hydrochloride hydrate

The methylation of lysine residues on histones plays a central role in determining euchromatin structure and gene expression. The histone methyltransferase (HMTase) G9a can mono- or dimethylate lysine 9 on histone 3 (H3), contributing to early embryogenesis, genomic imprinting, and lymphocyte development. BIX01294 (hydrochloride hydrate) is a selective inhibitor of G9a HMTase (IC50 = 1.7 μM). It less effectively inhibits the HMTase G9a-like protein (GLP; IC50 = 38 μM) and has no effect on other known HMTases. BIX01294 has been used in combination with the calcium channel activator BayK8644 to facilitate the generation of induced pluripotent stem cells from somatic cells in vitro.

A-943931 is a histamine H4receptor antagonist (Ki= 3.8 nM).1In vivo, A-943931 inhibits scratching induced by clobenpropit in mice (ED50= 26 μmoles/kg, i.p.). 1.Milicic, I., Witte, D.G., Miller, T.L., et al.Identification of two potent and selective histamine H4 receptor antagonists with antipruritic activityFASEB J.23(S1)760.768-760.768(2009)

NG 25 is a type II kinase inhibitor that inhibits MAP4K2 and TAK1 (IC50s = 21.7 and 149 nM, respectively).1It also inhibits the Src family kinases Src and LYN (IC50s = 113 and 12.9 nM, respectively) and Abl family kinases (IC50s = 75.2 nM), as well as CSK, FER, and p38α (IC50s = 56.4, 82.3, and 102 nM, respectively). NG 25 (100 nM) prevents TNF-α-induced IKKα/β phosphorylation and IκB-α degradation in L929 cells. It inhibits secretion of IFN-α and IFN-β induced by CpG type B and CL097, respectively, in Gen2.2 cells in a concentration-dependent manner.2NG 25 decreases cell viability of HCT116KRASWT, and to a greater degree of HCT116KRASG13D, colorectal cancer cells in a concentration-dependent manner.3It also reduces tumor growth and increases the number of TUNEL-positive tumor cells in a CT26KRASG12Dmouse orthotopic model of colorectal cancer. 1.Tan, L., Nomanbhoy, T., Gurbani, D., et al.Discovery of type II inhibitors of TGFβ-activated kinase 1 (TAK1) and mitogen-activated protein kinase kinase kinase kinase 2 (MAP4K2)J. Med. Chem.58(1)183-196(2015) 2.Pauls, E., Shpiro, N., Peggie, M., et al.Essential role for IKKβ in production of type 1 interferons by plasmacytoid dendritic cellsJ. Biol. Chem. 287(23)19216-19228(2012) 3.Ma, Q., Gu, L., Liao, S., et al.NG25, a novel inhibitor of TAK1, suppresses KRAS-mutant colorectal cancer growth in vitro and in vivoApoptosis24(1-2)83-94(2019)

Kasugamycin hydrochloride hydrate (Ksg (hydrochloride hydrate)) 是一种能结合 30s 和 70s 核糖体，但不能结合 50s 亚基的抗生素。它模拟 mRNA 核苷酸破坏 tRNA 结合并抑制典型翻译起始。

Valacyclovir hydrochloride hydrate 是一种有效的抗病毒剂，是一种前药，在体内可快速转化为阿昔洛韦。Valacyclovir hydrochloride hydrate 能够用于配制治疗眼部疱疹的眼部插入物。Valacyclovir hydrochloride hydrate 能够用于单纯疱疹、带状疱疹和乙型疱疹的治疗。

Iptacopan hydrochloride hydrate is a highly potent and highly selective factor B inhibitor.

CX-6258 hydrochloride hydrate 是强效的、选择性的 pan-Pim 激酶抑制剂，能够作用于 Pim-1 (IC50: 5 nM)、 Pim-2 (IC50: 25 nM) 和 Pim-3 (IC50: 16 nM)。

Zimeldine hydrochloride hydrate is a serotonin uptake inhibitor that was formerly used for depression but was withdrawn worldwide in September 1983 because of the risk of Guillain-Barre Syndrome associated with its use.

p-NH2-Bn-NOTA (hydrochloride hydrate) 是一种用于肿瘤预靶向的双功能螯合剂 (Bifunctional Chelator; BFC)，并且是一种大环 NOTA 衍生物。它可用于多肽和放射性核素的偶联。

