cl-1

steroidal androgen receptor agonist

Cl-Necrostatin-1 is an inhibitor of receptor-interacting protein kinase. It inhibits RIPK1 activity.

Looplure is a chemosterilant, insect attractant and repellent.

Selamectin (UK-124114) 是半合成的大环内酯，是一种驱虫剂，可增强线虫中谷氨酸和 GABA 门控氯离子通道的开放。它还是抗寄生虫剂，可激活神经元和咽肌中的谷氨酸门控氯离子通道，以预防恶丝虫，淋巴丝虫和线虫感染。它还是 P-糖蛋白底物和抑制剂，IC50为 120 nM。

4-(Imidazol-1-yl)phenol 是一种高效信号增强剂，用于辣根过氧化物酶（HRP）-鲁米诺化学发光（CL）免疫测定。

N-[1-(Aminocarbonyl)-4-[(2-chloro-1-iminoethyl)amino]butyl]benzamide 是Cl-amidine (S 构型)的消旋形式。Cl-amidine 口服有效的 PAD 抑制剂。

TH7127 是一种具有选择性的无菌 α 基序和含组氨酸-天冬氨酸结构域的蛋白-1 （SAMHD1） 抑制剂，抑制 ara-CTP 和 Cl-F-ara-ATP 水解，抑制 SAMHD1 对 dGTP、Cl-F-ara-ATP 和 ara-CTP 的酶活性。

T16Ainh-A01 是氨基苯基噻唑，是有效的跨膜蛋白 16A 的抑制剂，抑制 TMEM16A 介导的氯离子电流，IC50约为1 µM。TMEM16A (ANO1)起钙激活氯离子通道(CaCC)的作用。

CL-387785 (WAY-EKI 785) 是一种不可逆的EGFR 抑制剂，IC50为 370 pM。

RGH-122 (compound 43)是一种口服活性良好、选择性高、有效的V1a拮抗剂，Ki值为0.3 nM。

CK2-IN-9是一种有效的CK2 kinase选择性抑制剂，IC50值为3 nM。它能降低Wnt报告因子的活性，达到IC50为75 nM。在大鼠体内显示出低暴露量（AUC=0.36 μM/h）及高清除率（CL=65 mL/min/kg）。

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 HEK293T cells overexpressing PAD2 when used at concentrations up to 100 μM. However, it can rapidly be photoactivated with UV-A radiation to the more active cis-isomer, which is an irreversible, competitive inhibitor of histone H3 citrullination with an IC50 value of 9.1 μM.References1. Mondal, S., Parelkar, S.S., Nagar, M., et al. Photochemical control of protein arginine deiminase (PAD) activity. ACS Chem. Biol. 13(4), 1057-1065 (2018). 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 HEK293T cells overexpressing PAD2 when used at concentrations up to 100 μM. However, it can rapidly be photoactivated with UV-A radiation to the more active cis-isomer, which is an irreversible, competitive inhibitor of histone H3 citrullination with an IC50 value of 9.1 μM. References1. Mondal, S., Parelkar, S.S., Nagar, M., et al. Photochemical control of protein arginine deiminase (PAD) activity. ACS Chem. Biol. 13(4), 1057-1065 (2018).

Potent and selective inhibitor of the glial glycine transporter GlyT1b (IC50 = 6.9 nM). Displays negligible activity at GlyT-2, adrenoreceptors, dopamine, 5HT receptors and noradrenaline, dopamine, 5HT and GABA transporters (pIC50 in vivo. Chue et al (2013) Glycine reuptake inhibition as a new therapeutic approach in schizophrenia: focus on the glycine transporter 1 (GlyT1). Curr.Pharm.Des. 19 1311 PMID:23194655 |Brown et al (2001) Discovery and SAR of org 24598-a selective glycine uptake inhibitor. Bioorg.Med.Chem.Lett. 11 2007 PMID:11454468 |Williams et al (2003) Development of a scintillation proximity assay for analysis of Na+/Cl- -dependent neurotransmitter transporter activity. Anal. Biochem. 321 31 PMID:12963052

Boc-C1-PEG2-C4-Cl (PROTAC Linker 1) is a PEG-based compound utilized for the synthesis of PROTACs. This chemical compound serves as a linker in the development of PROTACs[1].

VH032-PEG5-C6-Cl (HaloPROTAC 2) is a small molecule HaloPROTAC that incorporates the VH032 based VHL ligand and 5-unit PEG linker. VH032-PEG5-C6-Cl is capable of inducing the degradation of GFP-HaloTag7 in cell-based assays[1].

