. [1]. Pingyuan Wang, et al. Synthesis and Pharmacological Evaluation of Noncatechol G Protein Biased and Unbiased Dopamine D1 Recept...
T36910	PF 04449913 maleate
	Potent Smo antagonist (IC50 = 5 nM). Attenuates the leukemia-initiation potential of AML cells in a serial transplantation mouse model. Also eliminates self-propagation capacity of AML cells. Munchhof et al (2011) Discovery of PF-04449913, a potent and orally bioavailable inhibitor of smoothened. ACS Med.Chem.Lett. 3 106 PMID:24900436 \|Fukushima et al (2016) Small-molecule Hedgehog inhibitor attenuates the leukemia-initiation potential of acute myeloid leukemia cells. Cancer Sci. 107 1422 PMID:2...
T36634	ZQ 16
	Selective medium-chain free fatty acid receptor GPR84 agonist (EC50 = 139 nM). Exhibits no response at GPR40, GPR41, GPR119 or GPR120 at 100 μM. Activates calcium mobilization, inhibits cAMP accumulation, and induces ERK1/2 phosphorylation, receptor desensitization and internalization in vitro. Liu et al (2016) Design and synthesis of 2-alkylpyrimidine-4,6-diol and 6-alkylpyridine-2,4-diol as potent GPR84 agonists. ACS Med.Chem.Lett. 7 579 PMID:27326330 \|Zhang et al (2016) Discovery and characte...
T35488	(S)-PI3Kα-IN-4 (S)-PI3Kα-IN-4
	(S)-PI3Kα-IN-4 is a potent inhibitor of PI3Kα, with an IC50 of 2.3 nM. (S)-PI3Kα-IN-4 shows 38.3-, 4.25-, and 4.93-fold selectivity for PI3Kα over PI3Kβ, PI3Kδ, and PI3Kγ, respectively. (S)-PI3Kα-IN-4 can be used for the research of cancer[1]. (S)-PI3Kα-IN-4 (compound 11) is a quinazolin-4(3H)-one derivative with 2-substituted-N-methylpropanamide substitution[1]. [1]. Dong J, et, al. Discovery of 3-Quinazolin-4(3 H)-on-3-yl-2, N-dimethylpropanamides as Orally Active and Selective PI3Kα Inhibitor...
T36504	STY-BODIPY STY-BODIPY,Styrene-BODIPY
	STY-BODIPY is a styrene-conjugated fluorogenic probe for radical-trapping antioxidant (RTA) activity.1 Co-autoxidation of the STY-BODIPY signal carrier and a hydrocarbon co-substrate can be quantified by monitoring the loss of absorbance at 571 nm. STY-BODIPY has been used to measure the activity of RTAs, as well as the kinetics and stoichiometry of RTA reactions in cell-free assays.1,2,3References1. Haidasz, E.A., Van Kessel, A.T.M., and Pratt, D.A. A continuous visible light spectrophotometric...
T35817	Photoswitchable PAD Inhibitor (technical grade)
	Photoswitchable PAD inhibitor is a photoactivated protein arginine deiminase (PAD) inhibitor and a derivative of BB-Cl-amidine that contains an azobenzene photoswitch allowing optical control of PAD activity.1 Without photoactivation, it is a weak inhibitor of PAD2 (IC50 = >100 μM) and is less potent than BB-Cl-amidine in inhibiting citrulline production in vitro (kinact/KIs = 2,300, 600, 1,000, and 10,510 M-1min-1 for PAD1-4, respectively) and does not inhibit histone H3 citrullination in HEK29...
T38106	JC-171
	JC-171 is a selective NLRP3 inflammasome inhibitor, with an IC50 of 8.45 μM for inhibiting LPS/ATP-induced interleukin-1β (IL-1β) release from J774A.1 macrophages[1]. JC-171 (0-100 μM) blocks NLRP3 inflammasome activation and IL-1β production in primary macrophages dose dependently[1]. ...
T35638	SR 1903
	SR 1903 is a modulator of retinoic acid receptor-related orphan receptor γ (RORγ) and liver X receptor (LXR).1 It is an inverse agonist of RORγ (IC50 = ~100 nM in a cell-based reporter assay) and an agonist of LXR. It also binds to peroxisome proliferator-activated receptor γ (PPARγ; IC50 = 209 nM) but does not activate it. SR 1903 (10 μM) inhibits LPS-induced expression of triggering receptor expressed on myeloid cells 1 (TREM-1) in RAW 264.7 cells. It also inhibits LPS-induced expression of th...
T35527	PI3Kα-IN-4 PI3Kα-IN-4
	PI3Kα-IN-4 is a potent, selective and orally active inhibitor of PI3Kα, with an IC50 of 1.8 nM. PI3Kα-IN-4 has antitumor activity[1]. PI3Kα-IN-4 (compound 10) inhibits PI3Kα, β, δ, and γ, with IC50s of 1.8, 271.0, 13.9, and 13.8 nM, respectively in kinase assays[1].PI3Kα-IN-4 inhibits PI3Kα, β, δ, and γ, with IC50s of 12.1,1393, 183, and >10000 nM, respectively in cell based assays[1]. PI3Kα-IN-4 (compound 10) (30 mg/kg; p.o. once daily for 21 d) achieves the best efficacy, which could inhibit t...