MCI-225 is a norepinephrine reuptake 5-HT3 5-HT reuptake inhibitor. MCI-225 could be effective in the treatment of senile dementia of the Alzheimer type, which is accompanied with both deficit in the BF-cortex cholinergic neuron and cerebral glucose hypom

Bepridil hydrochloride hydrate ((±)-Bepridil hydrochloride hydrate) 是一种长效的、非选择性的钙离子通道 (Ca+channel) 拮抗剂。Bepridil hydrochloride hydrate 是一种钠离子、钾离子通道 (Na+,K+channel) 抑制剂，也是心脏 Na+ Ca2+交换 (NCX1) 抑制剂。Bepridil hydrochloride hydrate 具有抗心绞痛和抗 I 型心律失常作用，能够用于研究心血管疾病。

Zoniporide hydrochloride hydrate is a potent and selective sodium-hydrogen exchanger type 1 (NHE-1) inhibitor. Zoniporide hydrochloride hydrate inhibits human NHE-1 with IC50 of 14 nM.

2-Amino-3-mercaptopropanoic acid hydrochloride hydrate 是一种有用的有机化合物，可用于生命科学领域的相关研究。其产品编号为 T64500，CAS号为 116797-51-4。

Tiagabine hydrochloride hydrate 是一种有效、选择性的 GABA uptake 抑制剂；在突触体、神经元和神经胶质中，能够抑制 [3H] GABA 的摄取，他们的 IC50 值分别为 67，446 和 182 nM。Tiagabine hydrochloride hydrate 能够用作抗惊厥剂。

PKRA83 hydrochloride hydrate是一种高效的促动力拮抗剂，与PK2及其受体PKR1和PKR2进行竞争性结合。该化合物在抑制PK2受体方面表现出色，其对PKR1和PKR2的IC50值分别为5.0 nM和8.2 nM。此外，PKRA83 hydrochloride hydrate还具备抗癌、抗关节炎以及抗血管生成的活性，并能够穿透血脑屏障。

(S)-2-Amino-3-mercaptopropanoic acid hydrochloride hydrate 是一种有用的有机化合物，可用于生命科学领域的相关研究。其产品编号为 T66658，CAS号为 207121-46-8。

CDK7-IN-2 hydrochloride hydrate (Example 6) is a highly effective and specific inhibitor of the CDK7 enzyme. This compound exhibits significant anti-cancer properties.

LP 12 hydrochloride hydrate 是一种选择性的、有效的 5-HT7 受体激动剂 (Ki: 0.13 nM)。LP 12 hydrochloride hydrate 对 5-HT7 的选择性高于 D2 受体 (Ki: 224 nM)、5-HT1A 受体 (Ki: 60.9 nM) 和 5-HT2A 受体 (Ki>1000 nM)。

N2-Boc-L-arginine Hydrochloride Hydrate 是一种有用的有机化合物，可用于生命科学领域的相关研究。其产品编号为 T65690，CAS号为 114622-81-0。

Topotecan hydrochloride hydrate 是一种口服具有活力的拓扑异构酶 I (Topoisomerase I) 抑制剂，具有抗癌作用。Topotecan hydrochloride hydrate 能够将细胞周期阻滞在 G0 G1 和 S 期，并诱导细胞凋亡。

p-NH2-CHX-A -DTPA (hydrochloride hydrate)是一种双功能螯合剂 (Bifunctional Chelator; BFC)，作为大环 DTPA 衍生物，可用于肿瘤的预靶向以及在多肽和放射性核素之间进行偶联。

Fedratinib hydrochloride hydrate (SAR 302503 hydrochloride hydrate) 是一种选择性的，ATP 竞争性和具有口服活性的JAK2抑制剂，对于JAK2和JAK2V617F 激酶的IC50均为 3 nM。它可诱导癌细胞凋亡，可研究骨髓增生性疾病。

TETA hydrochloride hydrate 是一种高效的、专一性针对铜 (II) 的选择性螯合剂，适用于药物耦联。

Fasudil hydrochloride hydrate is an HCl salt of Fasudil -- a Rho-kinase (ROCK) inhibitor that has been shown to be effective in hindering the development of mature Cerebral Cavernous Malformation (CCM) lesions as well as reducing portal venous pressure in cirrhotic rats.