[D-p-Cl-Phe6,Leu17]-VIP TFA，为竞争性及选择性血管活性肠肽(VIP)受体拮抗剂，其IC50为125.8 nM。该化合物针对胰高血糖素、促胰液素和GRF受体均不表现活性。

Hydrochloride salt of dTAGV-1. Suitable for use in vivo. Following ip administration of 10 mg/kg in mice: T = 4.43 h; Cmax = 2123 ng mL-1; AUCinf = 18517 hr*ng mL-1 and CL = 9.05 mL min-1 kg-1 Negative control dTAGV-1-NEG also available. Important: It is recommended that DMSO stock solutions of this compound are made and used on the same day and are not subjected to freeze/thaw.

U-89843A为GABAA受体的变构调节剂，能够增强GABA诱导的Cl-电流。

IRAK4-IN-25（化合物38）是口服活性IRAK4抑制剂，具有低清除率（Cl=12 mL/min/kg）和IC50值为7.3 nM。它能抑制促炎细胞因子产生，表现出良好的体外安全性和ADME特性。IRAK4-IN-25主要用于研究炎症和自身免疫性疾病。

YW3-56 is a potent peptidylarginine deiminase (PAD) inhibitor, with an IC50 of 1-5 μM for PAD4. Compared with Cl-amidine, YW3-56 shows >60-fold increase in cell growth inhibition efficacy (IC50 about 2.5 μM) but only 5-fold increase in PAD4 inhibition (IC sub>50 about 1-5 μM). At 2-4 μM concentrations, YW3-56 displays mainly cytostatic effects by slowing cell division, whereas at higher concentrations, it exerts cytotoxic effects by altering cell morphology and killing cells[1]. [1]. Wang Y, et al. Anticancer peptidylarginine deiminase (PAD) inhibitors regulate the autophagy flux and t he mammalian target of rapamycin complex 1 activity. J Biol Chem. 2012 Jul 27;287(31):25941-53.

Chlorido[N,N'-disalicylidene-1,2-phenylenediamine]iron(III) is an inducer of ferroptosis.1 It induces ferroptosis, but not apoptosis or necroptosis, in NB1 cancer cells when used at a concentration of 3 μM.1 Chlorido[N,N'-disalicylidene-1,2-phenylenediamine]iron(III) inhibits proliferation of BJAB, NALM-6, Jurkat, MelHO, and MCF-7 cancer cells (IC50s = 0.07, 2.5, 1.5, 3, and 5 μM, respectively), as well as NALM-6 cells resistant to daunorubicin and vincristine when used at concentrations ranging from 0.04 to 0.125 μM.2 |1. Sagasser, J., Ma, B., Baecker, D., et al. A new approach in cancer treatment: Discovery of chlorido[N,N'-disalicylidene-1,2-phenylenediamine]iron(III) complexes as ferroptosis inducers. J. Med. Chem. 62(17), 8053-8061 (2019).|2. Lee, S.-Y., Hille, A., Kitanovic, I., et al. [FeIII(salophene)Cl], a potent iron salophene complex overcomes multiple drug resistance in lymphoma and leukemia cells. Leuk. Res. 35(3), 387-393 (2011).

(S,R,S)-AHPC-(C3-PEG)2-C6-Cl is a small molecule HaloPROTAC incorporating the (S,R,S)-AHPC-based VHL ligand and a 2-unit PEG linker, capable of inducing degradation of GFP-HaloTag7 in cell-based assays [1].

Dox-Ph-PEG1-Cl, also referred to as PROTAC Linker 34, is a PEG-based compound employed for the synthesis of PROTACs[1].

(S,R,S)-AHPC-PEG6-C4-Cl is a small molecule HaloPROTAC that incorporates the (S,R,S)-AHPC based VHL ligand and 6-unit PEG linker. (S,R,S)-AHPC-PEG6-C4-Cl is capable of inducing the degradation of GFP-HaloTag7 in cell-based assays[1].