化合物

Desmethylanethol trithione

Cat.No: T3560

Synonym: ADT-OH

Target: VEGFR, Akt

Cat.No: T60060

Synonym: MTB-9655

Target: Fatty Acid Synthase

Cat.No: T5337

Synonym: IACS-10759,IACS 10759,IACS10759

Target: Apoptosis, Others, Mitochondrial Metabolism

Cat.No: T9196

Synonym: BBP-398

Target: Phosphatase

Cat.No: T11595

Target: Others

PHD2/HDACs-IN-1

Cat.No: T62298

IACS-8968 R-enantiomer

Cat.No: T11627

Synonym: IDO/TDO Inhibitor (R-enantiomer)

Target: IDO

Cat.No: T11596

Target: Others

Cat.No: T69759

Target: c-Fms

IACS-9571 hydrochloride

Cat.No: T72274

Synonym: ASIS-P040 hydrochloride

Cat.No: T39999

Cat.No: T63397

Cat.No: T70091

Cat.No: T78566

IACS-010759 hydrochloride

Cat.No: T27568

Synonym: IACS-010759 HCl,IACS-010759,IACS10759,IACS-10759,IACS 10759

IACS-8803 diammonium

Cat.No: T73939

IACS-8803 disodium

Cat.No: T73938

Cat.No: T22551

Target: Others

Cat.No: T79303

Cat.No: T27289

Synonym: GW 5638,GW-5638,GW5638,DPC974,DPC 974,DPC-974

IACS-9571 Hydrochloride (1800477-30-8 free base)

Cat.No: T11597L

Synonym: IACS-9571 Hydrochloride,ASIS-P040 Hydrochloride

Target: Epigenetic Reader Domain

Cat.No: T11597

Synonym: ASIS-P040

Target: Epigenetic Reader Domain

HDACs/mTOR Inhibitor 1

Cat.No: T11544

Target: HDAC

IACS-8779 disodium

Cat.No: T72516

IACS-8968 S-enantiomer

Cat.No: T11628

Synonym: IDO/TDO Inhibitor (S-enantiomer)

Target: IDO

Cat.No: T11626

Synonym: IDO/TDO Inhibitor

Target: IDO

Iodofiltic acid

Cat.No: T68088

Ticagrelor metabolite M5

Cat.No: T21059

Synonym: Ticagrelor metabolite M5,,T437700,替格瑞洛杂质H,AR-C133913XX

Target: P2Y Receptor

Acyl coenzyme A synthetase

Cat.No: T76124

Cat.No: T35674

PF 06260933 dihydrochloride

Cat.No: T36016

Cat.No: T36782

Synonym: TAK1-IN-2

Cat.No: T36946

Synonym: PW0464

PF 04449913 maleate

Cat.No: T36910

Cat.No: T36634

(S)-PI3Kα-IN-4

Cat.No: T35488

Synonym: (S)-PI3Kα-IN-4

Cat.No: T36504

Synonym: STY-BODIPY,Styrene-BODIPY

Photoswitchable PAD Inhibitor (technical grade)

Cat.No: T35817

Cat.No: T38106

Cat.No: T35638

Cat.No: T35527

Synonym: PI3Kα-IN-4

Cat. No.	Product Name	Target	Signaling Pathways
T1284	Megestrol acetate SC10363,醋酸甲地孕酮,BDH1298	Glucocorticoid Receptor; Estrogen/progestogen Receptor; Progesterone Receptor; HIV Protease; Autophagy	Autophagy; Endocrinology/Hormones; Microbiology/Virology; Others; Proteases/Proteasome
	Megestrol acetate (BDH1298) 是具有口服活性的合成孕激素。它还具有抗雄激素特性，可用于治疗厌食症和恶病质。
T13199	Triacsin C WS 1228A,FR 900190	Others	Others
	Triacsin C, from Streptomyces aureofaciens, is a natural intracellular long-chain inhibitor of acyl-CoA synthetases (ACSL).
T36950	Rubrofusarin triglucoside
	Rubrofusarin triglucoside is a glycoside compound isolated from Cassia obtusifolia Linn seeds. Rubrofusarin triglucoside inhibits human monoamine oxidase A (hMAO-A) with an IC50 of 85.5 μM[1]. [1]. Pradeep Paudel, et al. Rubrofusarin as a Dual Protein Tyrosine Phosphate 1B and Human Monoamine Oxidase-A Inhibitor: An in Vitro and in Silico Study. ACS Omega. 2019 Jul 3;4(7):11621-11630.

天然产物

Megestrol acetate

Cat.No: T1284

Synonym: SC10363,醋酸甲地孕酮,BDH1298

Target: Glucocorticoid Receptor, Estrogen/progestogen Receptor, Progesterone Receptor, HIV Protease, Autophagy

Cat.No: T13199

Synonym: WS 1228A,FR 900190

Target: Others

Rubrofusarin triglucoside

Cat.No: T36950

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