PAT1inh-B01为选择性SLC26A6抑制剂，抑制PAT1（Cl-/HCO3-交换器）介导的阴离子交换（IC50: 350 nM），并阻断小肠液体吸收，适用于小肠分泌不足相关疾病研究。

5-HT7R antagonist 2 (化合物 4h) 是一种效能显著的5-HT7R拮抗剂。其通过G蛋白和β-阻滞蛋白信号通路实现拮抗作用，对5-HT7R的Ki值达到67 nM。在cAMP和Tango测试中，IC50值分别达到2.59 μM和39.57 μM。此外，5-HT7R antagonist 2对神经发生具有积极影响，能够显著减少自闭症谱系障碍 (ASD) 相关的重复行为，并有助于恢复ASD受损的神经发生。

DOTA-LM3是一款靶向生长抑素受体(SSTR)的拮抗剂，其结构为p-Cl-Phe-cyclo(D-Cys-Tyr-D-4-amino-Phe(carbamoyl)-Lys-Thr-Cys)D-Tyr-NH2。该化合物通常通过同位素标记，如177Lu-DOTA-LM3和68Ga-DOTA-LM3，进行体内肿瘤示踪。68Ga-DOTA-LM3显示出有优异的生物分布特性、高度的肿瘤摄取能力、稳定的肿瘤内保留及较低的安全风险。而177Lu-DOTA-LM3则被用于研究DOTATOC阴性的肝转移案例，针对胰腺NET和广泛性的肿瘤血栓形成治疗具有潜在应用价值。

CC-90005 is a potent, selective and orally active inhibitor of protein kinase C-θ (PKC-θ), with an IC50 of 8 nM. CC-90005 shows selectivity for PKC-θ over PKC-δ (IC50=4440 nM). CC-90005 can inhibit T cell activation by IL-2 expression[1]. CC-90005 shows the exquisite selectivity of CC-90005, with IC50s for all other family members of >3 μM[1].CC-90005 is a moderate inhibitor of both CYP2C9 (IC50=8 μM) and CYP2C19 (IC50=5.9 μM) in human liver microsomes[1].CC-90005 inhibits IL-2 expression in LRS_WBC human PBMCs, with an IC50 of 0.15 μM[1].CC-90005 (1-10 μM; 24 h) inhibits T cell proliferation in PBMCs by 51% at 1 μM and 88% at 3 μM[1]. CC-90005 (3-30 mg kg; p.o. twice daily for 4 days) significantly reduces the popliteal lymph node (PLN) size in a model of chronic T cell activation[1].CC-90005 (100 mg kg; a single p.o.) significantly inhibits plasma and spleen IL-2 release by 51 and 54%, respectively[1].CC-90005 exhibits reasonable oral bioavailability (66 and 46%) and Cmax (1.18 and 1.2 μM) following oral administration (10 and 3 mg kg) in rat and dog, respectively[1].CC-90005 exhibits the mean residence time (0.52 and 2.0 h), CL (69.1 and 20.5 mL min kg) and Vss (2.11 and 2.44 L kg) following intravenous administration (2 and 1 mg kg) in rat and dog, respectively[1]. [1]. Papa P, et, al. Discovery of the Selective Protein Kinase C-θ Kinase Inhibitor, CC-90005. J Med Chem. 2021 Aug 26;64(16):11886-11903.

D-Cl-amidine hydrochloride is a potent and highly selective inhibitor of PAD1. It exhibits excellent tolerance and does not induce significant toxicity [1].

Skullcapflavone I has anti-inflammatory and anti-allergic potential, it can significantly inhibit LPS stimulated NO and PGE(2) release in J774A.1 macrophages and inhibit LPS induced IL-6 production in a concentration dependent manner. Skullcapflavone I se

DCEBIO 是1-EBIO 的衍生物，是 T84 结肠细胞中Cl-分泌的极有效的激活剂。DCEBIO 通过激活 hIK1 K+通道和顶端膜的 Cl-传导促进 Cl-的分泌。

CL 316243 free acid 在大鼠心脏和比目鱼肌的IC 50 值分别为0.6 μM 和1 μM。此化合物还能抑制大鼠逼尿肌条的自发收缩，在浓度依赖性的条件下，其平均浓度在抑制最大反应50%时为2.65 nM。

A3AR modulator 1 (MRS8054) 是口服活性 A3 腺苷受体 (A3AR(Adenosine Receptor)) 正变构调节剂 (PAM)。该化合物显著增强 Cl-IB-MECA 刺激的 [35S]GTPγS 结合 Emax。

CL 82198 hydrochloride is a selective inhibitor of MMP-13 (89% inhibition at 10μg/mL) that displays no activity at MMP-1, MMP-9 or TACE. Inhibitsin vitroinvasion by the human pituitary adenoma cell line HP75. Rescues paclitaxel induced axon degradation and reduces associated neurotoxicity in zebrafish.

PT4 可治疗皮肤利什曼病 (CL) ，它通过降低线粒体膜电位并增加活性氧的产生，从而寄生虫死亡。PT4 对两种利什曼原虫均产生效果，其对L. amazonensis 和L. braziliensis 的 IC50值分别为 125.18 和 233.18 μM。PT4 同时在体内具有有效的抗炎活性。

Etoxadrol (CL-1848C) 是一个有效且高亲和性的 N-methyl-D-aspartic acid (NMDA) 拮抗剂，可用于麻醉研究。

Azido-PEG1-CH2COO-Cl (compound 43a) is an alkyl ether-based PROTAC linker, commonly employed in the synthesis of PROTAC BRD4 Degrader-1[1].

(S,R,S)-AHPC-PEG2-C4-Cl is a small molecule HaloPROTAC that incorporates the (S,R,S)-AHPC based VHL ligand and 2-unit PEG linker. (S,R,S)-AHPC-PEG2-C4-Cl is capable of inducing the degradation of GFP-HaloTag7 in cell-based assays[1].

Mc-O-Si(di-iso)-Cl is a cleavable ADC linker, commonly employed in the synthesis of antibody-drug conjugates (ADCs) like Gemcitabine-O-Si(di-iso)-O-Mc [1].

DOTA-LM3 TFA是一種特定結合生長抑素受體(SSTR)的拮抗劑。其結構為p-Cl-Phe-cyclo(D-Cys-Tyr-D-4-amino-Phe(carbamoyl)-Lys-Thr-Cys)D-Tyr-NH2。這種複合物常以177Lu-DOTA-LM3 TFA和68Ga-DOTA-LM3 TFA的形式被同位素標記，用於腫瘤的體內示踪。68Ga-DOTA-LM3 TFA展示了優異的生物分布特性、高腫瘤吸收率、良好的腫瘤保留性以及較低的安全風險。而177Lu-DOTA-LM3 TFA則被用於研究DOTATOC陰性的肝轉移，例如胰腺神經內分泌腫瘤(NET)和廣泛的腫瘤血栓形成。

(5-Cl)-Exatecan (compound 1-5) 作为一种ADC细胞毒素，主要用于癌症研究。它是一种高效的DNA拓扑异构酶抑制剂。

cDPCP is a platinum-containing DNA-crosslinking agent.1Unlike cisplatin or oxaliplatin , cDPCP forms monofunctional DNA adducts. It is transported into cells by organic cation transporter 1 (OCT1) and OCT2, inhibiting proliferation of MDCK cells expressing the human transporters with IC50values of 8.1 and 1.5 μM, respectively. cDPCP inhibits RNA polymerase II-mediated transcription in a reporter assay using HeLa cells. It increases survival in murine S180 sarcoma and P388 leukemia models when administered at doses of 40 and 80 mg/kg, respectively.2 1.Lovejoy, K.S., Todd, R.C., Zhang, S., et al.cis-Diammine(pyridine)chloroplatinum(II), a monofunctional platinum(II) antitumor agent: Uptake, structure, function, and prospectsProc. Natl. Acad. Sci. USA105(26)8902-9807(2008) 2.Hollis, L.S., Amundsen, A.R., and Stern, E.W.Chemical and biological properties of a new series of cis-diammineplatinum(II) antitumor agents containing three nitrogen donors: cis-[Pt(NH3)2(N-donor)Cl]+J. Med. Chem.32128-136(1989)

Desacetyl bisacodyl为泻药比沙可啶的活性代谢产物，可诱导大鼠结肠及直肠上皮Cl(-)分泌增加，对结肠或直肠产生多种作用，包括促进粘液及氯化物的分泌。

LB244为BB-Cl-amidine的同系物，为口服有效的STING抑制剂（EC50=0.8 μM），适用于治疗STING依赖性炎症性疾病。药代动力学研究表明，LB244在小鼠中的口服活性受限。

BB-Cl-Amidine hydrochloride 是一种肽基精氨酸脱胺酶(PAD)的抑制剂。

CL-329167, a angiotensin type 1 receptor antagonist, is used potentially for the treatment of hypertension.

BMS-665053 is a corticotropin-releasing factor-1 (CRF1) receptor antagonist (IC50 = 1.0 nM). BMS-665053)11 is a potent inhibitor of CRF-stimulated cyclic adenosine monophosphate (cAMP) production in human Y-79 retinoblastoma cells (IC50 = 4.9 nM). In addi

Fludarabine-Cl 抑制 RNA 腺苷脱氨酶1 (ADAR1) ，它可用于预防和/或治疗与肿瘤或癌症相关的疾病。